An inhibitor of JNK (IC50 = 280 nM); competitive for JNK1 binding with pepJIP1 (IC50 = 500 nM); selective for JNK over p38α

BI-78D3 – 25 mg

Brand:
Cayman
CAS:
883065-90-5
Storage:
-20
UN-No:
Non-Hazardous - /

BI-78D3 is an inhibitor of JNK (IC50 = 280 nM in a TR-FRET assay) that is competitive for JNK1 binding with pepJIP1, a JNK-interacting protein, with an IC50 value of 500 nM.{38279} It is selective for JNK, being 100-fold less active for the structurally similar MAPK family protein p38α and inactive at mammalian target of rapamycin (mTOR) or phosphatidylinositol 3-kinase α (PI3Kα). In a cell-based kinase assay, BI-78D3 inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM). In a mouse model of type 2 diabetes, BI-78D3 (25 mg/kg) restores insulin sensitivity, reducing blood glucose levels when administered 30 minutes prior to insulin. BI-78D3 (30 µM) reduces contractions in human prostate strips induced by phenylephrine (Item Nos. 17205 | 18619) or norepinephrine (Item No. 16673) and reduces phosphorylation of c-Jun, a JNK substrate.{38280}  

 

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Description

An inhibitor of JNK (IC50 = 280 nM); competitive for JNK1 binding with pepJIP1 (IC50 = 500 nM); selective for JNK over p38α, mTOR, and PI3Kα; inhibits c-Jun phosphorylation induced by TNF-α (EC50 = 12.4 µM); restores insulin sensitivity in a mouse model of type 2 diabetes when administered at 25 mg/kg 30 minutes prior to insulin; reduces human prostate strip contractions induced by phenylephrine or norepinephrine when applied at 30 µM and reduces phosphorylation of c-Jun, a JNK substrate,

Formal name: 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2,4-dihydro-5-[(5-nitro-2-thiazolyl)thio]-3H-1,2,4-triazol-3-one

Synonyms:  c-Jun N-terminal Kinase Inhibitor X|JNK Inhibitor X

Molecular weight: 379.4

CAS: 883065-90-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JNK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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