CHIR-99021 trihydrochloride

CAS No. 1782235-14-6

CHIR-99021 trihydrochloride( CT99021 trihydrochloride | CHIR99021 trihydrochloride | CHIR 99021 trihydrochloride | CT-99021 trihydrochloride )

Catalog No. M12681 CAS No. 1782235-14-6

A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 47 Get Quote
5MG 77 Get Quote
10MG 124 Get Quote
25MG 255 Get Quote
50MG 482 Get Quote
100MG 646 Get Quote
500MG 1341 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    CHIR-99021 trihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively.
  • Description
    A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively; mimics Wnt signaling in preadipocytes, stabilizes free cytosolic beta-catenin and inhibits adipogenesis by blocking induction of C/EBPα and PPARγ; potentiates insulin activation of glucose transport and utilization in vitro and in vivo; also widely used for stem cell differentiation and naive stem cell generation.
  • In Vitro
    Laduviglusib trihydrochloride inhibits human GSK-3β with Ki values of 9.8 nM. Laduviglusib trihydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib trihydrochloride specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases. In the presence of Laduviglusib trihydrochloride the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib trihydrochloride with an IC50 of 4.9 μM.
  • In Vivo
    In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) trihydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. Laduviglusib (2 mg/kg) trihydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib trihydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h.
  • Synonyms
    CT99021 trihydrochloride | CHIR99021 trihydrochloride | CHIR 99021 trihydrochloride | CT-99021 trihydrochloride
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    GSK-3
  • Recptor
    GSK-3
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1782235-14-6
  • Formula Weight
    574.7208
  • Molecular Formula
    C22H21Cl5N8
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 32 mg/mL
  • SMILES
    CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N.Cl.Cl.Cl
  • Chemical Name
    3-Pyridinecarbonitrile, 6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-, hydrochloride (1:3)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ying QL, et al. Nature. 2008 May 22;453(7194):519-23. 2. Ring DB, et al. Diabetes. 2003 Mar;52(3):588-95. 3. Bennett CN, et al. J Biol Chem. 2002 Aug 23;277(34):30998-1004. 4. Li W, et al. Stem Cells. 2009 Dec;27(12):2992-3000.
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