CHIR-99021
货号：C252917
规格：10mg
品牌：OrganRegen
产品介绍
DESCRIPTION
|
CHIR-99021 is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy[1][2][3]. |
|||
|
Alias |
Laduviglusib; CT99021
|
||
|
M. W t |
465.34 |
||
|
Formula |
C22H18Cl2N8 |
||
|
CAS No |
252917-06-9 |
||
|
Storage |
Powder |
-20°C |
3 years |
|
4°C |
2 years C22H18Cl2N8 |
||
|
In solvent |
-80°C |
6 months |
|
|
-20°C |
1 month |
||
|
Solubility |
DMSO |
16.67 mg/mL(35.82 mM) |
|
|
H2O |
< 0.1 mg/mL(insoluble) |
||
BIOLOGICAL ALTIVITY
CHIR-99021 inhibits human GSK-3β with Ki values of 9.8 nM[1]. Laduviglusib is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[4]. In the presence of Laduviglusib 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 Laduviglusib with an IC50 of 4.9 mm[2].
In Vivo
In ZDF rats, a single oral dose of Laduviglusib (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]. Laduviglusib (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[5].
REFERENCES