5.34349

ABHD16A Inhibitor, KC01

• Synonym(s): ABHD16A Inhibitor, KC01, (Z)-6-(2-oxo-4-tridecyloxetan-3-ylidene)hexanamide, BAT5 Inhibitor, KC01
• Empirical Formula (Hill Notation): C₂₂H₃₉NO₃
• Molecular Weight: 365.55
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 5 mg/mL
• storage temp.: −20°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ABHD16A

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable