货号:A251413 同义名: NP 01139;GSK-3β Inhibitor I
TDZD-8, the derivative of thiadiazolidinone, is a selective inhibitor of GSK-3. It inhibits GSK-3β with IC50 of 2 μM.
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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 |
98+% | |||||||||||||||||
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 |
98% | |||||||||||||||||
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。 |
靶点 |
|
描述 | TDZD-8 is the first non-ATP competitive inhibitor of GSK-3β with IC50 value of 2μM. Pretreatment with TDZD-8 at 10μM for 1h showed neuroprotection against 6-OHDA-induced damage, shown by reduced cell death and apoptosis, in both SH-SY5Y cells and cultured CGNs. Intrahippocampal delivery of TDZD-8 blocked dephosphorylation and activation of GSK3β in db/db mice. This inhibition of GSK3β prevented accumulation of pS202Tau and hyperphosphorylation of pS396/404Tau in db/db mice. It also reduced somatodendritic tau phosphorylation in db/db mice. The normalization of spatial recognition memory in db/db mice and block of deficits in novel object study could also be observed. Recent study found that TDZD-8 showed inhibition effect on 2019-nCoV. |
作用机制 | TDZD-8 is a non-ATP competitive GSK-3β inhibitor. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.50mL 0.90mL 0.45mL |
22.50mL 4.50mL 2.25mL |
44.99mL 9.00mL 4.50mL |
CAS号 | 327036-89-5 |
分子式 | C10H10N2O2S |
分子量 | 222.264 |
别名 | NP 01139;GSK-3β Inhibitor I;TDZD 8. GSK3 Inhibitor I |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(472.41 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |