CT-4

Key Product Details

Product Description

CT-4 is a potent and selective histone deacetylase 8 (HDAC8) degrader (PROTAC^®) (DC₅₀ = 1.8 nM after 24 h, D_max 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, D_max 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

Product Specifications for CT-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for CT-4

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Zhao Discovery of highly potent HDAC8 PROTACs with anti-tumor activity. Bioorg.Chem. 2023 PMID: 37098288

Product Documents for CT-4