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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

1 Citations COA COA
In stock
Item Number
C125082
Grouped product items
SKU Size
Availability
 Price Qty
C125082-5mg
5mg
3
$70.90
C125082-25mg
25mg
3
$319.90
C125082-100mg
100mg
2
$509.90
C125082-500mg
500mg
1
$2,295.90
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Highly selective GSK-3 inhibitor; acts as Wnt activator

View related series
Autophagy (1917) cyclin dependent kinase 1 Inhibitor (46) glycogen synthase kinase 3 alpha Inhibitor (8) glycogen synthase kinase 3 beta Inhibitor (44) GSK-3 (104) mitogen-activated protein kinase 1 Inhibitor (14) PI3K/Akt/mTOR (765) Stem Cell/Wnt (1019) Wnt (104) β-catenin (56)

Basic Description

Synonyms GSK-3 Inhibitor XVI | 6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile | NCGC00250379-03 | NCGC00250379-21 | 6-[(2-{[4-(2,4-dichlorophenyl)-5-(4-methylimidazol -2-yl)-pyrimidin-2-yl]amino}e
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
This product requires cold chain shipping. Ground and other economy services are not available.
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 .
A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Diazines
Subclass Pyrimidines and pyrimidine derivatives
Intermediate Tree Nodes Not available
Direct Parent Phenylpyrimidines
Alternative Parents Dichlorobenzenes  3-pyridinecarbonitriles  Secondary alkylarylamines  Aminopyrimidines and derivatives  Aminopyridines and derivatives  Imidolactams  Aryl chlorides  Imidazoles  Heteroaromatic compounds  Nitriles  Azacyclic compounds  Organopnictogen compounds  Organochlorides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents 4-phenylpyrimidine - 5-phenylpyrimidine - 1,3-dichlorobenzene - 3-pyridinecarbonitrile - Aminopyridine - Aminopyrimidine - Chlorobenzene - Halobenzene - Secondary aliphatic/aromatic amine - Aryl chloride - Aryl halide - Monocyclic benzene moiety - Imidolactam - Benzenoid - Pyridine - Imidazole - Heteroaromatic compound - Azole - Nitrile - Carbonitrile - Azacycle - Secondary amine - Organohalogen compound - Hydrocarbon derivative - Organopnictogen compound - Organochloride - Organonitrogen compound - Amine - Organic nitrogen compound - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as phenylpyrimidines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrimidine ring through a CC or CN bond. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
External Descriptors Not available

Associated Targets(Human)

CDK1 Tchem Cyclin-dependent kinase 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
GSK3B Tclin Glycogen synthase kinase-3 beta (6 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
GSK3A Tclin Glycogen synthase kinase-3 alpha (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MAPK1 Tchem Mitogen-activated protein kinase 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK2A1 Tchem Casein kinase II alpha (3512 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DAPK3 Tchem Death-associated protein kinase 3 (2108 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK2B Tchem CaM kinase II beta (1626 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IKBKB Tchem Inhibitor of nuclear factor kappa B kinase beta subunit (5554 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCG Tchem Protein kinase C gamma (2471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKD3 Tchem Protein kinase C nu (2315 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKD1 Tchem Protein kinase C mu (1904 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ITK Tclin Tyrosine-protein kinase ITK/TSK (3699 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1E Tclin Casein kinase I epsilon (1412 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK1 Tchem CaM kinase I alpha (1664 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT1 Tclin Vascular endothelial growth factor receptor 1 (6262 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKG2 Tchem cGMP-dependent protein kinase 2 (1612 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKG1 Tchem cGMP-dependent protein kinase 1 beta (2814 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK13 Tchem MAP kinase p38 delta (2605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 (4814 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPKAPK5 Tchem MAP kinase-activated protein kinase 5 (2831 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Prkcd Protein kinase C delta (192 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
H4 (48 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504765152
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504765152
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)
InChIKey AQGNHMOJWBZFQQ-UHFFFAOYSA-N
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
Molecular Weight 465.34
Reaxy-Rn 25763160
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25763160&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

15 results found

Lot Number Certificate Type Date Item
C2521222 Certificate of Analysis Mar 27, 2025 C125082
F23151064 Certificate of Analysis Mar 04, 2025 C125082
F23151072 Certificate of Analysis Mar 04, 2025 C125082
F23151070 Certificate of Analysis Mar 04, 2025 C125082
F23151091 Certificate of Analysis Mar 04, 2025 C125082
F23151075 Certificate of Analysis Mar 04, 2025 C125082
F23151073 Certificate of Analysis Mar 04, 2025 C125082
F23151092 Certificate of Analysis Mar 04, 2025 C125082
F23151069 Certificate of Analysis Mar 04, 2025 C125082
K2212733 Certificate of Analysis Aug 23, 2024 C125082
K2212430 Certificate of Analysis Aug 23, 2024 C125082
K2212752 Certificate of Analysis Aug 23, 2024 C125082
K2126055 Certificate of Analysis Sep 12, 2023 C125082
B1525008 Certificate of Analysis Sep 13, 2022 C125082
K2212734 Certificate of Analysis Jul 20, 2022 C125082

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Chemical and Physical Properties

Solubility Solvent:DMSO, Max Conc. mg/mL: 9.31, Max Conc. mM: 20
Sensitivity Heat Sensitive
Molecular Weight 465.300 g/mol
XLogP3 4.300
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 7
Exact Mass 464.103 Da
Monoisotopic Mass 464.103 Da
Topological Polar Surface Area 115.000 Ų
Heavy Atom Count 32
Formal Charge 0
Complexity 645.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Alternative Products

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    Starting at $333.90

  2. CHIR 99021 trihydrochloride
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    • ≥98%(HPLC)

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