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RIPK1 inhibitor 13c

Chemical Structure : RIPK1 inhibitor 13c

CAS No.: 3026543-19-8

RIPK1 inhibitor 13c

货号: PC-24510Not For Human Use, Lab Use Only.

RIPK1 inhibitor 13c is a potent, selective RIPK1 inhibitor with IC50 of 59.8 nM and Kd of 3.5 nM, effectively prevented the necroptosis (HT-29, EC50=4.58 nM) by inhibiting phosphorylation of RIPK1/RIPK3/MLKL single pathway.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RIPK1 inhibitor 13c is a potent, selective RIPK1 inhibitor with IC50 of 59.8 nM and Kd of 3.5 nM, effectively prevented the necroptosis (HT-29, EC50=4.58 nM) by inhibiting phosphorylation of RIPK1/RIPK3/MLKL single pathway.
RIPK1 inhibitor 13c displays 486-fold selectivity toward RIPK1 over RIPK3, and no activity against MLKL.
RIPK1 inhibitor 13c inhibits TSZ-induced necroptosis in HT-29 cells, dose-dependently inhibits the phosphorylation of RIPK1 and RIPK3 13c at 3 nM and subsequently inhibits the phosphorylation of downstream MLKL at 30 nM.
13c (300 nM) completely inhibits the phosphorylation of RIPK1, RIPK3, and MLKL.
13c could dose-dependentlythe reduced concentrations of proinflammatory cytokines IL-6 in mice.

物理化学性质&存储条件

分子量 553.54
分子式 C28H26F3N5O4
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

4-Amino-1-((3-methyloxetan-3-yl)methyl)-3-(1-(2-(3-(trifluoromethoxy)phenyl) acetyl)indolin-5-yl)-1,6-dihydro-7H-pyrrolo [2,3-d]pyridazin-7-one

参考文献

1. Zhang C, et al. Eur J Med Chem. 2024 Feb 5;265:116076.

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