An inhibitor of MST1 and MST2 (IC50s = 71.1 and 38.1 nM

XMU-MP-1 – 5 mg

Brand:
Cayman
CAS:
2061980-01-4
Storage:
-20
UN-No:
Non-Hazardous - /

XMU-MP-1 is an inhibitor of the pro-apoptotic, sterile 20-like kinases MST1 and 2 (IC50s = 71.1 and 38.1 nM, respectively).{38542} It is selective for MST1 and 2 over a panel of 468 kinases at a concentration of 1 μM. XMU-MP-1 inhibits phosphorylation of MOB1, LATS1 and 2, and YAP in HepG2 cells as well as MST1 and 2 autophosphorylation in RAW 264.7, U2OS, SW480, RPE1, SNU423, and HepG2 cells in a concentration-dependent manner. It also prevents cell death induced by overexpression of MST2. XMU-MP-1 (1 mg/kg) enhances liver regeneration in mice post partial hepatectomy and reduces liver fibrosis in a mouse model of chronic liver injury.  

 

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Description

An inhibitor of MST1 and MST2 (IC50s = 71.1 and 38.1 nM, respectively); is selective for MST1 and 2 over a panel of 468 kinases at a concentration of 1 μM; inhibits phosphorylation of MOB1, LATS1 and 2, and YAP in HepG2 cells as well as MST1 and 2 autophosphorylation in RAW 264.7, U2OS, SW480, RPE1, SNU423, and HepG2 cells in a concentration-dependent manner; prevents cell death induced by overexpression of MST2; enhances liver regeneration in mice post partial hepatectomy and reduces liver fibrosis in a mouse model of chronic liver injury when administered at a dose of 1 mg/kg,

Formal name: 4-[(6,10-dihydro-5,10-dimethyl-6-oxo-5H-pyrimido[5,4-b]thieno[3,2-e][1,4]diazepin-2-yl)amino]-benzenesulfonamide

Synonyms: 

Molecular weight: 416.5

CAS: 2061980-01-4

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Endocrinology & Metabolism

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