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CHIR-99021 - ≥98%, high purity , CAS No.252917-06-9, 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

  • Moligand™
  • ≥98%
Item Number
C125082
Grouped product items
SKUSizeAvailabilityPrice Qty
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

Basic Description

Synonyms252917-06-9|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
Specifications & Purity≥98%
Storage TempStore at -20°C
Shipped InDry ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor 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 .
A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 1 Activities

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

GSK3B Tclin Glycogen synthase kinase-3 beta 6 Activities

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

GSK3A Tclin Glycogen synthase kinase-3 alpha 4 Activities

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

MAPK1 Tchem Mitogen-activated protein kinase 1 1 Activities

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

Names and Identifiers

IUPAC Name 6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile
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

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

14 results found

Lot NumberCertificate TypeDateItem
K2212430Certificate of AnalysisAug 23, 2024 C125082
K2212733Certificate of AnalysisAug 23, 2024 C125082
K2212752Certificate of AnalysisAug 23, 2024 C125082
K2126055Certificate of AnalysisSep 12, 2023 C125082
F23151064Certificate of AnalysisJun 02, 2023 C125082
F23151069Certificate of AnalysisJun 02, 2023 C125082
F23151070Certificate of AnalysisJun 02, 2023 C125082
F23151072Certificate of AnalysisJun 02, 2023 C125082
F23151073Certificate of AnalysisJun 02, 2023 C125082
F23151075Certificate of AnalysisJun 02, 2023 C125082
F23151091Certificate of AnalysisJun 02, 2023 C125082
F23151092Certificate of AnalysisJun 02, 2023 C125082
B1525008Certificate of AnalysisSep 13, 2022 C125082
K2212734Certificate of AnalysisJul 20, 2022 C125082

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Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 9.31, Max Conc. mM: 20
SensitivityHeat Sensitive

Safety and Hazards(GHS)

Pictogram(s) GHS06,   GHS07
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

Related Documents

References

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,  (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]

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