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MGH-CP1

Dangerous Goods

CAS number:896657-58-2    molecular formula:C20H24N4OS

overview

compound introduction

Information MGH-CP1 MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation . MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively. Targets TEAD4 (Cell-free assay); TEAD2 (Cell-free assay) 672 nM; 710 nM In vitro MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro. MGH-CP1 treatment markedly decreases the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 does not affect auto-palmitoylation of several ZDHHC-family palmitoyl acyltransferases, suggesting its selectivity toward TEADs. MGH-CP1 is a selective small-molecule pan-TEAD inhibitor by directly targeting TEAD auto-palmitoylation. In vivo MGH-CP1 inhibits TEAD activity in Lats1/2 KO intestine in vivo. MGH-CP1 can effectively inhibit the palmitoylation of TEAD proteins in the intestinal epithelium. MGH-CP1 is well tolerated and has no apparent adverse effect on overall animal health or body weight after 2 weeks of treatment. In contrast to its lack of apparent effect in wild-type intestine, MGH-CP1 treatment effectively inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO intestine. Cell Research(from reference) Cell lines:HEK293T cells, Lats1/2 conditional MEFs, MDA-MB-231 cells, Huh7 cells Concentrations:0.1 μM, 0.3 μM, 0.6 μM, 1 μM, 1.2 μM, 2.5 μM, 3 μM, 5 μM, 10 μM Incubation Time:24 h

Specs

Chinese alias-
English aliasMGH-CP1 | 896657-58-2 | N-[4-(adamantan-1-yl)phenyl]-2-(4H-1,2,4-triazol-3-ylsulfanyl)acetamide | 2-((1H-1,2,4-Triazol-5-yl)thio)-N-(4-(adamantan-1-yl)phenyl)acetamide | N-[4-(1-adamantyl)phenyl]-2-(1H-1,2,4-triazol-5-ylsulfanyl)acetamide | 2-[(4H-1,2,4-t
CAS number896657-58-2molecular formulaC20H24N4OS
molecular weight368.5 g/molExact mass10mM in DMSO
PSA96.000 Ųlogp5.100

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physicochemical properties

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Safety information

pictogram:
GHS07
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P321: 特殊处理(请参阅此标签上的...)。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时,请勿进食、饮水

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MSDS

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