XMU-MP-1 HYDROCHLORIDE

Stock Code: 3576005
Manufacturer Part No: SML2233-25MG
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£892.82 (exc VAT) per 25MG
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Biochem/physiol Actions


XMU-MP-1 inhibits MST kinase activity (IC50 = 9.8 nM/MST1, 18.2 nM/MST2, 44.8 nM/MST3, 27.3 nM/MST4) in a reversible and ATP-competitive manner (MST1 IC50/[ATP] = 164 nM/10 µM and 4036 nM/300 µM; MST2 IC50/[ATP] = 34 nM/10 µM and 1498 nM/300 µM), exhibiting significant affinity and/or inhibitory potency toward only 17 other kinases among a panel of 468 (401 unique kinases). XMU-MP-1 selectively inhibits H2O2-stimulated MST autophosphorylation and phosphorylation of endogenous MST1/2 substrates (MOB1, LATS, YAP), but not JNK, in human and murine cells (Effective conc. 1 µM), effectively upregulating YAP nuclear localization and protecting HepG2 cells (3 µM) against MST2 overexpression-induced cell death. XMU-MP-1 exhibits in vivo efficacy toward liver and intestinal repair and regeneration in various murine models (1-3 mg/kg/day i.p.) and oral availability in rats (t1/2 = 5.18 h, Tmax = 3 h, AUC = 993 ng h/mL, F = 39.48%; 10 mg/mL p.o.).

Colourwhite to beige
ManufacturerSIGMA-ALDRICH
Storage Temp.−20°C
SolubilityDMSO: 2 mg/mL, clear (warmed)
Formpowder
Assay≥98% (HPLC)

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