| Identification | Back Directory | [Name]
Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]- | [CAS]
2290608-13-6 | [Synonyms]
VT103
Benzenesulfonamide, N-methyl-3-(1-methyl-1H-imidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]amino]- | [Molecular Formula]
C18H17F3N4O2S | [MDL Number]
MFCD34567638 | [MOL File]
2290608-13-6.mol | [Molecular Weight]
410.41 |
| Chemical Properties | Back Directory | [Boiling point ]
583.6±60.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (121.83 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.55±0.50(Predicted) | [color ]
Off-white to gray |
| Hazard Information | Back Directory | [Biological Activity]
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[1].
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[1].VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1[1].
VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg[1]. | [References]
[1]. Tang TT, et al. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021;20(6):986-998. |
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