UNC 6852

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Description: Polycomb repressive complex 2 (PRC2) Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-2-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)benzamido)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for UNC 6852

UNC 6852 is a polycomb repressive complex 2 (PRC2) Degrader (PROTAC®; DC50 = 0.79 μM). It comprises an EED (embryonic ectoderm development) based ligand, joined by a linker to a von Hippel-Lindau ligand. In B lymphoblast cell lines, UNC 6852 selectively degrades PRC2 components EED (DC50 = 0.31 μM, Dmax = 94%), enhancer of zeste homolog 2 (EZH2, DC50 = 0.67 μM, Dmax = 96%), and suppressor of zeste homolog 12 (SUZ12, DC50 = 0.59 μM, Dmax = 82%). In zebrafish, UNC 6852 treatment increases transcription of tfpia and prolongs time to occlusion (TTO) in the caudal vein following laser injury.

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

Technical Data for UNC 6852

M. Wt 832.98
Formula C43H48N10O6S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2688842-08-0
PubChem ID 146014466
InChI Key PPNNFXIBKLCMTI-WXEAQWFJSA-N
Smiles O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)[C@H](C(C)(C)C)NC(CCCNC(C(C=C4)=CC=C4C5=CN=C(N6C5=NN=C6)NCC7=CC=CO7)=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 UNC 6852

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 83.3 100

Preparing Stock Solutions for UNC 6852

The following data is based on the product molecular weight 832.98. 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
1 mM 1.2 mL 6 mL 12.01 mL
5 mM 0.24 mL 1.2 mL 2.4 mL
10 mM 0.12 mL 0.6 mL 1.2 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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References for UNC 6852

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

Potjewyd et al (2020) Degradation of polycomb repressive complex 2 with an EED-targeted bivalent chemical degrader. Cell Chem.Biol. 27 47 PMID: 31831267

Raman et al (2021) Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target. Sci.Rep. 11 15238 PMID: 34315984


If you know of a relevant reference for UNC 6852, please let us know.

Keywords: UNC 6852, UNC 6852 supplier, UNC6852, polycomb, repressive, complex, 2, PRC2, degraders, degrades, PROTAC, tissue, factor, pathway, tfpia, EZH2, EED, SUZ12, Polycomb, Repressive, Complex, (PRC), Degraders, 7816, Tocris Bioscience

Citations for UNC 6852

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
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