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HHP 9

Cat. No. 7828 Submit a Review Datasheet / COA / SDS
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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)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

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)
InChI Key RJNFQVDPIFXYAO-UHFFFAOYSA-N
Smiles CC1=C(C(OCCOC)=O)C(C2=CC(OCC3=CN(CCCCCCOC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)N=N3)=CC=C2)C7=C(N1)CC(C8=C(OC)C=CC=C8)CC7=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 HHP 9

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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.

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

Citations for HHP 9

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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

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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