CHIR-98014 is a potent, cell-permeableGSK-3inhibitor withIC₅₀s of 0.65 and 0.58 nM forGSK-3αandGSK-3β, respectively; it shows less potent activities against cdc2 anderk2.

CHIR 98014 inhibits human GSK-3β with K_ivalue of 0.87 nM. CHIR 98014 causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC₅₀s of 106 nM and 107 nM, respectively^[1]. CHIR-98014 (1 μM) reduces the viability of ES-CCE cells by 52%, with IC₅₀of 1.1 μM. Moreover, CHIR-98014 in combination with CHIR-99021 results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells. In CHIR-98014 treated cells, the T gene expression is induced up to 2,500-fold. CHIR-98014 (1 μM) also yields around 50% Brachyury-positive cells, with EC₅₀of 0.32 μM^[2]. CHIR98014 (10 μM) prevents loss of neurites caused by 20 μM PrP1-30 in cortical and hippocampal neurons, and substantially decreases the amount of dead cells^[3].

CHIR 98014 (30 mg/kg, i.p.) exhibits a significant reduction in fasting hyperglycemia within 4 h of treatment and shows improved glucose disposal during an ipGTT in markedly diabetic and insulin-resistant db/db mice^[1].

486.31

Solid

C₂₀H₁₇Cl₂N₉O₂

252935-94-7

Room temperature in continental US; may vary elsewhere.

DMSO : 12.5 mg/mL(25.70 mM;ultrasonic and warming and heat to 60℃)

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