K-975 - 10mM in DMSO , CAS No.2563855-03-6

CAS: 2563855-03-6 Cat. No.: K655238 Formula: C₁₆H₁₄ClNO₂ Peso molecolare: 287.74 PubChem CID: 155353714

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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

In Vitro

K-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines. 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. 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AnalysisCell 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 . 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 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.\nDecreased the expressions of CTGF , IGFBP3 , and NPPB , and increased the expression of FBXO32 in the NCI-H226 xenograft model.

IC50& Target:TEAD

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

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 acrylami

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

• PubChem CID: 155353714
• Peso molecolare: 287.74

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2563855-03-6, the molecular formula is C16H14ClNO2, and the molecular weight is 287.74 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.