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Laduviglusib trihydrochloride

Catalog No. T22657 CAS 1782235-14-6

Synonyms: CT99021 trihydrochloride, CHIR 99021 trihydrochloride, CHIR 99021 trihydrochloride (252917-06-9 free base)

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.

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Laduviglusib trihydrochloride Chemical Structure

Laduviglusib trihydrochloride, CAS 1782235-14-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 138.00
25 mg	In stock	$ 283.00
50 mg	In stock	$ 536.00
100 mg	In stock	$ 718.00
500 mg	In stock	$ 1,490.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.03%

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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].

Synonyms	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

Solubility Information

H2O: 17.1 mg/mL (29.8 mM), Sonication and heating are recommended.

DMSO: 28.8 mg/mL (50.1 mM)

References 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：

Inhibitor Library Kinase Inhibitor Library Anti-Obesity Compound Library Metabolism Compound Library Anti-Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Laduviglusib trihydrochloride 1782235-14-6 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Stem Cells GSK-3 Wnt/beta-catenin 252917-06-9 free base CHIR 99021 Trihydrochloride CT99021 trihydrochloride Laduviglusib CHIR99021 Trihydrochloride CT99021 Trihydrochloride CT-99021 Trihydrochloride CT 99021 Trihydrochloride CT99021 CHIR 99021 CHIR 99021 trihydrochloride CHIR 99021 trihydrochloride (252917-06-9 free base) 252917-06-9 CHIR99021 CHIR-99021 CHIR-99021 Trihydrochloride CT-99021 Laduviglusib Trihydrochloride CT 99021 inhibitor inhibit

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