ABHD16A Inhibitor, KC01

A cell-permeable beta-lactone based compound that acts as a potent, selective, and covalent inhibitor of phosphatidylserine (PS) lipase ABHD16A (BAT5, IC₅₀ = 90 and 520 nM for human and mouse ABHD16A, respectively). Displays reduced effect on ~60 other serine hydrolases profiled. Shown to block the PS lipase activity of membrane fractions from COLO205, K562 and MCF7 cell lines and is also shown to diminish the PS lipase activity of brain membrane lysates from Abhd12+/+ (IC₅₀ = 290 nM) and Abhd12-/- (IC₅₀ = 340 nM) mice. Significantly reduces lysophosphatidylserine (lyso-PSs) levels in cells, without affecting the levels of other lipids, such as phosphatidylcholine (PC), phosphatidylethano-lamines (PE), lyso-PCs, lyso-PEs or monoacylglycerols. Blunts lipopolysaccharide-induce release of IL-6, IL-1β in mouse macrophages.

A cell-permeable beta-lactone based compound that acts as a potent, selective, and covalent inhibitor of phosphatidylserine (PS) lipase ABHD16A (BAT5, IC₅₀ = 90 and 520 nM for human and mouse ABHD16A, respectively). Displays reduced effect on ~60 other serine hydrolases profiled. Shown to block the PS lipase activity of membrane fractions from COLO205, K562 and MCF7 cell lines and is also shown to diminish the PS lipase activity of brain membrane lysates from Abhd12+/+ (IC₅₀ = 290 nM) and Abhd12-/- (IC₅₀ = 340 nM) mice. Significantly reduces lysophosphatidylserine (lyso-PSs) levels in cells, without affecting the levels of other lipids, such as phosphatidylcholine (PC), phosphatidylethano-lamines (PE), lyso-PCs, lyso-PEs or monoacylglycerols. Blunts lipopolysaccharide-induce release of IL-6, IL-1β in mouse macrophages.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
ABHD16A

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Kamat, S., et al. 2015. Nat. Chem. Biol.11, 164.

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