A cell-permeable inhibitor of PTPs (IC50s = 0.09-1.7 µM) through oxidation of the catalytic cysteine residue; inhibits redox-sensitive CYP isoforms with IC50 values less than 10 µM; inhibits the protein methyltransferases SETD8

BVT 948 – 5 mg

Brand:
Cayman
CAS:
39674-97-0
Storage:
-20
UN-No:
Non-Hazardous - /

BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC50s = 0.09-1.7 µM).{27664} It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.{27664} Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values less than 10 µM.{27664} BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm.{26934} Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.{27664,27665,27666}  

 

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Description

A cell-permeable inhibitor of PTPs (IC50s = 0.09-1.7 µM) through oxidation of the catalytic cysteine residue; inhibits redox-sensitive CYP isoforms with IC50 values less than 10 µM; inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm

Formal name: 4-hydroxy-3,3-dimethyl-2H-benz[g]indole-2,5(3H)-dione

Synonyms: 

Molecular weight: 241.2

CAS: 39674-97-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Cell Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation||Research Area|Neuroscience||Research Area|Toxicology|Drug Metabolism|Cytochrome P450

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