VT103

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VT103 是 VT101 的类似物，是一种具有口服活性和选择性的 TEAD1 蛋白棕榈酰化抑制剂。 VT103 抑制 YAP/TAZ-TEAD 促进的基因转录，阻断 TEAD auto-palmitoylation，阻断 YAP/TAZ和TEAD 之间的相互作用。VT103 可用于癌症研究。

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer.

VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP–TEAD1 interaction.VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1.VT103 shows an IC50 of 1.02 nM in YAP reporter assay.

VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg.Animal Model:NCI-H226-tumor bearing miceDosage:0.3~10 mg/kg Administration:P.o. once per day Result:Blocked tumor growth even at 0.3 mg/kg.

——

Others

Other Targets

YAP

——

——

2290608-13-6

410.41

C18H17F3N4O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (121.83 mM; 超声助溶 )

CNS(=O)(=O)c1ccc(Nc2ccc(cc2)C(F)(F)F)c(c1)-c1cn(C)cn1

——

(-20℃)

With Ice Pack

≥ 2 years