Click Here for 5% Off Your First Aladdin Purchase!

SP600125 - ≥98%, high purity , CAS No.129-56-6, Inhibitor of mitogen-activated protein kinase 10;Inhibitor of mitogen-activated protein kinase 8;Inhibitor of mitogen-activated protein kinase 9

  • Moligand™
  • ≥98%
Item Number
S125267
Grouped product items
SKUSizeAvailabilityPrice Qty
S125267-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$26.90
S125267-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$56.90
S125267-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$88.90
S125267-500mg
500mg
In stock
$177.90
S125267-1g
1g
In stock
$320.90
S125267-5g
5g
In stock
$1,441.90

JNK inhibitor

Basic Description

Synonyms129-56-6|1,9-Pyrazoloanthrone|SP600125|Pyrazolanthrone|Dibenzo[cd,g]indazol-6(2H)-one|Pyrazoleanthrone|SP 600125|Anthra[1,9-cd]pyrazol-6(2H)-one|SP-600125|JNK Inhibitor II|Anthra-1,9-pyrazol-6-none|ANTHRA(1,9-cd)PYRAZOL-6(2H)-ONE|C.I. 70300|2H-Dibenzo[cd,
Specifications & Purity≥98%
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of mitogen-activated protein kinase 10;Inhibitor of mitogen-activated protein kinase 8;Inhibitor of mitogen-activated protein kinase 9
Product Description

SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc.
A potent, selective and reversible inhibitor of JNK1, JNK-2, and JNK-3

Associated Targets

MAPK10 Tchem Mitogen-activated protein kinase 10 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK8 Tchem Mitogen-activated protein kinase 8 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK9 Tchem Mitogen-activated protein kinase 9 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one
INCHI InChI=1S/C14H8N2O/c17-14-9-5-2-1-4-8(9)13-12-10(14)6-3-7-11(12)15-16-13/h1-7H,(H,15,16)
InChi Key ACPOUJIDANTYHO-UHFFFAOYSA-N
Canonical SMILES C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O
Isomeric SMILES C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O
PubChem CID 8515
Molecular Weight 220.233

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

6 results found

Lot NumberCertificate TypeDateItem
L1805123Certificate of AnalysisMay 14, 2024 S125267
L1805121Certificate of AnalysisMay 14, 2024 S125267
F2209263Certificate of AnalysisMar 20, 2024 S125267
F2209277Certificate of AnalysisMar 20, 2024 S125267
F2209285Certificate of AnalysisMar 20, 2024 S125267
A2125110Certificate of AnalysisNov 16, 2022 S125267

Chemical and Physical Properties

SolubilityDMSO ≥42mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
SensitivityHeat Sensitive
Melt Point(°C)283°C

