2351820-19-2

2351820-19-2 structure

Name: (±)-trans-GK563
Chemical Name: (±)-trans-GK563
CAS Number: 2351820-19-2
Molecular Formula: C₁₆H₂₂O₂
Molecular Weight: 246.345
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2021-08-11 14:37:01
Modify Date: 2024-01-13 22:06:43
GK563 is a selective Ca2+-independent phospholipase A2 (GVIA iPLA2) inhibitor with an IC50 value of 1 nM. GK563 is 22000 times more active against GVIA iPLA2 than GIVA cPLA2. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes[1].

Name	(±)-trans-GK563
Synonyms	(Â±)-trans-GK563 (3S,4S)-3-(4-Phenylbutyl)-4-propyl-2-oxetanone 2-Oxetanone, 3-(4-phenylbutyl)-4-propyl-, (3S,4S)-

Description	GK563 is a selective Ca2+-independent phospholipase A2 (GVIA iPLA2) inhibitor with an IC50 value of 1 nM. GK563 is 22000 times more active against GVIA iPLA2 than GIVA cPLA2. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase Research Areas >> Inflammation/Immunology
Target	IC50: 1 nM (GVIA iPLA2), 22 μM (GVIA cPLA2)[1]
In Vitro	GK563 (0.091 M) inhibits the activity of 100% GVIA iPLA2, 88% GVIA cPLA2 and 25% GV sPLA2[1]. GK563 (0-0.1 μM) inhibits GVIA iPLA2 with a XI(50) value of 0.0000021 and inhibits GVIA cPLA2 with an IC50 value of 22 μM[1]. GK563 (0-0.1 μM) shows a better inhibitory effect than fluoroketone FKGK18 to GVIA iPLA2 with an IC50 value of 1 nM[1]. GK563 (0-0.1 μM; 16 h) reduces β-cell apoptosis induced by proinflammatory cytokines[1]. Apoptosis Analysis[1] Cell Line: β-cell line Concentration: 0.1-10 μM Incubation Time: 16 h Result: Promoted a slight but modest rise in cell death when worked alone, but produced a concentration-dependent inhibition of β-cell apoptosis by the co-treatment of cells with cytokines.