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Submit ReviewTM2 TEAD inhibitor
Description: Potent and reversible inhibitor of TEAD mediated Hippo/Yap signalling
Chemical Name: 4-[3-(2-Cyclohexylethoxy)benzoyl]-N-phenyl-1-piperazinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for TM2 TEAD inhibitor
TM2 TEAD inhibitor is a potent and reversible TEA domain transcription factor inhibitor (IC50 = 38 nM and 156 nM for TEAD4 auto-palmitoylation and TEAD2 palmitoylation, respectively). It inhibits TEAD-YAP association and transcriptional activity. TM2 TEAD inhibitor exhibits strong antiproliferation effects as a single agent or in combination with a MEK inhibitor in YAP-dependent cancer cells. Also inhibits YAP-dependent liver organoid growth ex vivo.
Technical Data for TM2 TEAD inhibitor
| M. Wt | 435.57 |
| Formula | C26H33N3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1008768-41-9 |
| PubChem ID | 68301145 |
| InChI Key | LWLAYULJAJMPKG-UHFFFAOYSA-N |
| Smiles | O=C(N1CCN(CC1)C(C2=CC(OCCC3CCCCC3)=CC=C2)=O)NC4=CC=CC=C4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TM2 TEAD inhibitor
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.56 | 100 | |
| ethanol | 43.56 | 100 |
Preparing Stock Solutions for TM2 TEAD inhibitor
The following data is based on the product molecular weight 435.57. 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 | 2.3 mL | 11.48 mL | 22.96 mL |
| 5 mM | 0.46 mL | 2.3 mL | 4.59 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for TM2 TEAD inhibitor
References for TM2 TEAD inhibitor
References are publications that support the biological activity of the product.
Hu et al (2022) Discovery of a new class of reversible TEA domain transcription factor inhibitors with a novel binding mode. eLife 11 e80210 PMID: 36398861
If you know of a relevant reference for TM2 TEAD inhibitor, please let us know.
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Citations for TM2 TEAD inhibitor
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.
Pathways for TM2 TEAD inhibitor
MAPK Signaling Pathway
The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.
Notch Signaling Pathway
The Notch pathway is involved in determination of cell fate, regulation of pattern formation and other developmental settings. Disrupted signaling can cause developmental defects and a range of adult pathologies.