Related Documents

References

1. Bennett BL, Sasaki DT, Murray BW, O'Leary EC, Sakata ST, Xu W, Leisten JC, Motiwala A, Pierce S, Satoh Y et al..  (2001)  SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase..  Proc Natl Acad Sci USA,  98  (24): (13681-6).  [PMID:11717429]
2. Joiakim A, Mathieu PA, Palermo C, Gasiewicz TA, Reiners Jr JJ.  (2003)  The Jun N-terminal kinase inhibitor SP600125 is a ligand and antagonist of the aryl hydrocarbon receptor..  Drug Metab Dispos,  31  (11): (1279-82).  [PMID:14570754]
3. Schmidt M, Budirahardja Y, Klompmaker R, Medema RH.  (2005)  Ablation of the spindle assembly checkpoint by a compound targeting Mps1..  EMBO Rep,  (9): (866-72).  [PMID:16113653]
4. Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U et al..  (2010)  Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase..  Cancer Res,  70  (24): (10255-64).  [PMID:21159646]
5. Cheng CY et al..  (2021)  Alpinia oxyphylla Miq extract reduces cerebral infarction by downregulating JNK-mediated TLR4/T3JAM- and ASK1-related inflammatory signaling in the acute phase of transient focal cerebral ischemia in rats..  Chin Med,  16  (82).  [PMID:34419138]
6. Fukami T et al..  (2022)  Anoctamin 5 regulates the cell cycle and affects prognosis in gastric cancer..  World J Gastroenterol,  28  (32): (4649-4667).  [PMID:36157935]
7. Hao D et al..  (2021)  Baicalin alleviates chronic obstructive pulmonary disease through regulation of HSP72-mediated JNK pathway..  Mol Med,  27  (53).  [PMID:34053448]
8. Singh TD et al..  (2015)  Anticancer properties and enhancement of therapeutic potential of cisplatin by leaf extract of Zanthoxylum armatum DC..  Biol Res,  48  (46).  [PMID:26290043]
9. Joung EJ et al..  (2012)  Anti-inflammatory effect of ethanolic extract from Myagropsis myagroides on murine macrophages and mouse ear edema..  BMC Complement Altern Med,  12  (171).  [PMID:23031211]
10. Muramatsu D et al..  (2017)  Aureobasidium pullulans produced ß-glucan is effective to enhance Kurosengoku soybean extract induced Thrombospondin-1 expression..  Sci Rep,  (2831).  [PMID:28588201]
11. Liu Y et al..  (2019)  c-Jun N-terminal kinase/transforming growth factor-ß/Smad3 pathway: Is it associated with endoplasmic reticulum stress-mediated renal interstitial fibrosis?.  Mol Med Rep,  20  (755-762).  [PMID:31180530]
12. Nunes JPS et al..  (2021)  Co-Exposure of Cardiomyocytes to IFN-? and TNF-a Induces Mitochondrial Dysfunction and Nitro-Oxidative Stress: Implications for the Pathogenesis of Chronic Chagas Disease Cardiomyopathy..  Front Immunol,  12  (755862).  [PMID:34867992]
13. Ivshina MP et al..  (2022)  CPEB1 regulates the inflammatory immune response, phagocytosis, and alternative polyadenylation in microglia..  Glia,  70  (10): (1850-1863).  [PMID:35635122]
14. Lee CW et al..  (2017)  DNA Methyltransferases Modulate Hepatogenic Lineage Plasticity of\xa0Mesenchymal Stromal Cells..  Stem Cell Reports,  (247-263).  [PMID:28602611]
15. Gao S et al..  (2023)  Effects of Holliday Junction-Recognition Protein-Mediated C-Jun N-Terminal Kinase/ Signal Transducer and Activator of Transcription 3 Signaling Pathway on Cell Proliferation, Cell Cycle and Cell Apoptosis in Bladder Urothelial Carcinoma..  Tohoku J Exp Med,  259  (3): (209-219).  [PMID:36543245]
16. Lanfranco MF et al..  (2021)  Expression and secretion of apoE isoforms in astrocytes and microglia during inflammation..  Glia,  69  (6): (1478-1493).  [PMID:33556209]
17. Barakat TS et al..  (2018)  Functional Dissection of the Enhancer Repertoire in Human Embryonic Stem Cells..  Cell Stem Cell,  23  (2): (276-288.e8).  [PMID:30033119]
18. Wang G et al..  (2022)  Exenatide exerts a neuroprotective effect against diabetic cognitive impairment in rats by inhibiting apoptosis: Role of the JNK/c-JUN signaling pathway..  Mol Med Rep,  25  (4):   [PMID:35119079]
19. Aguado J et al..  (2021)  Inhibition of the cGAS-STING pathway ameliorates the premature senescence hallmarks of Ataxia-Telangiectasia brain organoids..  Aging Cell,  20  (9): (e13468).  [PMID:34459078]
20. Chu X et al..  (2021)  JNK/c-Jun-driven NLRP3 inflammasome activation in microglia contributed to retinal ganglion cells degeneration induced by indirect traumatic optic neuropathy..  Exp Eye Res,  202  (108335).  [PMID:33141050]
