VT103

Protein target name:

TEAD1

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

up to 3 uM

Probe Availability

MedKoo Biosciences, Inc.

Probe Information

Target and Probe Information

Target Details

Target class:

Transcription factor

Subclass:

TEA domain

HUGO ID:

HGNC:11714

Entrez gene ID:

7003

UNIPROT ID:

P28347

Target alias:

AA; REF1; TCF13; TEF-1; NTEF-1; TCF-13; TEAD-1

Probe Details

Chemical Probes Portal ID:

CPP2364

PubChem CID:

137534047

SMILES string:

CN1C=NC(C2=C(NC3=CC=C(C(F)(F)F)C=C3)C=CC(S(=O)(NC)=O)=C2)=C1

InChi Key:

LLCVDQHLYHBAHR-UHFFFAOYSA-N

Control compound:

VT106

Orthogonal probe:

VT104

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

ΔTm (°C)

8.3 TEAD1, 4.1 TEAD2, 1.0 TEAD3, 1.9 TEAD4

Potency assay:

Thermal Shift Assays (TSA), Cell-free TEAD palmitoylation assay

Structure-activity relationship:

yes, to be published

In cell validation

On target activity in cells

Potency in cells:

IC50, GI50

1.02 ± 0.09 nM (Y), 1-21 nM (C)

Potency assay (cells):

YAP reporter assay (Y), Cell proliferation assay (C), Cell-based TEAD palmitoylation assays (APEGS Assay)

Off target activity in cells

Potency in cells, off target:

GI50

Potency assay, off target (cells):

Anti-proliferation activity in a panel of mesothelioma cell lines

Probe Selectivity in Cell:

GI50 (nM) NCI-H226 1, NCI-H2373 2, Mero-48a 5, SDM103T2 2, NCI-H2052 10, ACC-MESO-1 5, ZL34 21, JU77 232, Mero-95 >10000, ZL55 >10000, ZL5 >10000, Mero-82 >10000, ONE58 >2000, Mero-14 >10000, Mero-83 >10000, Mero-41 >10000, SPC111 >10000, SPC212 >10000, NO36 >10000, Mero-84 >10000, ACC-MESO-4 >10000, Mero-25 >10000, NCI-H28 >3000, NCI-H2452 >3000, MSTO-211H >3000.

In vivo validation

Organism:

Mouse

Dose:

10 mg/Kg

Route of delivery:

OralIntravenous

Plasma half life:

13.2 h (IV)

Systemic clearance:

4.7 mL/min/kg (IV)

Cmax:

896 ng/mL (PO)

Tmax:

1 h (PO)

Vss:

4.5 L/kg (IV)

AUC:

20.0 (IV), 14.9 (PO) μg*h/mL

Bioavailability:

75 %

Primary Reference

Reference (doi):

1535-7163.MCT-20-0717

Reference (PMID):

33850002

VT103

Probe Availability

Probe Information

Target Details

AA; REF1; TCF13; TEF-1; NTEF-1; TCF-13; TEAD-1

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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VT103

Probe Availability

Probe Information

Target Details

AA; REF1; TCF13; TEF-1; NTEF-1; TCF-13; TEAD-1

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?