Laduviglusib trihydrochloride

SKU: orb1704618

Description

Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a potent and selective GSK-3 inhibitor, activating Wnt/β-catenin signaling and inducing autophagy. It is widely used in research areas such as neurodegenerative diseases, cancer, and diabetes, with applications in both cellular and animal model studies to investigate related pathways.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1782235-14-6
• MW: 573.71
• Purity: 99.34%
• Formula: C₂₂H₂₀Cl₅N₈
• SMILES: Cl.Cl.Cl.Cc1cnc([nH]1)-c1cnc(NCCNc2ccc(cn2)C#N)nc1-c1ccc(Cl)cc1Cl
• Target: Wnt/beta-catenin,GSK-3,Autophagy
• Solubility: H2O:17.1 mg/mL (29.81 mM);DMSO:28.8 mg/mL (50.2 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (3.49 mM)

Bioactivity

• Target IC50:
  CDC2:8800 nM|GSK-3α:10 nM|GSK-3β:6.7 nM
• In Vivo:
  Oral administration of Laduviglusib trihydrochloride(16 mg/kg and 48 mg/kg) rapidly reduces plasma glucose with a maximal reduction of nearly 150 mg/dl in ZDF rats. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride (2 mg/kg) improves survival after 14.5 Gy abdominal irradiation. Laduviglusib trihydrochloride inhibits crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride blocks apoptosis, increases Lgr5+ cell survival and prevents the reduction of Olfm4, Lgr5 and CD44.
• In Vitro:
  Laduviglusib trihydrochloride(10 μM) lowers the viability of the ES-D3 cells by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% with an IC50 of 4.9 μM. Laduviglusib trihydrochloride shows >500-fold selectivity over ERK2, CDC2, and other protein kinases. Laduviglusib trihydrochloride specifically inhibits GSK3β and GSK3α with IC50s of 5nM and 10nM in vitro kinase assays.

Storage & Handling

• Storage: Powder: -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

GSK-3α, GSK3, GSK-3β, Laduviglusib, Laduviglusib Trihydrochloride, 252917-06-9, 252917-06-9 free base, bcatenin, beta-catenin, CHIR 99021, CHIR 99021 Trihydrochloride, CHIR 99021 trihydrochloride, CHIR 99021 trihydrochloride (252917-06-9 free base), CHIR99021 Trihydrochloride, CHIR-99021 Trihydrochloride, CHIR99021, CHIR-99021, betacatenin, CT99021 trihydrochloride, CT99021 Trihydrochloride, CT-99021 Trihydrochloride, CT99021, CT-99021, CT 99021, CT 99021 Trihydrochloride, βcatenin, Wnt, Wnt/b-catenin, Wnt/betacatenin, Wnt/β-catenin, Wnt/beta-catenin

Compound Identifiers

PubChem CID

78243722