21. Lv YC et al..  (2020)  Long-term adenosine A1 receptor activation-induced sortilin expression promotes a-synuclein upregulation in dopaminergic neurons..  Neural Regen Res,  15  (4): (712-723).  [PMID:31638096]
22. Flocke LS et al..  (2016)  Molecular mode of action of NKP-1339 - a clinically investigated ruthenium-based drug - involves ER- and ROS-related effects in colon carcinoma cell lines..  Invest New Drugs,  34  (3): (261-8).  [PMID:26988975]
23. Levitt ES & Williams JT.  (2012)  Morphine desensitization and cellular tolerance are distinguished in rat locus ceruleus neurons..  Mol Pharmacol,  82  (5): (983-92).  [PMID:22914548]
24. Lan CN et al..  (2021)  MAPK inhibitors protect against early-stage osteoarthritis by activating autophagy..  Mol Med Rep,  24  (6):   [PMID:34590154]
25. Liu X et al..  (2015)  Mechanical Tension Promotes the Osteogenic Differentiation of Rat Tendon-derived Stem Cells Through the Wnt5a/Wnt5b/JNK Signaling Pathway..  Cell Physiol Biochem,  36  (2): (517-30).  [PMID:25966835]
26. Chu CH et al..  (2016)  Neurons and astroglia govern microglial endotoxin tolerance through macrophage colony-stimulating factor receptor-mediated ERK1/2 signals..  Brain Behav Immun,  55  (260-72).  [PMID:27132056]
27. Zhang Q et al..  (2013)  NF-?B, ERK, p38 MAPK and JNK contribute to the initiation and/or maintenance of mechanical allodynia induced by tumor necrosis factor-alpha in the red nucleus..  Brain Res Bull,  99  (132-9).  [PMID:24161765]
28. Lu YQ et al..  (2017)  NLRP3 inflammasome activation results in liver inflammation and fibrosis in mice infected with Schistosoma japonicum in a Syk-dependent manner..  Sci Rep,  (8120).  [PMID:28808303]
29. Hu X et al..  (2022)  Operation of the Atypical Canonical Bone Morphogenetic Protein Signaling Pathway During Early Human Odontogenesis..  Front Physiol,  13  (823275).  [PMID:35211032]
30. Li H et al..  (2018)  p38 MAPK-MK2 pathway regulates the heat-stress-induced accumulation of reactive oxygen species that mediates apoptotic cell death in glial cells..  Oncol Lett,  15  (775-782).  [PMID:29387240]
31. Guo YJ et al..  (2018)  Red nucleus interleukin-1ß evokes tactile allodynia through activation of JAK/STAT3 and JNK signaling pathways..  J Neurosci Res,  96  (12): (1847-1861).  [PMID:30216497]
32. Zhang J et al..  (2022)  Resveratrol inhibits hepatic stellate cell activation by regulating autophagy and apoptosis through the SIRT1 and JNK signaling pathways..  J Food Biochem,  46  (12): (e14463).  [PMID:36314441]
33. Kim HJ et al..  (2012)  Reverse signaling through the costimulatory ligand CD137L in epithelial cells is essential for natural killer cell-mediated acute tissue inflammation..  Proc Natl Acad Sci U S A,  109  (E13-22).  [PMID:22160719]
34. Dong H et al..  (2019)  Role of FOXO3 Activated by HIV-1 Tat in HIV-Associated Neurocognitive Disorder Neuronal Apoptosis..  Front Neurosci,  13  (44).  [PMID:30778283]
35. Caunt CJ et al..  (2008)  Spatiotemporal regulation of ERK2 by dual specificity phosphatases..  J Biol Chem,  283  (39): (26612-23).  [PMID:18650424]
36. Kang K & Wang Y.  (2019)  Sevoflurane Inhibits Proliferation and Invasion of Human Ovarian Cancer Cells by Regulating JNK and p38 MAPK Signaling Pathway..  Drug Des Devel Ther,  13  (4451-4460).  [PMID:32021086]
37. Lin CC et al..  (2021)  Terminal uridyltransferase 7 regulates TLR4-triggered inflammation by controlling Regnase-1 mRNA uridylation and degradation..  Nat Commun,  12  (3878).  [PMID:34188032]
38. Zhang J et al..  (2021)  TGF-ß1-induced autophagy activates hepatic stellate\xa0cells via the ERK and JNK signaling pathways..  Int J Mol Med,  47  (256-266).  [PMID:33236148]
39. Alhuthali HM et al..  (2020)  The natural alkaloid Jerantinine B has activity in acute myeloid leukemia cells through a mechanism involving c-Jun..  BMC Cancer,  20  (629).  [PMID:32635894]
40. Trondl R et al..  (2014)  Triapine and a more potent dimethyl derivative induce endoplasmic reticulum stress in cancer cells..  Mol Pharmacol,  85  (3): (451-9).  [PMID:24378333]
41. Woida PJ & Satchell KJF.  (2020)  The Vibrio cholerae MARTX toxin silences the inflammatory response to cytoskeletal damage before inducing actin cytoskeleton collapse..  Sci Signal,  13  (614):   [PMID:31937566]

Solution Calculators