| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| Ab098463-10μl | 10μl | In stock | $66.90 | |
| Ab098463-50μl | 50μl | In stock | $189.90 | |
| Ab098463-100μl | 100μl | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $299.90 | |
| Ab098463-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,299.90 |
Recombinant; Rabbit anti Human Cyclin E1 Antibody; WB; Unconjugated
| Product Name | Recombinant Cyclin E1 Antibody - Primary antibody, specific to Cyclin E1, Rabbit IgG |
|---|---|
| Synonyms | CCNE antibody | Ccne1 antibody | CCNE1_HUMAN antibody | cyclin E variant ex5del antibody | cyclin E variant ex7del antibody | Cyclin E1 antibody | Cyclin Es antibody | Cyclin Et antibody | CyclinE antibody | G1/S specific cyclin E antibody | G1/S-specific |
| Specifications & Purity | ExactAb™, Validated, Recombinant, 1.0 mg/mL |
| Host species | Rabbit |
| Specificity | Cyclin E1 |
| Immunogen | A synthetic peptide derived from human Cyclin E1 (AA 393-410). |
| Positive Control | WB: K562, HeLa, MCF7, Hep G2 and HT-29 cell lysates. |
| Conjugation | Unconjugated |
| Grade | ExactAb™, Recombinant, Validated |
| Product Description | Rabbit anti Human Cyclin E1 Antibody, Recombinant, could be used for WB and so on. |
| Isotype | Rabbit IgG |
|---|---|
| SDS-PAGE | 150 kDa |
| Purification Method | Antigen affinity purified |
| Form | Liquid |
| Concentration | 1.0 mg/mL |
| Storage Temp | Store at -20°C,Avoid repeated freezing and thawing |
| Shipped In | Ice chest + Ice pads |
| Stability And Storage | Store at 4°C short term (1-2 weeks). Store at -20°C long term (24 months). Upon delivery aliquot. Avoid freeze/thaw cycle. |
Recombinant Cyclin E1 Antibody (Ab098463) - Western Blot
All lanes: Recombinant Cyclin E1 Antibody (Ab098463) at 1/1000 dilution
Samples: Lysates at 20 µg per lane
Secondary: Goat Anti-Rabbit IgG H&L (HRP) (Ab170144) at 1/20000 dilution
Predicted band size: 47 kDa
Observed band size: 42, 47 kDa
Exposure time: 200.0 s
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
|---|
| Application | Dilution info |
|---|---|
| WB | 1/500-1/1000"> 1/500-1/1000 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
 ZJ24F0202739 | Certificate of Analysis | Feb 06, 2024 | Ab098463 |
| ZJ24F0202740 | Certificate of Analysis | Feb 06, 2024 | Ab098463 |
| 1. Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR.. (2002) Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.. J Med Chem, 45 (18): (3905-3927). [PMID:12190313] [10.1021/jm0201520] |
| 2. Mettey Y, Gompel M, Thomas V, Garnier M, Leost M, Ceballos-Picot I, Noble M, Endicott J, Vierfond JM, Meijer L. (2003) Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.. J Med Chem, 46 (2): (222-36). [PMID:12519061] [10.1021/op500134e] |
| 3. Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ et al.. (2004) N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.. J Med Chem, 47 (7): (1719-28). [PMID:15027863] [10.1021/op500134e] |
| 4. Albrecht W, Unger A, Bauer SM, Laufer SA. (2017) Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.. J Med Chem, 60 (13): (5290-5305). [PMID:28613871] [10.1021/op500134e] |
| 5. Jorda R, Havlíček L, Šturc A, Tušková D, Daumová L, Alam M, Škerlová J, Nekardová M, Peřina M, Pospíšil T et al.. (2019) 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.. J Med Chem, 62 (9): (4606-4623). [PMID:30943029] [10.1021/acs.jmedchem.9b00189] |
| 6. Pomel V, Klicic J, Covini D, Church DD, Shaw JP, Roulin K, Burgat-Charvillon F, Valognes D, Camps M, Chabert C et al.. (2006) Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.. J Med Chem, 49 (13): (3857-71). [PMID:16789742] [10.1021/op500134e] |
