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Chemical Structure| 252935-94-7 Chemical Structure| 252935-94-7

Structure of CHIR-98014
CAS No.: 252935-94-7

Chemical Structure| 252935-94-7

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CHIR-98014 (CT98014) is highly selective aminopyrimidine-derivatived inhibitor of GSK-3 with IC50 of 650nM and 580nM for GSK-3 and GSK-3(measured by kinase assays), respectively, and exhibits >1000-fold selectivity for GSK-3 over closely related kinases, such as cdc2.

Synonyms: CT98014

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Product Details of CHIR-98014

CAS No. :252935-94-7
Formula : C20H17Cl2N9O2
M.W : 486.31
SMILES Code : NC1=C([N+]([O-])=O)C=CC(NCCNC2=NC=C(N3C=CN=C3)C(C4=CC=C(Cl)C=C4Cl)=N2)=N1
Synonyms :
CT98014
MDL No. :MFCD10565922
InChI Key :MDZCSIDIPDZWKL-UHFFFAOYSA-N
Pubchem ID :53396311

Safety of CHIR-98014

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CHIR-98014

PI3K-AKT
Hedgehog

Isoform Comparison

Biological Activity

Target
  • GSK-3α

    GSK-3α, IC50:0.65 nM

  • GSK-3β

    GSK-3β, IC50:0.58 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
CT26 cells 5 μmol/L CHIR98014 alone or combined with high glucose increased GSK-3β Ser9 phosphorylation, β-catenin accumulation, and Cyclin D1 expression. PMC3806619
mouse embryonic fibroblasts 3 μM 6 days Directly reprograμMed mouse embryonic fibroblasts into PRG4+ chondrocytes PMC7066361
LUHMES cells 2 µM 6 hours CHIR98014 at 2 µM significantly reduced Ser396 tau phosphorylation in LUHMES cells and showed neuroprotective effects. PMC2078230
19-9-11 iPSCs 0.6 μM 2 days To evaluate the effect of CHIR-98014 in inducing differentiation of hPSCs into CD34+CD31+ endothelial progenitors, results showed that CHIR-98014, like CHIR99021 and BIO-acetoxime, effectively induced endothelial progenitor differentiation. PMC4235141
SEM cells 0 25 400 6400 nM 96 hours To evaluate the combined effect of CHIR-98014 and ABBV-744, results showed that the combination significantly reduced cell viability PMC10120025
OCI-AML2 cells 100 nM 14 days To identify targetable pathways in BETi-resistant cells through CRISPR screening, GSK3β was identified as a synergistic gene associated with sensitivity to ABBV-744 treatment PMC10120025
Huh-7 cells 50 nM 48 hours Inhibited cell proliferation and invasion, promoted cell apoptosis and cell cycle arrest at G0/G1 phase PMC11194219
HCCLM3 cells 50 nM 48 hours Inhibited cell proliferation and invasion, promoted cell apoptosis and cell cycle arrest at G0/G1 phase PMC11194219
A549 cells 1 µM 30 hours CHIR-98014 significantly attenuated the upregulation of TREM2, BLNK, STING1, and CASP1 in A549 cells treated with A + N and promoted apoptosis. PMC8538697
NCI-H460 cells 1 µM 48 hours CHIR-98014 significantly attenuated the expression of TREM2 in NCI-H460 cells treated with A + N and promoted apoptosis. PMC8538697
NCI-H292 cells 1 µM 48 hours CHIR-98014 significantly attenuated the expression of TREM2 in NCI-H292 cells treated with A + N and promoted apoptosis. PMC8538697

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Postnatal day 12 rat model Intravenous injection 150 mg/kg 3 times per week for 33 days CHIR98014 significantly reduced tau phosphorylation in the cortex and hippocampus of postnatal day 12 rats and showed dose-dependent effects. PMC2078230
NSG mice KMT2A-r B-ALL PDX model Oral administration 30 mg/kg OSI-027 and 2 mg/kg doxorubicin every other day for 2 weeks To evaluate the combined effect of GSK3i and BETi, results showed that the combination significantly inhibited leukemia cell proliferation and extended survival PMC10120025

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.28mL

2.06mL

1.03mL

20.56mL

4.11mL

2.06mL

References

 

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