Cat. No.: HY-138565

K-975

34 Cited Publications

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Based on 34 publication(s) in Google Scholar

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.

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Pureté: 99.89%
CAS No.: 2563855-03-6
Formule: C₁₆H₁₄ClNO₂
Masse moléculaire:287.74

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

K-975 Chemical Structure

CAS No.: 2563855-03-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (34)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

TEAD^[1]

Voir tous les produits spécifiques à Isoform YAP :

Cellular Effect

Cell Line	Type	Value	Description	References
MSTO-211H	IC₅₀	<100 nM Compound: 123; K-975	Antiproliferative activity against human MSTO-211H cells assessed as cell growth inhibition incubated for 144 hrs by CCK-8 assay Antiproliferative activity against human MSTO-211H cells assessed as cell growth inhibition incubated for 144 hrs by CCK-8 assay	[PMID: 36063664]
NCI-H226	IC₅₀	<100 nM Compound: 123; K-975	Antiproliferative activity against human NCI-H226 cells assessed as cells growth inhibition incubated for 144 hrs by CCK-8 assay Antiproliferative activity against human NCI-H226 cells assessed as cells growth inhibition incubated for 144 hrs by CCK-8 assay	[PMID: 36063664]

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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS No. 2563855-03-6
Appearance Solid
Masse moléculaire 287.74
Formule C₁₆H₁₄ClNO₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (34)

All IFApoptosis AnalysisIn Vivo Efficacy Study

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Journal Impact Factor

Nat Mater

2026 Feb 20.
Sci Adv

Extracellular fluid viscosity regulates human mesenchymal stem cell lineage and function. [Abstract]

2025 Jan 3;11(1):eadr5023. PMID: 39742493

K-975 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jan 3;11(1):eadr5023. [Abstract]

Nuclear-to-cytosolic ratio of RUNX2 and YAP incubated with K-975 (5 μM) or vehicle during the 6-day culture.
Cancer Lett

Identification of SPP1+ macrophages in promoting cancer stemness via vitronectin and CCL15 signals crosstalk in liver cancer. [Abstract]

2024 Aug 29:217199. PMID: 39216547

K-975 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Aug 29:217199. [Abstract]

Patient-derived organoids and SMMC-7721 cells were co-cultured with SPP1- or SPP1+ macrophages, then treated with 5-Fu combined with PBS, K-975 (20 nM) and integrin αvβ1 inhibitor. Cell apoptosis was assessed.

K-975 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Aug 29:217199. [Abstract]

Mice were treated with PBS, 5-Fu, 5-Fu combining with K-975 (2 mg/kg, once a week, 25 d) or integrin αvβ1 inhibitor. Tumor volume was recorded.

K-975 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Aug 29:217199. [Abstract]

Mice were treated with PBS, 5-Fu, 5-Fu combining with K-975 (2 mg/kg, once a week) or integrin αvβ1 inhibitor. Mice weight was assessed on day 25.

K-975 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Aug 29:217199. [Abstract]

Mice were treated with PBS, 5-Fu, 5-Fu combining with K-975 (2 mg/kg, once a week) or integrin αvβ1 inhibitor. Mice ALT and CRE level were assessed on day 25.
NPJ Precis Oncol

Refined high-content imaging-based phenotypic drug screening in zebrafish xenografts. [Abstract]

2023 May 18;7(1):44. PMID: 37202469
Br J Cancer

Fibroblast growth factor signals drive the metastatic behavior in small cell lung cancer. [Abstract]

2025 Dec 13. PMID: 41390896
Br J Cancer

Hyperglycaemia induces metabolic reprogramming into a glycolytic phenotype and promotes epithelial-mesenchymal transitions via YAP/TAZ-Hedgehog signalling axis in pancreatic cancer. [Abstract]

2023 Mar;128(5):844-856. PMID: 36536047

K-975 purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2023 Mar;128(5):844-856. [Abstract]

K975 (1, 5 μM; 24 h) successfully suppresses PDAC cells invasiveness.
Cell Rep

Hypoxia restores the acidosis-induced inhibition of cancer cell dissemination. [Abstract]

2026 Feb 24;45(2):116970. PMID: 41686638
Cell Rep

Mechanosensitive calcium channels and integrins coordinate the reprogramming of colorectal cancer cells into a fetal-like state. [Abstract]

2025 Sep 22;44(10):116308. PMID: 40986425
Cell Rep

YAP1 is a key regulator of EWS::FLI1-dependent malignant transformation upon IGF-1-mediated reprogramming of bone mesenchymal stem cells. [Abstract]

2025 Mar 11;44(3):115381. PMID: 40080499
Cell Rep

Lysine long-chain fatty acylation regulates the TEAD transcription factor. [Abstract]

2023 Apr 25;42(4):112388. PMID: 37060904
J Med Chem

Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106. [Abstract]

