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CHIR-99021 HCl

Catalog No. T2310L   CAS 1797989-42-4
Synonyms: CT99021 HCl, Laduviglusib HCl

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

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CHIR-99021 HCl Chemical Structure
CHIR-99021 HCl, CAS 1797989-42-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 44.00
5 mg In stock $ 70.00
10 mg In stock $ 97.00
25 mg In stock $ 166.00
50 mg In stock $ 253.00
100 mg In stock $ 490.00
200 mg In stock $ 711.00
500 mg In stock $ 1,080.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 98.07%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].
In vitro Laduviglusib monohydrochloride is a potent inhibitor of human GSK-3β, demonstrating a K_i value of 9.8 nM. As a small organic molecule, it competitively inhibits GSK3α and GSK3β by binding to their ATP-binding sites. Kinase assay results reveal that Laduviglusib monohydrochloride specifically targets GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM) with minimal impact on other kinases. Studies show that at concentrations of 2.5 μM to 10 μM, Laduviglusib monohydrochloride significantly reduces the viability of ES-D3 cells in a dose-dependent manner, with an IC 50 of 4.9 μM, indicating a substantial reduction in cell viability at these concentrations.
In vivo In ZDF rats, administering a single oral dose of Laduviglusib monohydrochloride, either 16 mg/kg or 48 mg/kg, swiftly lowers plasma glucose levels, achieving a peak reduction of approximately 150 mg/dl within 3-4 hours post-dose [1]. Additionally, a one-time administration of Laduviglusib (2 mg/kg) monohydrochloride, 4 hours prior to exposure, markedly enhances survival rates following 14.5 Gy abdominal irradiation (ABI). This treatment significantly inhibits crypt cell apoptosis and the buildup of p-H2AX + cells, while fostering crypt regeneration and increasing villus height. Furthermore, Laduviglusib monohydrochloride enhances the survival of Lgr5 + cells by preventing apoptosis and effectively halts the early reduction of Olfm4, Lgr5, and CD44 markers, observable as soon as 4 hours post-treatment [5].
Synonyms CT99021 HCl, Laduviglusib HCl
Molecular Weight 501.8
Formula C22H19Cl3N8
CAS No. 1797989-42-4

Storage

keep away from direct sunlight,store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 54.0 mg/mL (107.6 mM), Sonification is recommended.

H2O: 6.4 mg/mL (12.8 mM), Sonification is recommended.

TargetMolReferences and Literature

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. 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. 3. 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. 4. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. 5. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Bioactive Compound Library Clinical Compound Library Neuronal Differentiation Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets
GSK3-IN-2 Bakkenolide A TCS 21311 Tideglusib CHIR-99021 GSK3β inhibitor II 5-Iodo-indirubin-3'-monoxime GSK3-IN-3

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Keywords

CHIR-99021 HCl 1797989-42-4 PI3K/Akt/mTOR signaling Stem Cells GSK-3 CT99021 HCl Laduviglusib HCl inhibitor inhibit

 

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