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Submit ReviewCT-4 is a potent and selective histone deacetylase 8 (HDAC8) degrader (PROTAC®) (DC50 = 1.8 nM after 24 h, Dmax 97%). Comprises a HDAC8-binding moiety joined by a linker to pomalidomide as the ligand for cereblon (CRBN) protein. Displays 20-fold selectivity over HDAC6 (DC50 = 38 nM after 24 h, Dmax 69%) and it does not degrade other HDACs.
Displays significant effect on metastasis of MDA-MB-231 cells, and induces degradation and cell death in T-cell leukemia Jurkat cells. Outperformed HDAC8 inhibitors in oncology models. HDAC8 mediates signalling via scaffolding functions in HDAC8/p53/fusion protein complexes, also interacts with STAT3, cAMP and DEC1 via scaffolding functions.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license
| M. Wt | 699.76 |
| Formula | C37H41N5O9 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 3057302-21-0 |
| PubChem ID | 171378332 |
| InChI Key | ARLOQCPNXYNVDU-UHFFFAOYSA-N |
| Smiles | ONC(C1=CC(OCC2=CC=C(C=C2)C(NCCCCCCCCNC3=CC=CC(C(N4C5CCC(NC5=O)=O)=O)=C3C4=O)=O)=C(C=C1)OC)=O |
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.
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 69.98 | 100 |
The following data is based on the product molecular weight 699.76. 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 | 1.43 mL | 7.15 mL | 14.29 mL |
| 5 mM | 0.29 mL | 1.43 mL | 2.86 mL |
| 10 mM | 0.14 mL | 0.71 mL | 1.43 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.29 mL |
References are publications that support the biological activity of the product.
Zhao et al (2023) Discovery of highly potent HDAC8 PROTACs with anti-tumor activity. Bioorg.Chem. 136 PMID: 37098288
If you know of a relevant reference for CT-4, please let us know.
Keywords: CT-4, CT-4 supplier, potent, selective, degrader, degrades, HDAC8, histone, deacetylase, PROTAC, PROTACs, targeted, protein, degradation, TPD, cancer, research, metastasis, leukemia, oncology, Histone, Deacetylase, (HDAC), Degraders, 8024, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia