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Description: BET bromodomain Degrader (PROTAC®); also potent Hedgehog pathway inhibitor
Chemical Name: 2-Methoxyethyl 4-(3-((1-(6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)hexyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-7-(2-methoxyphenyl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
Purity: ≥98% (HPLC)
Literature (4)

Biological Activity for HHP 9

HHP 9 is a potent BET bromodomain Degrader (PROTAC®; DC50 values are 0.03 μM, 0.2 μM and 0.2 μM at BRD3, BRD2 and BRD4 respectively). BRD2, BRD3 and BRD4 are almost completely degraded by HHP 9 in vitro (after 27h incubation with 0.5 - 5 μM of HHP 9). Comprises a Hedgehog Pathway Inhibitor-1 (HPI-1, Cat. No. 3839) coupled to a CRBN ligand. BET bromodomain degradation through HPP-9 results in long-acting Hh pathway inhibition.

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

Technical Data for HHP 9

M. Wt 900.99
Formula C49H52N6O11
Storage Store at -20°C
Purity ≥98% (HPLC)

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 HHP 9

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 90.1 100

Preparing Stock Solutions for HHP 9

The following data is based on the product molecular weight 900.99. 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 1.11 mL 5.55 mL 11.1 mL
5 mM 0.22 mL 1.11 mL 2.22 mL
10 mM 0.11 mL 0.55 mL 1.11 mL
50 mM 0.02 mL 0.11 mL 0.22 mL

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References for HHP 9

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

Bagka et al (2023) Targeted protein degradation reveals BET bromodomains as the cellular target of Hedgehog pathway inhibitor-1. Nat.Commun. 14 3893 PMID: 37393376

If you know of a relevant reference for HHP 9, please let us know.

Keywords: HHP 9, HHP 9 supplier, HHP9, PROTACs, Degraders, degrades, potent, BET, bromodomains, BRD2, BRD3, BRD4, HPI-1, Hedgehog, Pathway, Inhibitor-1, CRBN, Protein, Signaling, Bromodomains, 7828, Tocris Bioscience

Citations for HHP 9

Citations are publications that use Tocris products.

Currently there are no citations for HHP 9. Do you know of a great paper that uses HHP 9 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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Targeted Protein Degradation Research Product Guide

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Epigenetics Scientific Review

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 Poster

Epigenetics in Cancer Poster

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 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