K-975

    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.


Chemical Structure

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K-975
CAS# 2563855-03-6

Theoretical Analysis

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

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

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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.