Molecular Formula | C22H18Cl2N8 |
Molar Mass | 465.34 |
Density | 1.48 |
Boling Point | 784.1±70.0 °C(Predicted) |
Solubility | DMSO 93 mg/mL Water 8 mg/mL Ethanol 2 mg/mL |
Appearance | powder |
Color | white to light brown |
pKa | 11.92±0.10(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Use | A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor |
In vitro study | CHIR-99021 inhibits human GSK-3β with K i values of 9.8 nM. CHIR-99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR-99021 specifically inhibits GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM), with little effect on other kinases. In the presence of CHIR-99021 the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 with an IC 50 of 4.9 μM. |
In vivo study | In ZDF rats, a single oral dose of CHIR-99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis and accumulation of p-H2AX + cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5 + cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h. |
Hazard Symbols | T - Toxic |
Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
HS Code | 29335990 |
product description | CHIR99021 is an aminopyrimidine derivative, which inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM respectively. |
Biological activity | CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM respectively. CHIR99201 no cross reactivity for CDKs, the selectivity for GSK-3β was 350 times higher than that for CDKs. CHIR-99021 can be used as an activator of Wnt/β-catenin and induce autophagy. |
Target | Value |
GSK-3β (Cell-free assay) | 6.7 nM |
GSK-3α (Cell-free assay) | 10 nM |