896657-58-2
896657-58-2 structure
- Name: MGH-CP1
- Chemical Name: N-[4-(Adamantan-1-yl)phenyl]-2-(1H-1,2,4-triazol-5-ylsulfanyl)acetamide
- CAS Number: 896657-58-2
- Molecular Formula: C20H24N4OS
- Molecular Weight: 368.50
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2021-09-17 11:17:21
- Modify Date: 2024-01-14 20:35:52
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MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion[1].
| Name | N-[4-(Adamantan-1-yl)phenyl]-2-(1H-1,2,4-triazol-5-ylsulfanyl)acetamide |
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| Synonyms |
N-[4-(Adamantan-1-yl)phenyl]-2-(1H-1,2,4-triazol-5-ylsulfanyl)acetamide
Acetamide, 2-(1H-1,2,4-triazol-5-ylthio)-N-(4-tricyclo[3.3.1.13,7]dec-1-ylphenyl)- |
| Description | MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion[1]. |
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| Related Catalog | |
| Target |
IC50: 710 nM (TEAD2), 672 nM (TEAD4) [1] |
| In Vitro | MGH-CP1 (0-100 μM) inhibits auto-palmitoylation of recombinant TEAD2 and TEAD4 in a dose-dependent manner[1]. MGH-CP1 (0-2 μM) inhibits TEAD-binding sites (TBS)-Luc reporter activity in a dose-dependent manner in YAP-expressing HEK293 cells[1]. MGH-CP1 does not affect YAP nuclear localization or protein levels but potently inhibits TEAD-mediated transcription in a dose-dependent manner and effectively blocks cell over-proliferation[1]. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion[1]. |
| In Vivo | MGH-CP1 (75mg/kg; PO; daily, for 2 weeks) inhibits the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine[1]. Animal Model: Mice (induced high-dose Cre recombination by intraperitoneal injection of 120mg/kg Tamoxifen for two consecutive days)[1] Dosage: 75 mg/kg Administration: PO; daily, for 2 weeks Result: Effectively inhibited the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but effectively inhibited upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C20H24N4OS |
| Molecular Weight | 368.50 |
| Exact Mass | 368.167084 |
| LogP | 4.65 |
| Index of Refraction | 1.664 |
| Storage condition | 2-8°C |