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首页-小分子抑制剂&激动剂-Others-Other Targets-Pin1 inhibitor API-1
Pin1 inhibitor API-1

Chemical Structure : Pin1 inhibitor API-1

CAS No.: 680622-70-2

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Pin1 inhibitor API-1 (API-1)

货号: PC-35874Not For Human Use, Lab Use Only.

Pin1 inhibitor API-1 (API-1) is a potent, specific inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) and inhibits Pin1 cis-trans isomerizing activity with IC50 of 72.3 nM.

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10 mg ￥2280 In stock
25 mg ￥3780 In stock
50 mg ￥5880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pin1 inhibitor API-1 (API-1) is a potent, specific inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) and inhibits Pin1 cis-trans isomerizing activity with IC50 of 72.3 nM.
API-1 displays remarkable selectivity over other peptidyl-prolyl cis-trans isomerases, including Pin4, FKBP12, and cyclophilin A.
API-1 suppresses in vitro cell proliferation and migration of HCC cells with low IC50 values, which is depended on both Pin1 expression and XPO5 phosphorylation.
API-1 recognizes and isomerizes the phosphorylated serine-proline motif of phosphorylated XPO5 and passivates phosphorylated XPO5, maintains the active pXPO5 conformation, rescues the pre-miRNA loading of pXPO5 and increases mature miRNA biogenesis; suppresses tumour growth in mice.

物理化学性质&存储条件

分子量 366.304
分子式 C15H13F3N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-(((2-amino-9H-purin-6-yl)oxy)methyl)benzyl)-2,2,2-trifluoroacetamide

参考文献

1. Pu W, et al. Hepatology. 2018 Aug;68(2):547-560.

2. Pauly GT, et al. J Med Chem. 2008 Nov 27;51(22):7144-53.

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