JPS016

Key Product Details

Product Description

JSP016 is a selective Degrader (PROTAC^®) and inhibitor of class I HDACs (DC₅₀ values are 530 nM and 550 nM for HDAC3 and HDAC1; D_max is 77%, 66% and 45% at HDAC1, 3 and 2; IC₅₀ values are 380 nM, 570 nM and 820 nM at HDAC3, 1 and 2). Comprises a benzamide-based compound joined by a linker to a Von Hippel Lindau (VHL) E3 ligase ligand. JPS016 treatment up- or down-regulates nearly 4000 differentially expressed genes, arrests cells at sub-G₁ phase and promotes apoptosis in HCT116 cells.

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from the University of Leicester

Product Specifications for JPS016

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

Solubility

Preparing Stock Solutions for JPS016

The following data is based on the product molecular weight 898.13.

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
0.1 mM	11.13 mL	55.67 mL	111.34 mL
0.5 mM	2.23 mL	11.13 mL	22.27 mL
1 mM	1.11 mL	5.57 mL	11.13 mL
5 mM	0.22 mL	1.11 mL	2.23 mL

Calculators

Background References

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

• Smalley Optimization of class I hstone deacetylase PROTACs reveals that HDAC1/2 degradation is critical to induce apoptosis and cell arrest in cancer cells. J.Med.Chem. 2022 PMID: 35293758

Product Documents for JPS016