CHIR-99021 HCl

SKU: orb1704267

Description

CHIR-99021 HCl

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1797989-42-4
• MW: 501.8
• Purity: 98.44%
• Formula: C₂₂H₁₉Cl₃N₈
• SMILES: Cl.N#CC1=CN=C(C=C1)NCCNC=2N=CC(C3=NC=C(N3)C)=C(N2)C=4C=CC(Cl)=CC4Cl
• Target: Autophagy,Wnt/beta-catenin,GSK-3
• Solubility: DMSO:60 mg/mL (119.57 mM);H2O:6.4 mg/mL (12.75 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (4.98 mM)

Bioactivity

• 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 . 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 .
• 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.

Storage & Handling

• Storage: keep away from direct sunlight,store under nitrogen | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CT99021 HCl, CHIR-99021 HCl, GSK-3α/β, GSK3, Laduviglusib HCl

Compound Identifiers

PubChem CID

71295844