WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 463182
CAS#: 2563855-03-6
Description: K-975 is a first-in-class TEAD inhibitor, directly inhibiting YAP/TAZ-TEAD protein-protein interaction and showing a potent anti-tumor effect in malignant pleural mesothelioma. K-975 was covalently bound to an internal cysteine residue located in the palmitate-binding pocket of TEAD. K-975 had a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD in cell-free and cell-based assays. Furthermore, K-975 potently inhibited the proliferation of NF2-non-expressing MPM cell lines compared with NF2-expressing MPM cell lines. K-975 also suppressed tumor growth and provided significant survival benefit in MPM xenograft models.
MedKoo Cat#: 463182
Name: K-975
CAS#: 2563855-03-6
Chemical Formula: C16H14ClNO2
Exact Mass: 287.0713
Molecular Weight: 287.743
Elemental Analysis: C, 66.79; H, 4.90; Cl, 12.32; N, 4.87; O, 11.12
This product is not in stock, which may be available by custom synthesis.
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Synonym: K-975; K975; K 975;
IUPAC/Chemical Name: N-(3-(4-chlorophenoxy)-4-methylphenyl)acrylamide
InChi Key: KPXAHQSIROUBPH-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H14ClNO2/c1-3-16(19)18-13-7-4-11(2)15(10-13)20-14-8-5-12(17)6-9-14/h3-10H,1H2,2H3,(H,18,19)
SMILES Code: C=CC(NC1=CC=C(C)C(OC2=CC=C(Cl)C=C2)=C1)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 287.743 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1. Kaneda A, Seike T, Danjo T, Nakajima T, Otsubo N, Yamaguchi D, Tsuji Y, Hamaguchi K, Yasunaga M, Nishiya Y, Suzuki M, Saito JI, Yatsunami R, Nakamura S, Sekido Y, Mori K. The novel potent TEAD inhibitor, K-975, inhibits YAP1/TAZ-TEAD protein-protein interactions and exerts an anti-tumor effect on malignant pleural mesothelioma. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415. PMID: 33415007; PMCID: PMC7783735.
2. Lee S, Chung G, Kim J, Oh HB. Electron capture dissociation mass spectrometry of peptide cations containing a lysine homologue: a mobile proton model for explaining the observation of b-type product ions. Rapid Commun Mass Spectrom. 2006;20(21):3167-75. doi: 10.1002/rcm.2708. PMID: 17016809.
