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

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 & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent 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 TempStore at -20°C
Shipped InIce chest + Ice pads
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(Human)

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)

Tyrosine-protein kinase ABL 18331 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Epidermal growth factor receptor erbB1 33727 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Insulin receptor 5558 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Receptor protein-tyrosine kinase erbB-2 7851 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Insulin-like growth factor I receptor 8605 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Stem cell growth factor receptor 10667 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Casein kinase II alpha 3512 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Death-associated protein kinase 3 2108 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

MAP kinase p38 beta 2785 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Tyrosine-protein kinase LCK 9212 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

MAP kinase p38 alpha 12866 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Glycogen synthase kinase-3 beta 11785 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Protein kinase C zeta 2414 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Myosin light chain kinase, smooth muscle 1267 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Casein kinase I gamma 1 2496 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Fibroblast growth factor receptor 1 9149 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase MST2 3069 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Casein kinase I delta 4546 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

CaM kinase II beta 1626 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Tyrosine-protein kinase SRC 10310 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase Chk2 4015 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

3-phosphoinositide dependent protein kinase-1 3758 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase AKT2 4301 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase AKT3 3157 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Inhibitor of nuclear factor kappa B kinase alpha subunit 3170 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Inhibitor of nuclear factor kappa B kinase beta subunit 5554 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase Aurora-B 6805 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Rho-associated protein kinase 1 4723 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase PIM1 9629 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Protein kinase N2 1991 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Tyrosine-protein kinase CSK 2395 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Tyrosine-protein kinase JAK3 8349 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Ribosomal protein S6 kinase alpha 5 3355 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Protein kinase C gamma 2471 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Protein kinase C nu 2315 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Protein kinase C mu 1904 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Serine/threonine-protein kinase PLK1 28605 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Tyrosine-protein kinase ITK/TSK 3699 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Ribosomal protein S6 kinase alpha 1 2796 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Tyrosine-protein kinase JAK2 12915 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Casein kinase I epsilon 1412 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

CaM kinase I alpha 1664 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Vascular endothelial growth factor receptor 1 6262 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Vascular endothelial growth factor receptor 2 20924 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Glycogen synthase kinase-3 alpha 3764 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

cGMP-dependent protein kinase 2 1612 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

cGMP-dependent protein kinase 1 beta 2814 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

MAP kinase p38 delta 2605 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

MAP kinase-activated protein kinase 2 4814 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

MAP kinase-activated protein kinase 5 2831 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Protein kinase C delta 192 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

MAP kinase ERK2 650 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Histone deacetylase 6 222 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Fibroblast growth factor receptor 3 21 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

CaM kinase II gamma 1 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Staphylococcus aureus 210822 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Escherichia coli 133304 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mus musculus 284745 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Rattus norvegicus 775804 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

H4 48 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Replicase polyprotein 1ab 378 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Plasma 328 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

SARS-CoV-2 38078 Activities

Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

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:

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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

Citations of This Product

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]

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]
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]

Solution Calculators