Name | Laduviglusib trihydrochloride |
Description | Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor with IC50s of 10 nM and 6.7 nM for GSK-3α and GSK-3β. Laduviglusib trihydrochloride inhibits human GSK-3β with a Ki of 9.8 nM. Laduviglusib trihydrochloride is an activator of Wnt/β-catenin signaling. Laduviglusib trihydrochloride induces autophagy. |
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[2]. 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[4]. |
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[1]. 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[5]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : 17.1 mg/mL (29.8 mM), Sonication and heating are recommended. DMSO : 28.8 mg/mL (50.2 mM), Sonication is recommended.
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Keywords | βcatenin | Wnt/β-catenin | Wnt/beta-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | Laduviglusib Trihydrochloride | Laduviglusib | GSK-3β | GSK-3α | GSK3 | CT-99021 Trihydrochloride | CT99021 Trihydrochloride | CT-99021 | CT99021 | CT 99021 Trihydrochloride | CT 99021 | CHIR-99021 Trihydrochloride | CHIR99021 Trihydrochloride | CHIR-99021 | CHIR99021 | CHIR 99021 Trihydrochloride | CHIR 99021 | beta-catenin | betacatenin | bcatenin | 252917-06-9 free base | 252917-06-9 |
Inhibitors Related | Urea | Cromolyn sodium | Wnt pathway activator 1 | TNIK-IN-3 | GSK 3 Inhibitor IX | CHIR-99021 | AT7519 | 4-Chloro-2'-bromoacetophenone | XAV-939 | GSK-3 Inhibitor 5 | Nefopam hydrochloride | Bisdemethoxycurcumin |
Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Inhibitor Library | Neuroprotective Compound Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Wnt/Hedgehog/Notch Compound Library |