Chemical Structure : LK01003
CAS No.:
LK01003
(LK-01003)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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451.60
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Formula
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C24H25N3O2S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-cyclopentyl-N-(6-(isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine
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References
1. Su H, et al. Nat Commun. 2025 May 8;16(1):4288.
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