| Name | VT103 |
| Description | VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP/TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP/TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer. |
| In vitro | VT103 (3 mmol/L; 4 or 24 h; NF2-deficient NCI-H226 cells) selectively disrupts YAP–TEAD1 interaction.[1]
VT103 (3 μM; HEK293T cells) appeared to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4.[1]
VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1. VT103 shows an IC50 of 1.02 nM in the YAP reporter assay.[1] |
| In vivo | VT103 (0.3~10 mg/kg; p.o.; once daily; NCI-H226-tumor-bearing mice) inhibits tumor growth, with efficacy observed at 0.3 mg/kg[1]. Pharmacokinetics of VT103 in mice.[1] |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (121.83 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2.5 mg/mL (6.09 mM), Sonication is recommended.
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| Keywords | YAP–TEAD | VT103 |
| Inhibitors Related | AICAR | MY-1076 | YAP-TEAD-IN-3 | Verteporfin | DC-TEADin02 | MSC-4106 | Thiostrepton | OPN-9652 | VT107 | VT104 | alpha-Ionone | MYF-01-37 |
| Related Compound Libraries | Bioactive Compound Library | Anti-Breast Cancer Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Prostate Cancer Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Active Compound Library |
United States
