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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-SMIP-30
SMIP-30

Chemical Structure : SMIP-30

CAS No.: 2919466-30-9

SMIP-30 (SMIP30, PPM1A inhibitor)

货号: PC-72527Not For Human Use, Lab Use Only.

SMIP-30 is a potent and selective inhibitor of PPM1A with IC50 of 1 uM, selectively inhibits the phosphatase activity of PPM1A.

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纯度 & COA & 质检文件 纯度: 97.78% (HPLC) Select Batch:

生物&药学活性

SMIP-30 is a potent and selective inhibitor of PPM1A with IC50 of 1 uM, selectively inhibits the phosphatase activity of PPM1A.
SMIP-30 shows poor inhibitory activity against closest homolog PPM1B (IC50>30 uM).
SMIP-30 is an uncompetitive inhibitor for PPM1A (Ki=0.84 uM), does not exhibit any cytotoxic effects up to 30 uM in THP-1 macrophages.
SMIP-30 dose-dependently reduces the Mtb burden in infected macrophages, and is well tolerated in vivo and combined with rifampicin reduces Mtb burden in the lungs of infected mice.
SMIP-30 induces LC3B-II expression, activates autophagy in Mtb-infected macrophages in a PPM1A-dependent manner.
SMIP-30 induces a dose-dependent increase in phosphorylation of S403-p62 in WT macrophages.

物理化学性质&存储条件

分子量 352.203
分子式 C16H15BrFNO2
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

2-fluoro-5-(2-hydroxyethyl)-8-methoxyphenanthridin-5-ium bromide

参考文献

1. Stefania Berton, et al. Cell Chem Biol. 2022 Mar 18;S2451-9456(22)00094-0.

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