| 7. Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD et al.. (2019) 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.. J Med Chem, 62 (15): (6876-6893). [PMID:31282155] [10.1021/op500134e] |
| 8. Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D et al.. (2020) Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.. J Med Chem, 63 (24): (15564-15590). [PMID:33306391] [10.1021/op500134e] |
| 9. Reddy MV, Akula B, Cosenza SC, Athuluridivakar S, Mallireddigari MR, Pallela VR, Billa VK, Subbaiah DR, Bharathi EV, Vasquez-Del Carpio R et al.. (2014) Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).. J Med Chem, 57 (3): (578-99). [PMID:24417566] [10.1021/op500134e] |
| 10. Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H. (2018) A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.. Eur J Med Chem, 144 (13): (1-28). [PMID:29247857] [10.1021/op500134e] |
| 11. Robert M Rzasa,Matthew R Kaller,Gang Liu,Ella Magal,Thomas T Nguyen,Timothy D Osslund,David Powers,Vincent J Santora,Vellarkad N Viswanadhan,Hui-Ling Wang,Xiaoling Xiong,Wenge Zhong,Mark H Norman. (2007-08-19) Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.. Bioorganic & medicinal chemistry, 15 ((20)): (6574-6595). [PMID:17697781] |
| 12. Xiao-Guang Bai,Dong-Ke Yu,Ju-Xian Wang,Hao Zhang,Hong-Wei He,Rong-Guang Shao,Xue-Mei Li,Yu-Cheng Wang. (2012-10-06) Design, synthesis and anticancer activity of 1-acyl-3-amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives.. Bioorganic & medicinal chemistry letters, 22 ((22)): (6947-6951). [PMID:23036956] |
| 13. Misra RN, Xiao HY, Williams DK, Kim KS, Lu S, Keller KA, Mulheron JG, Batorsky R, Tokarski JS, Sack JS, Kimball SD, Lee FY, Webster KR.. (2004) Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.. Bioorg Med Chem Lett, 14 (11): (2973-2977). [PMID:15125971] [10.1016/j.bmcl.2004.02.105] |
| 14. Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA.. (2004) 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.. J Med Chem, 47 (13): (3367-3380). [PMID:15189033] [10.1021/jm031145u] |
| 15. Helal CJ, Sanner MA, Cooper CB, Gant T, Adam M, Lucas JC, Kang Z, Kupchinsky S, Ahlijanian MK, Tate B, Menniti FS, Kelly K, Peterson M.. (2004) Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.. Bioorg Med Chem Lett, 14 (22): (5521-5525). [PMID:15482916] [10.1016/j.bmcl.2004.09.006] |
| 16. VanderWel SN, Harvey PJ, McNamara DJ, Repine JT, Keller PR, Quin J, Booth RJ, Elliott WL, Dobrusin EM, Fry DW, Toogood PL.. (2005) Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.. J Med Chem, 48 (7): (2371-2387). [PMID:15801830] [10.1021/jm049355+] |
| 17. Krystof V, Cankar P, Frysová I, Slouka J, Kontopidis G, Dzubák P, Hajdúch M, Srovnal J, de Azevedo WF, Orság M, Paprskárová M, Rolcík J, Látr A, Fischer PM, Strnad M.. (2006) 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.. J Med Chem, 49 (22): (6500-6509). [PMID:17064068] [10.1021/jm0605740] |
| 18. Shiradkar MR, Akula KC, Dasari V, Baru V, Chiningiri B, Gandhi S, Kaur R.. (2007) Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease.. Bioorg Med Chem, 15 (7): (2601-2610). [PMID:17291769] [10.1016/j.bmc.2007.01.043] |
| 19. Martínez-Urbina MA, Zentella A, Vilchis-Reyes MA, Guzmán A, Vargas O, Ramírez Apan MT, Ventura Gallegos JL, Díaz E.. (2010) 6-Substituted 2-(N-trifluoroacetylamino)imidazopyridines induce cell cycle arrest and apoptosis in SK-LU-1 human cancer cell line.. Eur J Med Chem, 45 (3): (1211-1219). [PMID:20045224] [10.1016/j.ejmech.2009.11.049] |
