1. Metabolic Enzyme/Protease Apoptosis
  2. Phospholipase Apoptosis
  3. GK563

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.

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GK563

GK563 Chemische Struktur

CAS. Nr. : 2351820-19-2

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Beschreibung

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].

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molekulargewicht

246.34

Formel

C16H22O2

CAS. Nr.
SMILES

CCC[C@H]1[C@@H](C(O1)=O)CCCCC2=CC=CC=C2

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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