1402612-58-1
Chemical Structure
KT195
- CAS No.: 1402612-58-1
- Formula:C27H26N4O2
- Molecular Weight:438.52
IUPAC Name: (4-(4'-methoxy-[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-phenylpiperidin-1-yl)methanone
InChIKey: OEHLNQDRVMDXQD-UHFFFAOYSA-N
SMILES: O=C(N1CCCCC1C2=CC=CC=C2)N3N=NC(C4=CC=C(C5=CC=C(OC)C=C5)C=C4)=C3
Biological Activity: KT195 is a serine hydrolase inhibitor that targets ABHD6 (IC50 = 10 nM) and ABHD2, with no significant activity against DAGLβ. KT195 inhibits endoplasmic reticulum calcium release and mitochondrial calcium uptake by targeting ABHD2, thereby blocking A23187 (HY-N6687) and H2O2-induced necrotic cell death and apoptosis. By inhibiting ABHD6 activity, KT195 significantly induces 2-AG accumulation in Neuro2A cells and reduces IL-1β secretion in lipopolysaccharide-treated macrophages. KT195 has been used as a negative control probe for DAGLβ and can be applied in studies of ABHD6 and ABHD2 in calcium signaling, lipid metabolism, neuronal function, and inflammatory[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
KT195 | KT195 is a serine hydrolase inhibitor that targets ABHD6 (IC50 = 10 nM) and ABHD2, with no significant activity against DAGLβ. KT195 inhibits endoplasmic reticulum calcium release and mitochondrial calcium uptake by targeting ABHD2, thereby blocking A23187 (HY-N6687) and H2O2-induced necrotic cell death and apoptosis. By inhibiting ABHD6 activity, KT195 significantly induces 2-AG accumulation in Neuro2A cells and reduces IL-1β secretion in lipopolysaccharide-treated macrophages. KT195 has been used as a negative control probe for DAGLβ and can be applied in studies of ABHD6 and ABHD2 in calcium signaling, lipid metabolism, neuronal function, and inflammatory. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Yun B, et al. Regulation of calcium release from the endoplasmic reticulum by the serine hydrolase ABHD2. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1226-1231. [Content Brief]
- [2]. Yun B, et al. Serine hydrolase inhibitors block necrotic cell death by preventing calcium overload of the mitochondria and permeability transition pore formation. J Biol Chem. 2014 Jan 17;289(3):1491-504. [Content Brief]
- [3]. Hsu KL, et al. DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nat Chem Biol. 2012 Dec;8(12):999-1007. [Content Brief]
- [4]. Manterola A, et al. Re-examining the potential of targeting ABHD6 in multiple sclerosis: Efficacy of systemic and peripherally restricted inhibitors in experimental autoimmune encephalomyelitis. Neuropharmacology. 2018 Oct;141:181-191. [Content Brief]
Keywords