| 20. Yu H, Jung Y, Kim H, Lee J, Oh CH, Yoo KH, Sim T, Hah JM.. (2010) 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors.. Bioorg Med Chem Lett, 20 (12): (3805-3808). [PMID:20466542] [10.1016/j.bmcl.2010.04.039] |
| 21. Velankar AD, Quintini G, Prabhu A, Weber A, Hunaeus G, Voland B, Wuest M, Orjeda C, Harel D, Varghese S, Gore V, Patil M, Gayke D, Herdemann M, Heit I, Zaliani A.. (2010) Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).. Bioorg Med Chem, 18 (12): (4547-4559). [PMID:20472447] [10.1016/j.bmc.2010.04.056] |
| 22. MacCallum DE, Melville J, Frame S, Watt K, Anderson S, Gianella-Borradori A, Lane DP, Green SR.. (2005) Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.. Cancer Res, 65 (12): (5399-5407). [PMID:15958589] [10.1158/0008-5472.can-05-0233] |
| 23. Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.. (2011) Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.. Bioorg Med Chem Lett, 21 (1): (315-319). [PMID:21112785] [10.1016/j.bmcl.2010.11.010] |
| 24. Kim MH, Kim M, Yu H, Kim H, Yoo KH, Sim T, Hah JM.. (2011) Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.. Bioorg Med Chem, 19 (6): (1915-1923). [PMID:21353571] [10.1016/j.bmc.2011.01.067] |
| 25. Jorda R, Havlícek L, McNae IW, Walkinshaw MD, Voller J, Sturc A, Navrátilová J, Kuzma M, Mistrík M, Bártek J, Strnad M, Krystof V.. (2011) Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.. J Med Chem, 54 (8): (2980-2993). [PMID:21417417] [10.1021/jm200064p] |
| 26. Shiradkar M, Thomas J, Kanase V, Dighe R.. (2011) Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity.. Eur J Med Chem, 46 (6): (2066-2074). [PMID:21420204] [10.1016/j.ejmech.2011.02.059] |
| 27. Kim H, Kim M, Lee J, Yu H, Hah JM.. (2011) Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.. Bioorg Med Chem, 19 (22): (6760-6767). [PMID:22014755] [10.1016/j.bmc.2011.09.042] |
| 28. Caruso M, Valsasina B, Ballinari D, Bertrand J, Brasca MG, Caldarelli M, Cappella P, Fiorentini F, Gianellini LM, Scolaro A, Beria I.. (2012) 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.. Bioorg Med Chem Lett, 22 (1): (96-101). [PMID:22154349] [10.1016/j.bmcl.2011.11.065] |
| 29. Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM.. (2012) Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.. Bioorg Med Chem Lett, 22 (5): (2015-2019). [PMID:22335895] [10.1016/j.bmcl.2012.01.028] |
| 30. Malmström J, Viklund J, Slivo C, Costa A, Maudet M, Sandelin C, Hiller G, Olsson LL, Aagaard A, Geschwindner S, Xue Y, Vasänge M.. (2012) Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.. Bioorg Med Chem Lett, 22 (18): (5919-5923). [PMID:22889803] [10.1016/j.bmcl.2012.07.068] |
| 31. Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.. (2011) Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).. J Med Chem, 54 (22): (7860-7883). [PMID:22039836] [10.1021/jm200900q] |
| 32. Tell V, Holzer M, Herrmann L, Mahmoud KA, Schächtele C, Totzke F, Hilgeroth A.. (2012) Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.. Bioorg Med Chem Lett, 22 (22): (6914-6918). [PMID:23039927] [10.1016/j.bmcl.2012.09.006] |
| 33. Dolečková I, Cesnek M, Dračinský M, Brynda J, Voller J, Janeba Z, Kryštof V.. (2013) Synthesis and biological evaluation of guanidino analogues of roscovitine.. Eur J Med Chem, 62 (443-452). [PMID:23399722] [10.1016/j.ejmech.2013.01.021] |
| 34. Schonbrunn E, Betzi S, Alam R, Martin MP, Becker A, Han H, Francis R, Chakrasali R, Jakkaraj S, Kazi A, Sebti SM, Cubitt CL, Gebhard AW, Hazlehurst LA, Tash JS, Georg GI.. (2013) Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.. J Med Chem, 56 (10): (3768-3782). [PMID:23600925] [10.1021/jm301234k] |
