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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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C125082-5mg | 5mg | In stock | $70.90 | |
C125082-25mg | 25mg | In stock | $319.90 | |
C125082-100mg | 100mg | In stock | $509.90 | |
C125082-500mg | 500mg | In stock | $2,295.90 |
Highly selective GSK-3 inhibitor; acts as Wnt activator
Synonyms | 252917-06-9 | CHIR-99021 | CHIR99021 | laduviglusib | CHIR 99021 | CT99021 | CT-99021 | 6-((2-((4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile | GSK-3 Inhibitor XVI | CHIR-911 | 6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent and highly selective inhibitor of glycogen synthase kinase 3 (GSK-3) (IC50values are 6.7 and 10 nM for GSK-3β and GSK-3α respectively). Acts as Wnt activator. Exhibits >500-fold selectivity for GSK-3 over closely related kinases; also displays >800 |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of cyclin dependent kinase 1;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of mitogen-activated protein kinase 1 |
Product Description | CHIR-99021 (CT99021) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. IC50 value: 10 nM/6.7 nM for GSK-3α/β . |
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IUPAC Name | 6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile |
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INCHI | InChI=1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32) |
InChi Key | AQGNHMOJWBZFQQ-UHFFFAOYSA-N |
Canonical SMILES | CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N |
Isomeric SMILES | CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N |
PubChem CID | 9956119 |
Molecular Weight | 465.34 |
Reaxy-Rn | 25763160 |
PubChem CID | 9956119 |
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CAS Registry No. | 252917-06-9 |
ChEMBL Ligand | CHEMBL412142 |
RCSB PDB Ligand | 65C |
Reactome Reaction | R-HSA-9687724 |
Reactome Drug | R-ALL-9687650 |
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Lot Number | Certificate Type | Date | Item |
---|---|---|---|
K2212430 | Certificate of Analysis | Aug 23, 2024 | C125082 |
K2212733 | Certificate of Analysis | Aug 23, 2024 | C125082 |
K2212752 | Certificate of Analysis | Aug 23, 2024 | C125082 |
K2126055 | Certificate of Analysis | Sep 12, 2023 | C125082 |
F23151064 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151069 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151070 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151072 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151073 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151075 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151091 | Certificate of Analysis | Jun 02, 2023 | C125082 |
F23151092 | Certificate of Analysis | Jun 02, 2023 | C125082 |
B1525008 | Certificate of Analysis | Sep 13, 2022 | C125082 |
K2212734 | Certificate of Analysis | Jul 20, 2022 | C125082 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 9.31, Max Conc. mM: 20 |
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Sensitivity | Heat Sensitive |
Pictogram(s) | GHS06, GHS07 |
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Signal | Danger |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H300:Fatal if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
Reaxy-Rn | 25763160 |
Starting at $333.90
Starting at $169.90
1. Xuan Ren, Jianchun Xu, Qingsong Xue, Yi Tong, Tairan Xu, Jinli Wang, Ting Yang, Yuan Chen, Deshun Shi, Xiangping Li. (2024) BRG1 enhances porcine iPSC pluripotency through WNT/β-catenin and autophagy pathways. THERIOGENOLOGY, 215 (22): (10). [PMID:38000125] |
1. Eldar-Finkelman H, Schreyer SA, Shinohara MM, LeBoeuf RC, Krebs EG. (1999) Increased glycogen synthase kinase-3 activity in diabetes- and obesity-prone C57BL/6J mice.. Diabetes, 48 (8): (1662-6). [PMID:10426388] |
2. Nikoulina SE, Ciaraldi TP, Mudaliar S, Mohideen P, Carter L, Henry RR. (2000) Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes.. Diabetes, 49 (2): (263-71). [PMID:10868943] |
3. Ring DB, Johnson KW, Henriksen EJ, Nuss JM, Goff D, Kinnick TR, Ma ST, Reeder JW, Samuels I, Slabiak T et al.. (2003) Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.. Diabetes, 52 (3): (588-95). [PMID:12606497] |
4. Cai Z, Zhao Y, Zhao B. (2012) Roles of glycogen synthase kinase 3 in Alzheimer's disease.. Curr Alzheimer Res, 9 (7): (864-79). [PMID:22272620] |
5. Hurtado DE, Molina-Porcel L, Carroll JC, Macdonald C, Aboagye AK, Trojanowski JQ, Lee VM. (2012) Selectively silencing GSK-3 isoforms reduces plaques and tangles in mouse models of Alzheimer's disease.. J Neurosci, 32 (21): (7392-402). [PMID:22623685] |
6. An WF, Germain AR, Bishop JA, Nag PP, Metkar S, Ketterman J, Walk M, Weiwer M, Liu X, Patnaik D et al.. (2010) Discovery of Potent and Highly Selective Inhibitors of GSK3b. Probe Reports from the NIH Molecular Libraries Program, 129 (3): (589-97). [PMID:23658955] |
7. Chai G, Szenker-Ravi E, Chung C, Li Z, Wang L, Khatoo M, Marshall T, Jiang N, Yang X, McEvoy-Venneri J et al.. (2021) A Human Pleiotropic Multiorgan Condition Caused by Deficient Wnt Secretion.. N Engl J Med, 385 (14): (1292-1301). [PMID:34587386] |
8. Badimon L, Casaní L, Camino-Lopez S, Juan-Babot O, Borrell-Pages M. (2019) GSK3β inhibition and canonical Wnt signaling in mice hearts after myocardial ischemic damage.. PLoS ONE, 14 (6): (e0218098). [PMID:31220102] |
9. Yoshida Y, Soma T, Matsuzaki T, Kishimoto J. (2019) Wnt activator CHIR99021-stimulated human dermal papilla spheroids contribute to hair follicle formation and production of reconstituted follicle-enriched human skin.. Biochem Biophys Res Commun, 516 (3): (599-605). [PMID:31221480] |
10. Takashima A, Noguchi K, Sato K, Hoshino T, Imahori K. (1993) Tau protein kinase I is essential for amyloid beta-protein-induced neurotoxicity.. Proc Natl Acad Sci USA, 90 (16): (7789-93). [PMID:8356085] |
11. Xuan Ren, Jianchun Xu, Qingsong Xue, Yi Tong, Tairan Xu, Jinli Wang, Ting Yang, Yuan Chen, Deshun Shi, Xiangping Li. (2024) BRG1 enhances porcine iPSC pluripotency through WNT/β-catenin and autophagy pathways. THERIOGENOLOGY, 215 (22): (10). [PMID:38000125] |