ZXH 3-26

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Cat.No. 6713 - ZXH 3-26 | C38H37ClN8O7S | CAS No. 2243076-67-5
Description: Potent and selective BRD4 degrader
Chemical Name: Methyl (6S)-4-(4-chlorophenyl)-2-[[[5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]pentyl]amino]carbonyl]-3,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective BRD4 degrader (DC50 ~ 5 nM). Exhibits no significant degradation of BRD2 and BRD3. Whole proteome mass spectometry shows significant downregulation of BRD4 only. Active intracellularly.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M. Wt 785.27
Formula C38H37ClN8O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2243076-67-5
PubChem ID 132427808
InChI Key OTKOFICOCDRNDA-PMCHYTPCSA-N
Smiles COC(C[C@@H]1N=C(C2=CC=C(C=C2)Cl)C3=C(N4C(C)=NN=C14)SC(C(NCCCCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=C3C)=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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 78.53 100

Preparing Stock Solutions

The following data is based on the product molecular weight 785.27. 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
1 mM 1.27 mL 6.37 mL 12.73 mL
5 mM 0.25 mL 1.27 mL 2.55 mL
10 mM 0.13 mL 0.64 mL 1.27 mL
50 mM 0.03 mL 0.13 mL 0.25 mL

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References

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

Nowak et al (2018) Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat.Chem.Biol. 14 706 PMID: 29892083


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Citations for ZXH 3-26

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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* or download your copy today!

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
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  • Angiogenesis
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Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

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Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation

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.