| 35. Ragab FA, Yahya TA, El-Naa MM, Arafa RK.. (2014) Design, synthesis and structure-activity relationship of novel semi-synthetic flavonoids as antiproliferative agents.. Eur J Med Chem, 82 (506-520). [PMID:24937184] [10.1016/j.ejmech.2014.06.007] |
| 36. Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L.. (2015) Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.. Bioorg Med Chem, 23 (21): (7000-7006). [PMID:26455654] [10.1016/j.bmc.2015.09.038] |
| 37. Gao J, Fang C, Xiao Z, Huang L, Chen CH, Wang LT, Lee KH.. (2015) Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.. Medchemcomm, 6 (3): (444-454). [PMID:25914804] [10.1039/c4md00412d] |
| 38. Aman W, Lee J, Kim M, Yang S, Jung H, Hah JM.. (2016) Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.. Bioorg Med Chem Lett, 26 (4): (1188-1192). [PMID:26810260] [10.1016/j.bmcl.2016.01.037] |
| 39. Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.. (2016) Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.. Bioorg Med Chem Lett, 26 (5): (1443-1451). [PMID:26852363] [10.1016/j.bmcl.2016.01.062] |
| 40. Sonawane YA, Taylor MA, Napoleon JV, Rana S, Contreras JI, Natarajan A.. (2016) Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.. J Med Chem, 59 (19): (8667-8684). [PMID:27171036] [10.1021/acs.jmedchem.6b00150] |
| 41. Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K.. (2016) Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.. Medchemcomm, 7 (8): (1580-1586). [PMID:27746890] [10.1039/C6MD00159A] |
| 42. Li Y, Luo X, Guo Q, Nie Y, Wang T, Zhang C, Huang Z, Wang X, Liu Y, Chen Y, Zheng J, Yang S, Fan Y, Xiang R.. (2018) Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.. J Med Chem, 61 (7): (3166-3192). [PMID:29518312] [10.1021/acs.jmedchem.8b00209] |
| 43. Bharate SB, Kumar V, Jain SK, Mintoo MJ, Guru SK, Nuthakki VK, Sharma M, Bharate SS, Gandhi SG, Mondhe DM, Bhushan S, Vishwakarma RA.. (2018) Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.. J Med Chem, 61 (4): (1664-1687). [PMID:29370702] [10.1021/acs.jmedchem.7b01765] |
| 44. Zhou A, Yan L, Lai F, Chen X, Goto M, Lee KH, Xiao Z.. (2017) Design, synthesis and biological evaluation of novel indolin-2-ones as potent anticancer compounds.. Bioorg Med Chem Lett, 27 (15): (3326-3331). [PMID:28625363] [10.1016/j.bmcl.2017.06.019] |
| 45. Li Y, Guo Q, Zhang C, Huang Z, Wang T, Wang X, Wang X, Xu G, Liu Y, Yang S, Fan Y, Xiang R.. (2017) Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.. Bioorg Med Chem Lett, 27 (15): (3231-3237). [PMID:28651979] [10.1016/j.bmcl.2017.06.041] |
| 46. Wang Y, Zhi Y, Jin Q, Lu S, Lin G, Yuan H, Yang T, Wang Z, Yao C, Ling J, Guo H, Li T, Jin J, Li B, Zhang L, Chen Y, Lu T.. (2018) Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.. J Med Chem, 61 (4): (1499-1518). [PMID:29357250] [10.1021/acs.jmedchem.7b01261] |
| 47. Wang Y, Chen Y, Cheng X, Zhang K, Wang H, Liu B, Wang J.. (2018) Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.. Bioorg Med Chem, 26 (12): (3491-3501). [PMID:29853338] [10.1016/j.bmc.2018.05.024] |
| 48. Farag AK, Elkamhawy A, Londhe AM, Lee KT, Pae AN, Roh EJ.. (2017) Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.. Eur J Med Chem, 141 (657-675). [PMID:29107425] [10.1016/j.ejmech.2017.10.003] |
| 49. Kurasawa O, Oguro Y, Miyazaki T, Homma M, Mori K, Iwai K, Hara H, Skene R, Hoffman I, Ohashi A, Yoshida S, Ishikawa T, Cho N.. (2017) Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.. Bioorg Med Chem, 25 (7): (2133-2147). [PMID:28284870] [10.1016/j.bmc.2017.02.021] |
