LK01003 | RIPK3 inhibitor | Probechem Biochemicals

Chemical Structure : LK01003

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LK01003 (LK-01003)

货号: PC-24570Not For Human Use, Lab Use Only.

LK01003 is a potent, highly selective inhibitor targeting RIPK3 with IC50 of 2 nM in ADP-Glo assays, shows anti-necroptotic activities in L929 cells with EC50 of 3.7 uM.

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生物&药学活性

LK01003 is a potent, highly selective inhibitor targeting RIPK3 with IC50 of 2 nM in ADP-Glo assays, shows anti-necroptotic activities in L929 cells with EC50 of 3.7 uM.
LK01003 demonstrates significantly enhanced on-target selectivity against a panel of 379 kinases with an S (35) score of approximately 0.005, wekaly inhibits RIPK2 and BRK with 24 and 124-fold selectivity.
LK01003 inhibits HT29 cells, zVAD, human TNF-α, and Smac mimetic SM-164 induced necroptosis with EC50 of 7.9 uM.
LK01003 is much more potent than GSK'872 to block necroptosis in HT29 cells.
LK01003 effectively inhibits RIPK3 and MLKL phosphorylation induced by TNF-α in both L929 and HT29 cells.
LK01003 mimics the R69H mutation and achieves remarkably high selectivity, engaging a unique hydrophobic site and stabilizing an inactive conformation of RIPK3.

物理化学性质&存储条件

分子量	451.60
分子式	C24H25N3O2S2
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-cyclopentyl-N-(6-(isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine

参考文献

1. Su H, et al. Nat Commun. 2025 May 8;16(1):4288.

LK01003 (LK-01003)

生物&药学活性

物理化学性质&存储条件

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LK01003 (LK-01003)

生物&药学活性

物理化学性质&存储条件

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