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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-LC-TEAD01
LC-TEAD01

Chemical Structure : LC-TEAD01

CAS No.:

LC-TEAD01

货号: PC-26706Not For Human Use, Lab Use Only.

LC-TEAD01 is a potent, selective and covalent TEAD inhibitor with IC50 of 116 nM for TEAD1, inhibits TEAD1-YAP peptide binding with IC50 of 48.29 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LC-TEAD01 is a potent, selective and covalent TEAD inhibitor with IC50 of 116 nM for TEAD1, inhibits TEAD1-YAP peptide binding with IC50 of 48.29 nM.
LC-TEAD01 exhibits cellular proliferation activity in the NCI-H226 cell line with IC50 of 618 nM.
LC-TEAD01 covalently binds to the conserved palmitoylation site (Cys359) of TEAD1 ipid pocket (LP).
LC-TEAD01 is a pan-TEAD inhibitor that can bind to all four TEAD isoform proteins.
LC-TEAD01 shows effective suppression of TEAD-dependent transcriptional activity in transfected HEK-293T cells.
LC-TEAD01 (30 and 50 mg/kg, qd, i.p.) demonstrates vivo antitumor efficacy of LC-TEAD01 in an NCI-H226 xenograft model in nude mice.

物理化学性质&存储条件

分子量 322.38
分子式 C14H18N4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((1-(4-Propoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)ethenesulfonamide

参考文献

1. Yuhui Miao, et al. J Med Chem. 2026 May 5. doi: 10.1021/acs.jmedchem.6c00104.

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