| 50. Malínková V, Řezníčková E, Jorda R, Gucký T, Kryštof V.. (2017) Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.. Bioorg Med Chem, 25 (24): (6523-6535). [PMID:29089259] [10.1016/j.bmc.2017.10.032] |
| 51. Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.. (2018) Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.. Bioorg Med Chem Lett, 28 (20): (3356-3362). [PMID:30227946] [10.1016/j.bmcl.2018.09.006] |
| 52. Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q.. (2018) Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.. Eur J Med Chem, 158 (896-916). [PMID:30253346] [10.1016/j.ejmech.2018.09.025] |
| 53. Zhang Q, Hu X, Wan G, Wang J, Li L, Wu X, Liu Z, Yu L.. (2019) Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.. Eur J Med Chem, 184 (111728-111728). [PMID:31610375] [10.1016/j.ejmech.2019.111728] |
| 54. Tear WF, Bag S, Diaz-Gonzalez R, Ceballos-Pérez G, Rojas-Barros DI, Cordon-Obras C, Pérez-Moreno G, García-Hernández R, Martinez-Martinez MS, Ruiz-Perez LM, Gamarro F, Gonzalez Pacanowska D, Caffrey CR, Ferrins L, Manzano P, Navarro M, Pollastri MP.. (2020) Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-b]pyridazines for the Treatment of Human African Trypanosomiasis.. J Med Chem, 63 (2): (756-783). [PMID:31846577] [10.1021/acs.jmedchem.9b01741] |
| 55. Rana S, Sonawane YA, Taylor MA, Kizhake S, Zahid M, Natarajan A.. (2018) Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.. Bioorg Med Chem Lett, 28 (23-24): (3736-3740). [PMID:30343954] [10.1016/j.bmcl.2018.10.020] |
| 56. Narayan S, Ramisetti S, Jaiswal AS, Law BK, Singh-Pillay A, Singh P, Amin S, Sharma AK.. (2019) ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.. Eur J Med Chem, 161 (456-467). [PMID:30384048] [10.1016/j.ejmech.2018.10.052] |
| 57. Wang Y, Dou X, Jiang L, Jin H, Zhang L, Zhang L, Liu Z.. (2019) Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.. Eur J Med Chem, 171 (221-234). [PMID:30925338] [10.1016/j.ejmech.2019.03.039] |
| 58. Abdelaziz AM, Basnet SKC, Islam S, Li M, Tadesse S, Albrecht H, Gerber C, Yu M, Wang S.. (2019) Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.. Bioorg Med Chem Lett, 29 (18): (2650-2654). [PMID:31362920] [10.1016/j.bmcl.2019.07.043] |
| 59. Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.. (2019) Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.. J Med Chem, 62 (10): (5096-5110). [PMID:31013427] [10.1021/acs.jmedchem.9b00318] |
| 60. Wang J, Li T, Zhao T, Wu T, Liu C, Ding H, Li Z, Bian J.. (2019) Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.. Eur J Med Chem, 178 (782-801). [PMID:31238183] [10.1016/j.ejmech.2019.06.024] |
| 61. Wang X, Yu C, Wang C, Ma Y, Wang T, Li Y, Huang Z, Zhou M, Sun P, Zheng J, Yang S, Fan Y, Xiang R.. (2019) Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.. Eur J Med Chem, 181 (111535-111535). [PMID:31376566] [10.1016/j.ejmech.2019.07.038] |
| 62. Zhao L, Li Y, Wang Y, Qiao Z, Miao Z, Yang J, Huang L, Tian C, Li L, Chen D, Yang S.. (2019) Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models.. J Med Chem, 62 (23): (10691-10710). [PMID:31693351] [10.1021/acs.jmedchem.9b01143] |
| 63. Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP.. (2019) Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.. Bioorg Med Chem Lett, 29 (16): (2294-2301). [PMID:31307887] [10.1016/j.bmcl.2019.06.021] |
