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Laduviglusib (trihydrochloride)

Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy[1][2][3].

Product Specifications

CAS Number

[1782235-14-6]

Product Name Alternative

CHIR-99021 (trihydrochloride) ; CT99021 trihydrochloride

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; GSK-3; Organoid; Wnt; β-catenin

Type

Reference compound

Related Pathways

Autophagy; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/laduviglusib-trihydrochloride.html

Purity

99.11

Solubility

DMSO : 250 mg/mL (ultrasonic) |H2O : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N#CC1=CC=C(NCCNC2=NC=C(C3=NC=C(C)N3)C(C4=CC=C(Cl)C=C4Cl)=N2)N=C1.[H]Cl.[H]Cl.[H]Cl

Molecular Formula

C22H21Cl5N8

Molecular Weight

574.72

Precautions

H302, H315, H319, H335

References & Citations

[1]Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52 (3) :588-95.|[2]Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277 (34) :30998-1004.|[3]Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273.|[4]Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.|[5]Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7 (4) :e35892.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

GSK-3α; GSK-3β

Citation 01

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