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JPS016

Cat. No. 8083 Submit a Review Datasheet / COA / SDS
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Description: Selective class I HDAC Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-2-(2-((9-(2-((4-((2-Aminophenyl)carbamoyl)phenyl)amino)-2-oxoethoxy)nonyl)oxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for JPS016

JSP016 is a selective Degrader (PROTAC®) and inhibitor of class I HDACs (DC50 values are 530 nM and 550 nM for HDAC3 and HDAC1; Dmax 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.

Licensing Information

Sold under license from the University of Leicester

Technical Data for JPS016

M. Wt 898.13
Formula C48H63N7O8S
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 2669785-77-5
PubChem ID 163322304
InChI Key BOXZMOCGSKLDAH-OUZJXKGJSA-N
Smiles NC(C=CC=C1)=C1NC(C(C=C2)=CC=C2NC(COCCCCCCCCCOCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)=O)=O)=O)=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.

Solubility Data for JPS016

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.98 10

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for JPS016

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

Smalley et al (2022) 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. 65 5642 PMID: 35293758

If you know of a relevant reference for JPS016, please let us know.

View Related Products by Target

Keywords: JPS016, JPS016 supplier, PROTAC, proteolysis, targeting, chimera, chimeras, PROTACs, degrader, degraders, histone, deacetylase, HDAC, HDAC1, HDAC2, HDAC3, vhl, von, hippel, lindau, E3, ligase, Histone, Deacetylase, (HDAC), Degraders, Class, I, HDACs, 8083, Tocris Bioscience

Citations for JPS016

Citations are publications that use Tocris products.

Currently there are no citations for JPS016. Do you know of a great paper that uses JPS016 from Tocris? Please let us know.

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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!

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Epigenetics in Cancer Research Product Guide

Epigenetics in Cancer Research Product Guide

This product guide reviews some of the main areas in cancer epigenetics research and lists around 120 products that can be used for the main epigenetic targets including:

  • Histone Methylation
  • Histone Acetylation
  • DNA Methylation
  • Ubiquitination
  • Bromodomains
TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
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Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

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