(+)-JQ1 bump, acid functionalized

Name: (+)-JQ1 bump, acid functionalized
Brand: Tocris Bioscience
SKU: 7689

Tocris Bioscience, part of Bio-Techne | Catalog # 7689

COA / SDS

Functionalized BET bromodomain ligand; precursor for Tag Degraders

Key Product Details

Description:	Functionalized BET bromodomain ligand; precursor for Tag Degraders
Chemical Name:	(R)-2-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)butanoic acid
Purity:	≥98% (HPLC)
Molecular Weight:	428.94

View Full Technical Details for (+)-JQ1 bump, acid functionalized

Technical Data
Citations

Biological Activity for (+)-JQ1 bump, acid functionalized

(+)-JQ1 bump, acid functionalized is a BET bromodomain binding analog of (+)-JQ1 (Cat. No. 4499) that selectively binds single point mutant form of Brd4 (Brd4^{BD2 L387A}). Functionalized with a carboxylic acid group to enable onward chemistry. The position of the carboxylic acid group represents an 'exit vector' allowing modification without interfering with compound binding ability.

Technical Data for (+)-JQ1 bump, acid functionalized

M. Wt	428.94
Formula	C₂₁H₂₁ClN₄O₂S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2421153-77-5
InChi Key	UAFUXHFSKWIFOW-QAPCUYQASA-N
Smiles	CC1=C(C)C(C(C2=CC=C(C=C2)Cl)=N[C@@H]([C@H](C(O)=O)CC)C3=NN=C(C)N43)=C4S1

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 (+)-JQ1 bump, acid functionalized

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	42.89	100

Preparing Stock Solutions for (+)-JQ1 bump, acid functionalized

The following data is based on the product molecular weight 428.94.

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	2.33 mL	11.66 mL	23.31 mL
5 mM	0.47 mL	2.33 mL	4.66 mL
10 mM	0.23 mL	1.17 mL	2.33 mL
50 mM	0.05 mL	0.23 mL	0.47 mL

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References for (+)-JQ1 bump, acid functionalized

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

Bond Development of BromoTag: a 'Bump-and-Hole'-PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins. J.Med.Chem 2021 PMID: 34652918