IHMT-MST1-58_product_DataBase

Bioactivity	IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes[1].
Invitro	IHMT-MST1-58 (compound 19) shows good activity against MST1 with an IC50 value of 23 nM[1].IHMT-MST1-58 (1 μM) displays strong inhibitory activity against MST1 (IC50 = 23 nM), weak activity against MST2 (IC50 = 652 nM), but no activity against NEK3 even at 10 μM (IC50 > 10 μM) [1].IHMT-MST1-58 (1 μM) shows strong binding affinity to MST1 and weak binding affinity to MST2 with Kd values of 240 nM and 2.7 μM[1].IHMT-MST1-58 (0.1-10 μM; 1-2 h) inhibits the phosphorylation of MST1 in vitro[1].IHMT-MST1-58 (0.03, 0.1 and 0.3 μM; 48 h) exhibits a significant protective effect of β cells from the damage caused by inflammatory cytokines[1]. Western Blot Analysis[1] Cell Line:
In Vivo	IHMT-MST1-58 (compound 19) (p.o, 50 mg/kg/day, QD) combination with metformin led to the decline of fasting blood glucose, show protective effect of β cells and decrease the hemoglobin A1c level in the STZ-induced T1D/T2D mouse models[1].Pharmacokinetic Parameters of IHMT-MST1-58 in different species (i.v. or p.o; 1 mg/kg, 5 mg/kg and 10 mg/kg)[1].
Name	IHMT-MST1-58
CAS	2414484-25-4
Formula	C21H22N6O3S
Molar Mass	438.50
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yun Wu, et al. Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes. J Med Chem. 2022 Sep 8;65(17):11818-11839

PeptideDB

IHMT-MST1-58

CAS: 2414484-25-4 F: C21H22N6O3S W: 438.50