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Cat. No. Name Size Price Add Cart
KI0321CT990212 mg$160
CT990215 mg$270
CT9902125 mg$742.5
CT99021100 mg$1600

Chemical Characteristic

Product NameCT99021
SynonymsCHIR-99021
CAS No.252917-06-9
Molecular Weight 465.34
FormulaC22H18Cl2N8
Chemical Name6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino]ethylamino]pyridine-3-carbonitrile
Smilesc1c(ccc(n1)NCCNc1nc(c(cn1)c1nc(c[nH]1)C)c1c(cc(cc1)Cl)Cl)C#N
Chemical Structure

Biological activities

CT99021 is a GSK-3 inhibitor with IC50 of 10 and 6.7 nM for GSK-3α and GSK-3β, respectively. CT99021 inhibits human GSK-3b with a Ki value of 9.8 nM. CT99021 acts as a competitive inhibitor of ATP binding and exhibits >500-fold selectivity for GSK-3 versus other kinase and non kinase enzymes. Meanwhile, CT99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with an EC50 of 0.76 μM.[1] Pretreatment with CT99021 completely prevents Aβ from inhibiting LTP, as assesses using whole-cell patch-clamp recording in cultured slices.[2] Besides, CT99021 potentiates and mimics the actions of insulin. CT99021 inhibits GSK3 and mimics Wnt signaling in 3T3-L1 preadipocytes, with half-maximal inhibition of preadipocyte differentiation of ~0.3 μM. Preadipocyte differentiation is inhibited when 3T3-L1 cells are exposed to CT99021 for any 24 h period during the first 3 days of adipogenesis. In vitro, CT99021 activates Wnt signaling as assessed by stabilization of free cytosolic b-catenin and inhibition of adipogenesis. Activation of Wnt signaling with CT99021 inhibits adipogenesis and induces C/EBPa and PPARg, without detectable effects on transient induction of C/EBPband C/EBPδ. In addition, the time during adipogenesis in which preadipocytes are sensitive to inhibition by CT99021.[3] The treatment with CT99021 increases the rate of proliferation of INS-1E cells in a dose-dependent manner and the proliferation rate reaches a maximum in the presence of 2.5-10 μM.[4] In ZDF rats, a single oral dose of CT99021 rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dL 3-4 hours after administration.[1]

Protocols

CT99021 is diluted in DMSO. [4]

References

[1] Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabets. 2003, 52 (3): 588-595.
[2] Jo J, et al. Aβ (1-42) inhibition of LTP is mediated by a signaling pathway involving caspase-3, Akt1 and GSK-3β. Nat Neurosci. 2011, 14(5): 545-547.
[3] Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002, 277(34): 30998-31004.
[4] Mussamann R, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. J Biol Chem. 2007, 282(16): 12030-12037.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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