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JPS036

Cat. No. 8085 Submit a Review Datasheet / COA / SDS
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Description: Selective HDAC3 Degrader (PROTAC®)
Chemical Name: (2S,4R)-N-[2-[[12-[[4-[(2-Aminophenyl)carbamoyl]phenyl]amino]-12-oxododecyl]oxy]-4-(4-methylthiazol-5-yl)benzyl]-1-[(S)-2-(1-fluorocyclopropan-1-ylcarbonylamino)-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for JPS036

JPS036 is a selective HDAC3 Degrader (PROTAC®) (DC50 = 440 nM; Dmax = 77 %). JPS036 comprises a benzamide-based compound joined by a linker to a Von Hippel Lindau (VHL) E3 ligase ligand.

Negative control JPS016NC also available.

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

Licensing Information

Sold under license from the University of Leicester

Technical Data for JPS036

M. Wt 940.19
Formula C51H66FN7O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2669785-85-5
PubChem ID 156808378
InChI Key NAADBQUVFJWCFU-XVYMMXEDSA-N
Smiles O=C(C1(CC1)F)N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=C(C=C(C4=C(N=CS4)C)C=C3)OCCCCCCCCCCCC(NC5=CC=C(C=C5)C(NC6=C(C=CC=C6)N)=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 JPS036

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.8 20 with gentle warming

Preparing Stock Solutions for JPS036

The following data is based on the product molecular weight 940.19. 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
0.2 mM 5.32 mL 26.59 mL 53.18 mL
1 mM 1.06 mL 5.32 mL 10.64 mL
2 mM 0.53 mL 2.66 mL 5.32 mL
10 mM 0.11 mL 0.53 mL 1.06 mL

Molarity Calculator

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Reconstitution Calculator

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References for JPS036

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

Smalley et al (2022) Optimization of class I histone 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 JPS036, please let us know.

View Related Products by Target

Keywords: JPS036, JPS036 supplier, JPS036, HDAC3, protac, degrader, degraders, degrades, selective, VHL, von, hippel, lindau, Protein, Degraders, PROTACs, proteolysis, targeting, chimera, active, Class, I, HDACs, Histone, Deacetylase, (HDAC), 8085, Tocris Bioscience

Citations for JPS036

Citations are publications that use Tocris products.

Currently there are no citations for JPS036. Do you know of a great paper that uses JPS036 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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
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