LC-TEAD01
LC-TEAD01 is a potent covalent transcription enhancer-associated domain (TEAD) inhibitor with an IC50 of 116 nM and a Ki of 0.132 μM. LC-TEAD01 disrupts the TEAD-YAP interaction and inhibits TEAD-dependent transcriptional activity. LC-TEAD01 suppresses the proliferation of NF2-deficient cancer cells. LC-TEAD01 inhibits tumor growth in NF2-deficient xenograft models. LC-TEAD01 can be used in studies related to NF2-deficient malignant pleural mesothelioma.
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- Fòrmula: C13H16N4O3S
- Peso molecular:308.36
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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TEAD 116 nM (IC50) |
TEAD 0.132 μM (Ki) |
LC-TEAD01 (1 h) binds to the lipid pocket of purified TEAD1 protein with an IC50 of 116 nM[1].
LC-TEAD01 inhibits the autopalmitoylation of purified TEAD1 protein, with an IC50 value of 220 nM[1].
LC-TEAD01 disrupts the interaction between purified TEAD1 protein and YAP peptide, with an IC50 of 48.29 nM, and this effect depends on binding to Cys359[1].
LC-TEAD01 (0.0001-100 μM; 5 days) potently and selectively inhibits the proliferation of NF2-deficient NCI-H226 mesothelioma cells, with an IC50 of 0.618 μM[1].
LC-TEAD01 (0-30 μM) dose-dependently disrupts the TEAD1-YAP protein-protein interaction in HEK-293T cells overexpressing TEAD1 and YAP proteins[1].
LC-TEAD01 (0-3 μM) dose-dependently inhibits TEAD-dependent transcriptional activity in HEK-293T cells transfected with a TEAD-responsive luciferase reporter gene[1].
LC-TEAD01 (0.625-2.5 μM) reduces the mRNA expression levels of TEAD downstream target genes CTGF and CYR61 in NCI-H226 cells in a dose-dependent manner[1].
LC-TEAD01 (0.625-10 μM) dose-dependently inhibits the protein expression of CYR61, a downstream target gene of TEAD, in NCI-H226 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H226 (NF2-deficient mesothelioma), NCI-H2452 (NF2 wild-type mesothelioma), HEK-293T
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Concentration:0.0001, 0.01, 1, 100 μM
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Incubation Time:5 days
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Result:Inhibited proliferation of NCI-H226 cells with an IC50 of 0.618 μM.
Inhibited proliferation of NCI-H2452 cells with an IC50 of 9.839 μM.
Showed minimal activity against HEK-293T cells (IC50 > 15 μM).
Exhibited a selectivity ratio between NCI-H2452 and NCI-H226 cells exceeding 17-fold.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c Nude (male, 6 weeks old, subcutaneously injected with 2 × 106 NCI-H226 NF2-deficient malignant pleural mesothelioma cells)[1]
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Dosage:30 mg/kg; 50 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Induced marked tumor growth inhibition relative to vehicle control.
Did not cause significant body weight loss.
Reduced tumor cellularity, increased intratumoral vacuolization, and decreased Ki67-positive cell proportions in treated tumors.
Significantly downregulated TEAD downstream target gene CYR61 mRNA and protein levels in tumor tissues.
Chemical Information
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Peso molecular 308.36
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Fòrmula C13H16N4O3S
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SMILES
C=CS(=O)(NCC1=CN(N=N1)C2=CC=C(C=C2)OCC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LC-TEAD01 Related Classifications
HY-183728 Related Classifications
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