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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Hippo-LPi-1
LPi-1

Chemical Structure : LPi-1

CAS No.: 2251130-98-8

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LPi-1 (LATS1/2 kinases inhibitor)

货号: PC-25218Not For Human Use, Lab Use Only.

LPi-1 is a highly potent, selective and ATP-competitive inhibitor of large tumor suppressor kinases (LATS1 and LATS2) with IC50 of 4.4 nM and 1.3 nM respectively, abrogates the LATS1/2-mediated YAP1 inhibition in cells, activates YAP1 and its paralogue TAZ in vitro and in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LPi-1 is a highly potent, selective and ATP-competitive inhibitor of large tumor suppressor kinases (LATS1 and LATS2) with IC50 of 4.4 nM and 1.3 nM respectively, abrogates the LATS1/2-mediated YAP1 inhibition in cells, activates YAP1 and its paralogue TAZ in vitro and in vivo.
LPi-1 inhibits LATS1- or LAST2-mediated phosphorylation of YAP1 in a dose-dependent and time-dependent manner.
LPi-1 displaysa high-affinity interaction with the LATS1 and LATS2 proteins, with Kd values of 243.3 and 111.6  nM, respectively, in MST assays.
LPi-1 reduces the phosphorylation of endogenous YAP1 in a dose-dependent manner across various cell lines, including HepG2, HEK293T, Bel7404, HeLa, SNU-423, HCT116, U2OS and primary mouse hepatocytes.
LPi-1 effectively blocked Hippo signalling activity in HepG2 cells.
LPi-1 (10 mg/kg, i.p.) promotes the activation of YAP in vivo in in ICR mouse without any apparent side effects.
LPi-1 (3 mg/kg) promotes liver repair and regeneration in mice, ameliorates paracetamol (APAP)-induced liver injury.
LPi-1 provides protection against dextran sulphate sodium salt (DSS)-induced colitis in mice.

物理化学性质&存储条件

分子量 369.78
分子式 C19H13ClFN3O2
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-(2-chloro-6-fluorobenzyl)-5-(1H-pyrrolo[2,3-b] pyridin-3-yl) furan-3-carboxamide

参考文献

1. Xiao C, et al. Br J Pharmacol. 2025 Jul 22. doi: 10.1111/bph.70137.

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