VT00278 | YAP/TEAD inhibitor | Probechem Biochemicals

Chemical Structure : VT00278

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VT00278 (VT-00278)

货号: PC-28468Not For Human Use, Lab Use Only.

VT00278 is a small molecule YAP/TEAD inhibitor, strongly binds to TEAD4 with SPR KD of 3.52 uM, downregulates YAP/TEAD transcriptional activity and potently suppresses tumor-promoting phenotypes including proliferation, invasion and tumor sphere formation.

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生物&药学活性

VT00278 is a small molecule YAP/TEAD inhibitor, strongly binds to TEAD4 with SPR KD of 3.52 uM, downregulates YAP/TEAD transcriptional activity and potently suppresses tumor-promoting phenotypes including proliferation, invasion and tumor sphere formation.
VT00278 is 10-fold more potent in inhibiting YAP/TEAD reporter activity than its parental compound CA3.
VT00278 greatly down-regulates YAP/TEAD transcriptional activity in the gastric cancer (GC) cell line AGS and GA0518 tumor cells.
VT00278 (200 nM) downregulates genes involved in cell adhesion and cell junctions (both closely linked to the Hippo signaling pathway) in GA0518 cells.
VT00278 exhibits potent antitumor effects and disturbed RNA polymerase II activity, especially inhibiting tumor proliferation, invasion, and cancer stem cell traits.
VT00278 markedly downregulates regulators of RNAPII transcription, impairs cell cycle checkpoints, and strongly induces apoptosis.
VT00278 robustly induces DNA damage, and enhances response to immunotherapy via activating the cytosolic DNA sensing pathway in vivo.
VT00278 exerts strong anti-tumor activity and enhanced the efficacy of immune checkpoint blockade in KP-luc2 syngeneic model.

物理化学性质&存储条件

分子量	643.78
分子式	C33H33N5O5S2
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	2,7-bis((4-phenylpiperazin-1-yl)sulfonyl)-9H-fluoren-9-one oxime

参考文献

1. Zhang YY, et al. Mol Cancer Ther. 2026 Oct 8. doi: 10.1158/1535-7163.MCT-25-1491.

VT00278 (VT-00278)

生物&药学活性

物理化学性质&存储条件

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VT00278 (VT-00278)

生物&药学活性

物理化学性质&存储条件

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