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CHIR-98014
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CHIR-98014图片
CAS NO:252935-94-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
CHIR-98014 是一种有效的,细胞通透的GSK-3抑制剂,可抑制GSK-3αGSK-3β的活性,IC50值分别为 0.65 和 0.58 nM;CHIR-98014 对 cdc2 和 erk2 的作用较弱。
生物活性

CHIR-98014 is a potent, cell-permeableGSK-3inhibitor withIC50s of 0.65 and 0.58 nM forGSK-3αandGSK-3β, respectively; it shows less potent activities against cdc2 anderk2.

IC50& Target[1]

GSK-3β

0.58 nM (IC50)

GSK-3α

0.65 nM (IC50)

cdc2

3700 nM (IC50)

体外研究
(In Vitro)

CHIR 98014 inhibits human GSK-3β with Kivalue of 0.87 nM. CHIR 98014 causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC50s of 106 nM and 107 nM, respectively[1]. CHIR-98014 (1 μM) reduces the viability of ES-CCE cells by 52%, with IC50of 1.1 μM. Moreover, CHIR-98014 in combination with CHIR-99021 results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells. In CHIR-98014 treated cells, the T gene expression is induced up to 2,500-fold. CHIR-98014 (1 μM) also yields around 50% Brachyury-positive cells, with EC50of 0.32 μM[2]. CHIR98014 (10 μM) prevents loss of neurites caused by 20 μM PrP1-30 in cortical and hippocampal neurons, and substantially decreases the amount of dead cells[3].

体内研究
(In Vivo)

CHIR 98014 (30 mg/kg, i.p.) exhibits a significant reduction in fasting hyperglycemia within 4 h of treatment and shows improved glucose disposal during an ipGTT in markedly diabetic and insulin-resistant db/db mice[1].

分子量

486.31

性状

Solid

Formula

C20H17Cl2N9O2

CAS 号

252935-94-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL(25.70 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0563 mL10.2815 mL20.5630 mL
5 mM0.4113 mL2.0563 mL4.1126 mL
10 mM0.2056 mL1.0282 mL2.0563 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。