EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
EMT inhibitor-1 (5-20 mg/kg; intraperitoneal injection) exerts strong antitumor activity in a mouse tumor model. Mechanistically, EMT inhibitor-1 induces GSK3-β–mediated degradation of the Hippo transducer TAZ, through activation of the Hippo kinases Mst/Lats and the tumor suppressor kinase AMPK upstream of the degradation complex.
| Molecular Weight | 319.21 |
| Formula | C12H12Cl2N2O2S |
| CAS Number | 1638526-21-2 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Hippo (MST) Products |
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| IHMT-MST1-58
IHMT-MST1-58 is an orally active, potent and selective inhibitor of STE20-like protein 1 kinase (MST1) with an IC50 value of 23 nM.It can be used in studies related to type 1 or type 2 diabetes. |
| I3MT-3
I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST. |
| XMU-MP-1
XMU-MP-1 is a potent and selective Hippo/ MST1/2 inhibitor with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM, respectively. |
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