Revision 1

#54290Store at -20C

5 mg

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

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For Research Use Only. Not for Use in Diagnostic Procedures.

Background

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).

  1. Ring, D.B. et al. (2003) Diabetes 52, 588-95.
  2. Mussmann, R. et al. (2007) J Biol Chem 282, 12030-7.

Molecular Formula

C22H18CI2N8

Molecular Weight

465.3 g/mol

Purity

>98%

CAS

252917-06-9

Solubility

Soluble in DMSO at 25 mg/ml with slight warming.

Storage

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.

Directions for Use

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.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

    Trademarks and Patents

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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    Revision 1
    #54290

    CHIR-99021

    CHIR-99021: Image 1 Expand Image
    使用 Phospho-c-Myc (Thr58) (E4Z2K) Rabbit mAb #46650(上图)、c-Myc (E5Q6W) Rabbit mAb #18583(中间)或 β-Actin (D6A8) Rabbit mAb #8457(下图)对未经 (-) 或已经 Calyculin A #9902(50 nM,1 小时;+)处理且细胞用或不用 CHIR-99021(10 μM,1 小时;+)预处理的 293 细胞的提取物进行蛋白印迹分析。
    CHIR-99021: Image 2 Expand Image
    CHIR-99021 的化学结构。