(+)-JQ1 carboxylic acid

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Cat.No. 6588 - (+)-JQ1 carboxylic acid | C19H17ClN4O2S | CAS No. 202592-23-2
Chemical Name: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity

BET bromodomain inhibitor (+)-JQ1 (Cat. No. 4499) with a carboxylic acid functional group for conjugation reactions. Can be used as a precursor to PROTACs that target BET bromodomains after conjugation to a linker and E3 ligase ligand.

Technical Data

M. Wt 400.88
Formula C19H17ClN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 202592-23-2
PubChem ID 66828107
InChI Key LJOSBOOJFIRCSO-AWEZNQCLSA-N
Smiles OC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=C(SC(C)=C3C)N4C1=NN=C4C)=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 40.09 100
ethanol 40.09 100

Preparing Stock Solutions

The following data is based on the product molecular weight 400.88. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.49 mL 12.47 mL 24.95 mL
5 mM 0.5 mL 2.49 mL 4.99 mL
10 mM 0.25 mL 1.25 mL 2.49 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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References

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

Winter et al (2015) DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370

Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem Biol. 10 1770 PMID: 26035625

Gadd et al (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 13 514 PMID: 28288108


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