XMU-MP-1

XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50s of 71.1 and 38.1 nM, respectively.

Product information

CAS Number: 2061980-01-4

Molecular Weight: 416.48

Formula: C17H16N6O3S2

Chemical Name: 4-({2,9-dimethyl-8-oxo-6-thia-2,9,12,14-tetraazatricyclo[8.4.0.0³,⁷]tetradeca-1(14),3(7),4,10,12-pentaen-13-yl}amino)benzene-1-sulfonamide

Smiles: CN1C2=NC(NC3C=CC(=CC=3)S(N)(=O)=O)=NC=C2N(C)C(=O)C2SC=CC1=2

InChiKey: YRDHKIFCGOZTGD-UHFFFAOYSA-N

InChi: InChI=1S/C17H16N6O3S2/c1-22-12-7-8-27-14(12)16(24)23(2)13-9-19-17(21-15(13)22)20-10-3-5-11(6-4-10)28(18,25)26/h3-9H,1-2H3,(H2,18,25,26)(H,19,20,21)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 8 mg/mL (19.21 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

At concentrations ranging from 0.1 to 10 μM, XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in HepG2 cells in a dose-dependent manner. XMU-MP-1 treatment inhibits hydrogen peroxide-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a variety of cell lines, including mouse macrophage-like cells, human osteosarcoma, human colorectal adenocarcinoma cells. XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 can potently and reversibly suppress the activities of kinases MST1/2 and enhance their downstream YAP activation in cells.

In Vivo:

XMU-MP-1 displays excellent in 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 exhibits 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.

Products are for research use only. Not for human use.