货号:A962469
同义名:
CT99021 trihydrochloride; CHIR-99021 trihydrochloride
CHIR-99021 3HCl is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM, showing > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
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产品名称 | GSK-3 ↓ ↑ | GSK-3α ↓ ↑ | GSK-3β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD2858 |
+
GSK-3, IC50: 68 nM |
99% | |||||||||||||||||
Bikinin | ✔ | 99%+ | |||||||||||||||||
GSK 3 Inhibitor IX |
++++
GSK-3, IC50: 5 nM |
99%+ | |||||||||||||||||
AZD1080 |
+++
GSK-3α, IC50: 6.9 nM |
++
GSK-3β, IC50: 31 nM |
99%+ | ||||||||||||||||
BIO-acetoxime |
+++
GSK-3α, IC50: 10 nM |
+++
GSK-3β, IC50: 10 nM |
95% | ||||||||||||||||
SB-216763 |
++
GSK-3α, IC50: 34.3 nM |
++
GSK-3β, IC50: ~34.3 nM |
98% | ||||||||||||||||
SB 415286 |
+
GSK-3α, IC50: 78 nM |
+
GSK-3β, IC50: ~78 nM |
99%+ | ||||||||||||||||
CHIR-98014 |
++++
GSK-3α, IC50: 0.65 nM |
++++
GSK-3β, IC50: 0.58 nM |
98% | ||||||||||||||||
LY2090314 |
++++
GSK-3α, IC50: 1.5 nM |
++++
GSK-3β, IC50: 0.9 nM |
99%+ | ||||||||||||||||
CHIR 99021 |
+++
GSK-3α, IC50: 10 nM |
++++
GSK-3β, IC50: 6.7 nM |
99%+ | ||||||||||||||||
TDZD-8 |
+
GSK-3β, IC50: 2 μM |
99%+ | |||||||||||||||||
Indirubin |
+
GSK-3β, IC50: 0.6 μM |
98% | |||||||||||||||||
IM-12 |
++
GSK-3β, IC50: 53 nM |
98% | |||||||||||||||||
TWS119 |
++
GSK-3β, IC50: 30 nM |
99% | |||||||||||||||||
1-Azakenpaullone |
+++
GSK-3β, IC50: 18 nM |
99%+ | |||||||||||||||||
AR-A014418 |
++
GSK-3β, Ki: 38 nM |
99%+ | |||||||||||||||||
Tideglusib |
+
GSK-3β, IC50: 60 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Laduviglusib 3HCl is an effective and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM, respectively, acting through competitive binding at the ATP site to inhibit GSK3α and GSK3β. It is over 500 times more selective for GSK-3 than for CDC2, ERK2, and other protein kinases. Laduviglusib 3HCl is also an effective activator of the Wnt/β-catenin signaling pathway. It enhances self-renewal in both mouse and human embryonic stem cells and induces autophagy[1][2][3]. At a concentration of 2.5 μM, Laduviglusib 3HCl treatment reduces the viability of ES-D3 cells by 24.7%, at 5 μM by 56.3%, at 7.5 μM by 61.9%, and at 10 μM by 69.2%, with an IC50 of 4.9 μM[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.74mL 0.35mL 0.17mL |
8.70mL 1.74mL 0.87mL |
17.40mL 3.48mL 1.74mL |
CAS号 | 1782235-14-6 |
分子式 | C22H21Cl5N8 |
分子量 | 574.72 |
SMILES Code | N#CC1=CN=C(NCCNC2=NC=C(C3=NC=C(C)N3)C(C4=CC=C(Cl)C=C4Cl)=N2)C=C1.[H]Cl.[H]Cl.[H]Cl |
MDL No. | MFCD29079432 |
别名 | CT99021 trihydrochloride; CHIR-99021 trihydrochloride; Laduviglusib trihydrochloride |
运输 | 蓝冰 |
InChI Key | DSFVSCNMMZRCIA-UHFFFAOYSA-N |
Pubchem ID | 78243722 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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