2022 Jul 14;65(13):9206-9229. PMID: 35763499
Commun Biol

Two distinct modes of Vgll4-mediated Tead regulation control organ size in zebrafish. [Abstract]

2026 Apr 25;9(1):574. PMID: 42032219
Int Immunopharmacol

ACTL6A accelerates the progression of NSCLC through hippo/YAP signaling axis and TAMs-mediated immune regulation. [Abstract]

2026 Jan 1;168(Pt 1):115828. PMID: 41223612
Sci Rep

PPARα activation promotes liver progenitor cell-mediated liver regeneration by suppressing YAP signaling in zebrafish. [Abstract]

2023 Oct 25;13(1):18312. PMID: 37880271
iScience

YAP condensates are highly organized hubs. [Abstract]

2024 May 7;27(6):109927. PMID: 38784009
Exp Dermatol

Targeting the Hippo/YAP/TAZ signalling pathway: Novel opportunities for therapeutic interventions into skin cancers. [Abstract]

2022 Oct;31(10):1477-1499. PMID: 35913427
Life Sci Alliance

Pipeline to evaluate YAP-TEAD inhibitors indicates TEAD inhibition represses NF2-mutant mesothelioma. [Abstract]

2025 Jul 31;8(10):e202503241. PMID: 40744733
Biochem Biophys Res Commun

Estrogen receptors regulate sex disparity in the immune responses during zebrafish liver regeneration following partial hepatectomy. [Abstract]

2024 Dec 17:738:150937. PMID: 39515092
Biosci Biotechnol Biochem

Identification of a derivative of the alkaloid emetine as an inhibitor of the YAP-TEAD interaction and its potential as an anticancer agent. [Abstract]

2023 Apr 24;87(5):501-510. PMID: 36809780
Res Sq

2026 Jun 17.
bioRxiv

YAP/TAZ inhibition refines TGF-β signaling to prevent laryngeal fibrosis. [Abstract]

2026 May 21:2026.05.18.726086. PMID: 42239264
SSRN

2026 Mar 20.
bioRxiv

2026 Mar 25.
Purdue University

2025 Jul 23.
the Scripps Research Institute

2025.
Preprints

2025 Mar 31.
bioRxiv

2024 November 12.
bioRxiv

2024 November 17.
University of Puerto Rico

2024 Jun.
bioRxiv

CRB2 Depletion Induces YAP Signaling and Disrupts Mechanosensing in Podocytes. [Abstract]

2024 Oct 26:2024.10.22.619513. PMID: 39484460
University of Southern Denmark

2024
bioRxiv

2023 Sep 17.
Biomed Pharmacother

Mitoquinone ameliorated airway inflammation by stabilizing β-catenin destruction complex in a steroid-insensitive asthma model. [Abstract]

2023 Jun:162:114680. PMID: 37060658
Research Square Print

September 14th, 2022.

Solvant et solubilité

In Vitro:

DMSO : 220 mg/mL (764.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4754 mL

17.3768 mL

34.7536 mL

5 mM

0.6951 mL

3.4754 mL

6.9507 mL

10 mM

0.3475 mL

1.7377 mL

3.4754 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 5.5 mg/mL (19.11 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5.5 mg/mL (19.11 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5.5 mg/mL (19.11 mM); Clear solution

This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kaneda A, et, al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4754 mL	17.3768 mL	34.7536 mL	86.8840 mL
	5 mM	0.6951 mL	3.4754 mL	6.9507 mL	17.3768 mL
	10 mM	0.3475 mL	1.7377 mL	3.4754 mL	8.6884 mL
	15 mM	0.2317 mL	1.1585 mL	2.3169 mL	5.7923 mL
	20 mM	0.1738 mL	0.8688 mL	1.7377 mL	4.3442 mL
	25 mM	0.1390 mL	0.6951 mL	1.3901 mL	3.4754 mL
	30 mM	0.1158 mL	0.5792 mL	1.1585 mL	2.8961 mL
	40 mM	0.0869 mL	0.4344 mL	0.8688 mL	2.1721 mL
	50 mM	0.0695 mL	0.3475 mL	0.6951 mL	1.7377 mL
	60 mM	0.0579 mL	0.2896 mL	0.5792 mL	1.4481 mL
	80 mM	0.0434 mL	0.2172 mL	0.4344 mL	1.0860 mL
	100 mM	0.0348 mL	0.1738 mL	0.3475 mL	0.8688 mL

Keywords

K-975

34 Cited Publications

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K-975

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) K-975

Voir tous les produits spécifiques à Isoform YAP

Activité biologique

Chemical Information

Publications (34)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

K-975

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) K-975

Voir tous les produits spécifiques à Isoform YAP

Activité biologique

Chemical Information

Publications (34)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

K-975 Related Classifications

HY-138565 Related Classifications