2. Stem Cell/Wnt
  3. YAP
  4. 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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LC-TEAD01

LC-TEAD01 Chemical Structure

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LC-TEAD01 Related Antibodies

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

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Description

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[1].

IC50 & Target[1]

TEAD

116 nM (IC50)

TEAD

0.132 μM (Ki)

In Vitro

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.

LC-TEAD01 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: NCI-H226 (NF2-deficient mesothelioma), NCI-H2452 (NF2 wild-type mesothelioma), HEK-293T
Concentration: 0.0001, 0.01, 1, 100 μM
Incubation Time: 5 days
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.
Parmacokinetics
Species Dose Route Cmax AUC0-∞
Rat[1] 10 mg/kg p.o. 81.4 ng/mL 78.8 ng·h/mL
Rat[1] 50 mg/kg i.p. 6207 ng/mL 4291 ng·h/mL
In Vivo

LC-TEAD01 (30-50 mg/kg; i.p.; daily; 21 days) exhibits potent, well-tolerated antitumor activity in NF2-deficient NCI-H226 mesothelioma xenografts, reducing tumor growth, proliferation, and TEAD-dependent gene expression[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c Nude (male, 6 weeks old, subcutaneously injected with 2 × 106 NCI-H226 NF2-deficient malignant pleural mesothelioma cells)[1]
Dosage: 30 mg/kg; 50 mg/kg
Administration: i.p.; daily; 21 days
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.
Molecular Weight

308.36

Formula

C13H16N4O3S
SMILES

C=CS(=O)(NCC1=CN(N=N1)C2=CC=C(C=C2)OCC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LC-TEAD01 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LC-TEAD01YAPYes-associated proteinTEADNF2-deficient cancer cellsNCI-H226 mesothelioma cellsNCI-H2452 cellsCys359NF2-deficient malignant pleural mesotheliomaTEAD1HEK-293T cellsNF2-deficient xenograftsInhibitorinhibitorinhibit

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