Western blot analysis of extracts from 293 cells, untreated (-) or treated with Calyculin A #9902 (50 nM, 1 hr; +) with or without pretreating the cells with CHIR-99021 (10 μM, 1 hr; +), using Phospho-c-Myc (Thr58) (E4Z2K) Rabbit mAb #46650 (upper), c-Myc (E5Q6W) Rabbit mAb #18583 (middle), or β-Actin (D6A8) Rabbit mAb #8457 (lower).
Chemical structure of CHIR-99021.
CHIR-99021 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.07 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Molecular Weight: 465.3 g/mol
Molecular Formula: C22H18CI2N8
Solubility: Soluble in DMSO at 25 mg/ml with slight warming.
CHIR-99021, also known as CT-99021, is a potent and selective inhibitor of glycogen synthase kinase-3β (GSK-3β) and GSK-3α with IC50 values of 6.7 and 10 nM, respectively. This small compound has been shown to have >500-fold selectivity for GSK-3 when tested against 20 different protein kinases (1). Studies have shown that treating isolated rat islets with CHIR-99021 can increase beta cell replication 2-3-fold, making this an important compound when studying type 1 and type 2 diabetes (2).
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