VT103

Research use only, not for human use.

VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101.

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.

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Others

Other Targets

YAP

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2290608-13-6

410.41

C18H17F3N4O2S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (121.83 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years