1. Stem Cell/Wnt
  2. YAP
  3. K-975

K-975 

Cat. No.: HY-138565
Handling Instructions

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma.

For research use only. We do not sell to patients.

K-975 Chemical Structure

K-975 Chemical Structure

CAS No. : 2563855-03-6

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Description

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma[1].

IC50 & Target

TEAD[1]

In Vitro

K-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines[1].
K-975 (10-10000 nM; 24 h) inhibits protein-protein interaction (PPI) between Halo-YAP and endogenous TEAD1/4 and Halo-TAZ and TEAD1/4 in NCI-H226 cells[1].
K-975 (0.1-10000 nM; 24 h) strongly inhibits the reporter activity in NCI-H661/CTGF-Luc cells, with the maximum inhibition of ~70%, and does not inhibit the reporter activity in NCI-H661/NRF2-Luc cells[1].
K-975 (1-10000 nM; 24 h) decreases the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCI-H226 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: NF2-non-expressing MPM and NF2-expressing malignant MPM cells
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 144 hours
Result: Had a stronger inhibitory effect against NF2-non-expressing cell lines than NF2-expressing cell lines.
Inhibited the proliferation of MSTO-211H cells, an NF2-expressing cell line.

Western Blot Analysis[1]

Cell Line: NCI-H226 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 24 hours
Result: Inhibited TEAD1-YAP1 PPI and TEAD4-YAP1 PPI.
Inhibited TEAD1-TAZ PPI and TEAD4-TAZ PPI.
In Vivo

K-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models[1].

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

Animal Model: Male SCID mice (5 weeks) injected with NCI-H226 or MSTO-211H cells[1]
Dosage: 10, 30, 100, 300 mg/kg
Administration: P.o. twice a day for 14 days
Result: Exhibited strong anti-tumor effect in MPM s.c. xenograft mouse models. Decreased the expressions of CTGF, IGFBP3, and NPPB, and increased the expression of FBXO32 in the NCI-H226 xenograft model.
Molecular Weight

287.74

Formula

C₁₆H₁₄ClNO₂

CAS No.

2563855-03-6

SMILES

C=CC(NC1=CC=C(C)C(OC2=CC=C(Cl)C=C2)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

K-975K975K 975YAPYes-associated proteinTEADYAP1TAZCys359antitumormalignantpleuralmesotheliomacancerInhibitorinhibitorinhibit

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