XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1 12.9 nM and 38.1 6.9 nM against MST1 and MST2, respectively. XMU-MP-1 also reduces the phosphorylation of LATS1/2, and YAP by inhibiting MST1/2 kinase activities.
XMU-MP-1 is on-target to MST1/2. XMU-MP-1 block MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 is dissolved in DMSO (stock concentration, 10 mM).
XMU-MP-1 displayed excellent in vivo pharmacokinetics and is able to augment mouse intestinal repair, as well as liver repair and regeneration, in both acute and chronic liver injury mouse models at a dose of 1 to 3 mg/kg via intraperitoneal injection. XMUMP-1 treatment exhibit substantially greater repopulation rate of human hepatocytes in the Fah-deficient mouse model than in the vehicle-treated control, indicating that XMU-MP-1 treatment might facilitate human liver regeneration.
XMUMP-1 is dissolved in 0.1% citric acid aqueous solution containing 20% Kolliphor HS 15.
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名称 | XMU-MP-1 |
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Iupac 化学名称 | XMU-MP-1 |
分子式 | C17H16N6O3S2 |
分子量 | 416.48 |
Smile | C[Si](C)(C)CSCCl |
InChiKey | IKWIERSJEROYFH-UHFFFAOYSA-N |
InChi | InChI=1S/C5H13ClSSi/c1-8(2,3)5-7-4-6/h4-5H2,1-3H3 |
Cas号 | |
MDL | MFCD17013410 |
相关CAS号 |
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