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BioChemicals
CHIR-99021
tcsc0181
CHIR-99021
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$
103.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
CHIR-99021 is a
GSK-3α/β
inhibitor with an
IC
50
of 10 and 6.7 nM,showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases.
IC50 & Target: IC50: 10 nM/6.7 nM (GSK-3α/β)
[1]
In Vitro:
CHIR 99021inhibits human GSK-3β with K
i
values of 9.8 nM
[1]
. CHIR 99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR 99021 specifically inhibits GSK3β (IC
50
=~5 nM) and GSK3α (IC
50
=~10 nM), with little effect on other kinases
[2]
. In the presence of CHIR-99021 the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 with an IC
50
of 4.9 μM
[3]
.
In Vivo:
In ZDF rats, a single oral dose of CHIR 99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration
[1]
. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis and accumulation of p-H2AX
+
cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5
+
cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h
[4]
.
Information
CAS No
252917-06-9
Formula
C
22
H
18
Cl
2
N
8
Clinical Information
clinicalinformation
Pathway
Stem Cell/Wnt
PI3K/Akt/mTOR
Autophagy
Target
GSK-3
GSK-3
Autophagy
Specifications
Form
Yellow Solid
Purity / Grade
>99.86
Solubility
DMSO 127.5 mg/mL (274.0 mM) warming
Water : Insoluble.
Smiles
smiles
Misc Information
Storage Instruction
Powder : -20°C for 3 years
In solvent : -80°C for 12 months
Alternative Names
CT99021
Observed Molecular Weight
465.34
References
[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
[2]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004.
[3]. 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.
[4]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.
[5]. 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.
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