CHIR 98014

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Cat.No. 6695 - CHIR 98014 | C20H17Cl2N9O2 | CAS No. 252935-94-7
Description: Highly potent and selective GSK-3 inhibitor
Chemical Name: N6-[2-[[4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl]amino]ethyl]-3-nitro-2,6-pyridinediamine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity

Highly potent and selective GSK-3 inhibitor (IC50 values are 0.58 and 0.65 nM for the β and α isoforms, respectively). Exhibits >500-fold selectivity for GSK-3β over a range of other kinases. Improves insulin sensitivity of muscle strips from diabetic rats in vitro and decreases insulin and glucose levels in the oral glucose tolerance test in vivo. Activates Wnt signaling in human adipose stem cells (hASC) and promotes the production of definitive endoderm. Has been used in protocols to derive epicardial cells from hPSCs.

Technical Data

M. Wt 486.31
Formula C20H17Cl2N9O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 252935-94-7
PubChem ID 53396311
InChI Key MDZCSIDIPDZWKL-UHFFFAOYSA-N
Smiles NC1=NC(NCCNC2=NC=C(C(C3=C(C=C(C=C3)Cl)Cl)=N2)N4C=CN=C4)=CC=C1[N+]([O-])=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.73 20 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 486.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 10.28 mL 51.41 mL 102.82 mL
1 mM 2.06 mL 10.28 mL 20.56 mL
2 mM 1.03 mL 5.14 mL 10.28 mL
10 mM 0.21 mL 1.03 mL 2.06 mL

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References

References are publications that support the biological activity of the product.

Ring et al (2003) Selective glycogen synthase kinase 3 inhibitors potentiate Ins activation of glucose transport and utilization in vitro and in vivo. Diabetes 52 588 PMID: 12606497

Paik and Wu et al (2017) Simply derived epicardial cells. Nat.Biomed.Eng. 1 PMID: 29354320

Huang et al (2017) Activation of Wnt/β-catenin signalling via GSK3 inhibitors direct differentiation of human adipose stem cells into functional hepatocytes. Sci.Rep. 7 40716 PMID: 28094799


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View all Glycogen Synthase Kinase 3 Inhibitors

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Citations for CHIR 98014

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