| 64. Khair NZ, Lenjisa JL, Tadesse S, Kumarasiri M, Basnet SKC, Mekonnen LB, Li M, Diab S, Sykes MJ, Albrecht H, Milne R, Wang S.. (2019) Discovery of CDK5 Inhibitors through Structure-Guided Approach.. ACS Med Chem Lett, 10 (5): (786-791). [PMID:31098000] [10.1021/acsmedchemlett.9b00029] |
| 65. Teng Y, Lu K, Zhang Q, Zhao L, Huang Y, Ingarra AM, Galons H, Li T, Cui S, Yu P, Oumata N.. (2019) Recent advances in the development of cyclin-dependent kinase 7 inhibitors.. Eur J Med Chem, 183 (111641-111641). [PMID:31514062] [10.1016/j.ejmech.2019.111641] |
| 66. Sánchez-Martínez C, Lallena MJ, Sanfeliciano SG, de Dios A.. (2019) Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).. Bioorg Med Chem Lett, 29 (20): (126637-126637). [PMID:31477350] [10.1016/j.bmcl.2019.126637] |
| 67. Venkanna A, Cho KH, Dhorma LP, Kumar DN, Hah JM, Park HG, Kim SY, Kim MH.. (2019) Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.. Eur J Med Chem, 163 (453-480). [PMID:30530196] [10.1016/j.ejmech.2018.11.037] |
| 68. Baillache, Daniel J., Unciti-Broceta, Asier. (2020) Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold. RSC Med Chem, 11 (10): (1112-1135). [PMID:33479617] [10.1039/d0md00227e] |
| 69. Said MA,Eldehna WM,Nocentini A,Fahim SH,Bonardi A,Elgazar AA,Kryštof V,Soliman DH,Abdel-Aziz HA,Gratteri P,Abou-Seri SM,Supuran CT. (2020) Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.. Eur J Med Chem, 189 (112019-112019). [PMID:31972394] [10.1016/j.ejmech.2019.112019] |
| 70. Zhang S,Huang C,Lyu X,Wang P,Zang Y,Wang Z,Wang H,Li J,Zhao Y. (2020) Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).. Eur J Med Chem, 195 (112277-112277). [PMID:32289582] [10.1016/j.ejmech.2020.112277] |
| 71. Wu T,Qin Z,Tian Y,Wang J,Xu C,Li Z,Bian J. (2020) Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.. J Med Chem, 63 (22): (13228-13257). [PMID:32866383] [10.1021/acs.jmedchem.0c00744] |
| 72. Ding X,Stasi LP,Ho MH,Zhao B,Wang H,Long K,Xu Q,Sang Y,Sun C,Hu H,Yu H,Wan Z,Wang L,Edge C,Liu Q,Li Y,Dong K,Guan X,Tattersall FD,Reith AD,Ren F. (2018) Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.. Bioorg Med Chem Lett, 28 (9.0): (1615-1620). [PMID:29588215] [10.1016/j.bmcl.2018.03.045] |
| 73. Yu M,Teo T,Yang Y,Li M,Long Y,Philip S,Noll B,Heinemann GK,Diab S,Eldi P,Mekonnen L,Anshabo AT,Rahaman MH,Milne R,Hayball JD,Wang S. (2021) Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.. Eur J Med Chem, 214 (113248-113248). [PMID:33571827] [10.1016/j.ejmech.2021.113248] |
| 74. Yang J,Chen K,Zhang G,Yang QY,Li YS,Huang SZ,Wang YL,Yang W,Jiang XJ,Yan HX,Zhu JQ,Xiang R,Luo YF,Li WM,Wei YQ,Li LL,Yang SY. (2018) Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.. Eur J Med Chem, 143 (1148-1164). [PMID:29133048] [10.1016/j.ejmech.2017.09.018] |
| 75. Xu J,Li H,Wang X,Huang J,Li S,Liu C,Dong R,Zhu G,Duan C,Jiang F,Zhang Y,Zhu Y,Zhang T,Chen Y,Tang W,Lu T. (2020) Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.. Eur J Med Chem, 200 (112424-112424). [PMID:32447197] [10.1016/j.ejmech.2020.112424] |
| 76. Long Y, Yu M, Ochnik AM, Karanjia JD, Basnet SK, Kebede AA, Kou L, Wang S.. (2021) Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.. Eur J Med Chem, 213 (113215-113215). [PMID:33516985] [10.1016/j.ejmech.2021.113215] |
| 77. Lew, D J DJ, Dulić, V V and Reed, S I SI.. (1991) Isolation of three novel human cyclins by rescue of G1 cyclin (Cln) function in yeast.. Cell, (20): [PMID:1833066] |
| 78. Koff, A A and 6 more authors.. (1991) Human cyclin E, a new cyclin that interacts with two members of the CDC2 gene family.. Cell, (20): [PMID:1833068] |
