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MC 1

Cat. No. 8843 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Selective EP300 Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-2-(8-(2-(4-(6-((R)-2-(((S)-2-(4-Cyanophenyl)propyl)amino)-2-phenylacetamido)pyridin-3-yl)-1H-pyrazol-1-yl)acetamido)octanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MC 1

MC 1 is a selective degrader of the lysine acetyltransferase EP300. Displays selectivity for EP300 over CREBBP. Comprises an EP300-binding moiety (CPI-1612) joined by a linker to VH032 as the ligand for von Hippel-Lindau E3 ubiquitin ligase. MC 1 inhibits cell proliferation in a subset of cancer cell lines and provides a new tool to investigate the noncatalytic functions of EP300 and CREBBP.

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

Technical Data for MC 1

M. Wt 1062.35
Formula C59H71N11O6S
Storage Store at -20°C
Purity ≥95% (HPLC)
InChI Key NKGYKZVOVOJLDL-HITCUEKTSA-N
Smiles O=C(CCCCCCCNC(CN1N=CC(C2=CC=C(NC([C@H](NC[C@@H](C)C3=CC=C(C#N)C=C3)C4=CC=CC=C4)=O)N=C2)=C1)=O)N[C@H](C(N5[C@H](C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)C[C@@H](O)C5)=O)C(C)(C)C

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 MC 1

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.62 10 with gentle warming

Preparing Stock Solutions for MC 1

The following data is based on the product molecular weight 1062.35. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 9.41 mL 47.07 mL 94.13 mL
0.5 mM 1.88 mL 9.41 mL 18.83 mL
1 mM 0.94 mL 4.71 mL 9.41 mL
5 mM 0.19 mL 0.94 mL 1.88 mL

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Product Datasheets for MC 1

Certificate of Analysis is currently unavailable on-line.
Please contact Customer Service
Safety Datasheet

References for MC 1

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

Chen et al (2024) Paralogue-selective degradation of the lysine acetyltransferase EP300. JACS Au. 29 3094 PMID: 39211607

If you know of a relevant reference for MC 1, please let us know.

View Related Products by Target

Keywords: MC 1, MC 1 supplier, MC1, selective, degrader, EP300, over, CREBBP, lysine, acetyltransferase, degradation, CPI-1612, warhead, VHL, PROTAC, PROTACs, targeted, protein, TPD, cancer, research, oncology, CBP, and, p300, Degraders, 8843, Tocris Bioscience

Citations for MC 1

Citations are publications that use Tocris products.

Currently there are no citations for MC 1. Do you know of a great paper that uses MC 1 from Tocris? Please let us know.

Reviews for MC 1

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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.

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