A PKCα and PKCβ1 inhibitor with IC50 values of 2.3 and 6.2 nM

Gö 6976 – 1 mg

Brand:
Cayman
CAS:
136194-77-9
Storage:
-20
UN-No:
Non-Hazardous - /

Gö 6976 is a nonglycosidic indolocarbazole that inhibits protein kinase C (PKC) with IC50 values of 2.3 and 6.2 nM for PKCα and PKCβ1, respectively.{9057} It does not inhibit the activity of PKCδ, PKCε, or PKCζ (IC50s > 3 μM), indicating a preference for the Ca2+-dependent subtypes, PKCα and PKCβ1.{9057} Gö 6976 also inhibits the checkpoint kinases Chk1/2.{30717} It was shown to abrogate DNA damage-induced S- and G2-phase cell cycle arrest, leading to cytotoxicity in p53 mutant tumor cells.{30717,24026}  

 

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Description

A PKCα and PKCβ1 inhibitor with IC50 values of 2.3 and 6.2 nM, respectively; also inhibits the checkpoint kinases Chk1/2 and abrogates DNA damage-induced cell cycle arrest, leading to cytotoxicity in p53 mutant tumor cells

Formal name: 5,6,7,13-tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile

Synonyms:  PD 406976

Molecular weight: 378.4

CAS: 136194-77-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Signaling|PKC Signaling

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