| 79. Ohtsubo, M M, Theodoras, A M AM, Schumacher, J J, Roberts, J M JM and Pagano, M M.. (1995) Human cyclin E, a nuclear protein essential for the G1-to-S phase transition.. Molecular and cellular biology, [PMID:7739542] |
| 80. Sewing, A A, Rönicke, V V, Bürger, C C, Funk, M M and Müller, R R.. (1994) Alternative splicing of human cyclin E.. Journal of cell science, [PMID:8207080] |
| 81. Geng, Y Y and 7 more authors.. (1996) Regulation of cyclin E transcription by E2Fs and retinoblastoma protein.. Oncogene, (21): [PMID:8649818] |
| 82. Li, H H and 6 more authors.. (1996) Molecular cloning and chromosomal localization of the human cyclin C (CCNC) and cyclin E (CCNE) genes: deletion of the CCNC gene in human tumors.. Genomics, (1): [PMID:8833152] |
| 83. Won, K A KA and Reed, S I SI.. (1996) Activation of cyclin E/CDK2 is coupled to site-specific autophosphorylation and ubiquitin-dependent degradation of cyclin E.. The EMBO journal, (15): [PMID:8861947] |
| 84. Zariwala, M M, Liu, J J and Xiong, Y Y.. (1998) Cyclin E2, a novel human G1 cyclin and activating partner of CDK2 and CDK3, is induced by viral oncoproteins.. Oncogene, (26): [PMID:9840943] |
| 85. Welcker, Markus M and 7 more authors.. (2003) Multisite phosphorylation by Cdk2 and GSK3 controls cyclin E degradation.. Molecular cell, [PMID:14536078] |
| 86. Li, Yuanyuan Y, Mori, Tsutomu T, Hata, Hiroaki H, Homma, Yoshimi Y and Kochi, Hideo H.. (2004) NIRF induces G1 arrest and associates with Cdk2.. Biochemical and biophysical research communications, (25): [PMID:15178429] |
| 87. Honda, Reiko R and 6 more authors.. (2005) The structure of cyclin E1/CDK2: implications for CDK2 activation and CDK2-independent roles.. The EMBO journal, (9): [PMID:15660127] |
| 88. Tang, Lin L and 13 more authors.. (2005) Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.. The Journal of biological chemistry, (2): [PMID:15985434] |
| 89. Caligiuri, Maureen M and 11 more authors.. (2005) A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.. Chemistry & biology, [PMID:16242653] |
| 90. Hao, Bing B, Oehlmann, Stephanie S, Sowa, Mathew E ME, Harper, J Wade JW and Pavletich, Nikola P NP.. (2007) Structure of a Fbw7-Skp1-cyclin E complex: multisite-phosphorylated substrate recognition by SCF ubiquitin ligases.. Molecular cell, (13): [PMID:17434132] |
| 91. Dephoure, Noah N and 6 more authors.. (2008) A quantitative atlas of mitotic phosphorylation.. Proceedings of the National Academy of Sciences of the United States of America, (5): [PMID:18669648] |
| 92. Daub, Henrik H and 9 more authors.. (2008) Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle.. Molecular cell, (8): [PMID:18691976] |
| 93. Bäumer, Nicole N and 13 more authors.. (2011) Inhibitor of cyclin-dependent kinase (CDK) interacting with cyclin A1 (INCA1) regulates proliferation and is repressed by oncogenic signaling.. The Journal of biological chemistry, (12): [PMID:21540187] |
| 94. Mori, Tsutomu T, Ikeda, Daisuke D DD, Fukushima, Toshihiko T, Takenoshita, Seiichi S and Kochi, Hideo H.. (2011) NIRF constitutes a nodal point in the cell cycle network and is a candidate tumor suppressor.. Cell cycle (Georgetown, Tex.), (1): [PMID:21952639] |
| 95. Zhou, Houjiang H and 6 more authors.. (2013) Toward a comprehensive characterization of a human cancer cell phosphoproteome.. Journal of proteome research, (4): [PMID:23186163] |
| 96. May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K,Wu P,Xin Z,Burkly LC. (2018) Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.. Bioorg Med Chem Lett, 28 (10): (1964-1971). [PMID:29636220] [10.1016/j.bmcl.2018.03.032] |
