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K-975

🥰Excellent
Catalog No. T9954Cas No. 2563855-03-6

K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.

K-975

K-975

🥰Excellent
Purity: 99.81%
Catalog No. T9954Cas No. 2563855-03-6
K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
Pack SizePriceAvailabilityQuantity
1 mg$67In Stock
5 mg$163In Stock
10 mg$263In Stock
25 mg$528In Stock
50 mg$747In Stock
1 mL x 10 mM (in DMSO)$178In Stock
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Purity:99.81%
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Product Introduction

Bioactivity
Description
K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
In vitro
K-975 inhibits the cell proliferation of NRF2-non-expressing malignant pleural mesothelioma (MPM) cell lines, protein-protein interaction (PPI) between Halo-TAZ and TEAD1/4 and Halo-YAP and endogenous TEAD1/4 in NCl-H226 cells and the reporter activity in NCl-H661/CTGF-Luc cells with the maximum of ~70%, at concentration of 0.1-10000 nM at 144 h and 24 h, respectively [1]. K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells [1].
In vivo
K-975 (10-300 mg/kg; p.o. twice daily for 14 days) suppresses tumor growth by inhibiting TEAD-YAP1/TAZ signaling in MPM xenograft mouse models [1].
Chemical Properties
Molecular Weight287.74
FormulaC16H14ClNO2
Cas No.2563855-03-6
SmilesCc1ccc(NC(=O)C=C)cc1Oc1ccc(Cl)cc1
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 215 mg/mL (747.20 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.4754 mL17.3768 mL34.7536 mL173.7680 mL
5 mM0.6951 mL3.4754 mL6.9507 mL34.7536 mL
10 mM0.3475 mL1.7377 mL3.4754 mL17.3768 mL
20 mM0.1738 mL0.8688 mL1.7377 mL8.6884 mL
50 mM0.0695 mL0.3475 mL0.6951 mL3.4754 mL
100 mM0.0348 mL0.1738 mL0.3475 mL1.7377 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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