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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $36 | In Stock | |
2 mg | $52 | In Stock | |
5 mg | $85 | In Stock | |
10 mg | $138 | In Stock | |
25 mg | $283 | In Stock | |
50 mg | $536 | In Stock | |
100 mg | $718 | In Stock | |
500 mg | $1,490 | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $108 | In Stock |
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. |
Targets&IC50 | GSK-3α:10 nM, GSK-3β:6.7 nM, CDC2:8800 nM |
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]. |
Alias | CT99021 trihydrochloride, CHIR 99021 trihydrochloride, CHIR 99021 trihydrochloride (252917-06-9 free base) |
Molecular Weight | 574.72 |
Formula | C22H21Cl5N8 |
Cas No. | 1782235-14-6 |
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 (50.1 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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