CHIR-99021 , ≥98% , 252917-06-9

Synonym(s):
6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile;6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile

CAS NO.：252917-06-9

Empirical Formula: C22H18Cl2N8

Molecular Weight: 465.34

MDL number: MFCD11846251

EINECS: 809-015-4

PRODUCT Properties

• Boiling point: 784.1±70.0 °C(Predicted)
• Density: 1.48
• storage temp.: -20°C
• solubility: DMSO: soluble2mg/mL, clear (warmed)
• pka: 11.92±0.10(Predicted)
• form: powder
• color: white to light brown
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
• InChIKey: AQGNHMOJWBZFQQ-UHFFFAOYSA-N
• SMILES: C1=NC(NCCNC2=NC=C(C3NC(C)=CN=3)C(C3=CC=C(Cl)C=C3Cl)=N2)=CC=C1C#N
• CAS DataBase Reference: 252917-06-9

Description and Uses

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that plays a key inhibitory role in both the insulin and Wnt signaling pathways. CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC₅₀ values of 10 and 6.7 nM, respectively. When tested against twenty different protein kinases, this inhibitor shows greater than 500-fold selectivity for GSK3. CHIR99021 activates glycogen synthesis in CHO-IR cells (EC₅₀ = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle. A single oral dose (30 mg/kg) of CHIR99021 enhances in vivo glucose metabolism in a rodent model of type 2 diabetes. CHIR99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells.

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that plays a key inhibitory role in both the insulin and Wnt signaling pathways. CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. When tested against twenty different protein kinases, this inhibitor shows greater than 500-fold selectivity for GSK3. CHIR99021 activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle. A single oral dose (30 mg/kg) of CHIR99021 enhances in vivo glucose metabolism in a rodent model of type 2 diabetes. CHIR99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells.

Safety

• Symbol(GHS): GHS06
• Signal word: Danger
• Hazard statements: H300-H315-H319-H335
• Precautionary statements: P261-P264-P301+P310-P305+P351+P338
• Hazard Codes: T
• Risk Statements: 25-36/37/38
• Safety Statements: 26-36/37/39-45
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: 3
• HS Code: 29335990
• Storage Class: 11 - Combustible Solids
• Hazard Classifications: Acute Tox. 4 Oral