HHP 9

Name: HHP 9
Brand: Tocris Bioscience
SKU: 7828

Tocris Bioscience, part of Bio-Techne | Catalog # 7828

COA / SDS

BET bromodomain Degrader (PROTAC®); also potent Hedgehog pathway inhibitor

Key Product Details

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)
Molecular Weight:	900.99

View Full Technical Details for HHP 9

Technical Data
Citations

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 for HHP 9

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

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.11 mL	5.55 mL	11.10 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 Targeted protein degradation reveals BET bromodomains as the cellular target of Hedgehog pathway inhibitor-1. Nat.Commun. 2023 PMID: 37393376