A selective PKC inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC; exhibits PKC isozyme specificity with preference for PKCα over PKCβI

Bisindolylmaleimide VIII (acetate) – 5 mg

Brand:
Cayman
CAS:
138516-31-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bisindolylmaleimide VIII (BIM VIII) is a selective protein kinase C (PKC) inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC.{17342,17339} This compound exhibits some degree of PKC isozyme specificity with preference for PKCα over PKCβI, PKCβII, PKCγ, or PKCε (IC50s = 53, 195, 163, 213, and 175 nM, respectively).{17342} At 10 µM BIM VIII does not inhibit the tyrosine phosphorylation or the activation of phospholipase C γ1.{17340} BIM VIII inhibits carbachol-evoked noradrenaline release from human SH-SY5Y neuroblastoma cells with an IC50 value of 600 nM.{17341}  

 

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Description

A selective PKC inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC; exhibits PKC isozyme specificity with preference for PKCα over PKCβI, PKCβII, PKCγ, or PKCε (IC50s = 53, 195, 163, 213, and 175 nM, respectively)

Formal name: 3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione, acetate

Synonyms:  BIM VIII|Ro 31-7549

Molecular weight: 458.5

CAS: 138516-31-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling

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