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Tocris/(+)-JQ1/4499/10/10 mg

价格: ¥3828.00 市场价: 6380.00

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货号: 4499/10

品牌: Tocris

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Description: Potent, selective BET bromodomain inhibitor; cell permeable

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 1,1-dimethylethyl ester

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, high affinity, selective BET bromodomain inhibitor (IC₅₀ values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; K_d values are 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively). Induces squamous differentiation in NUT midline carcinoma (NMC) cell lines; inhibits tumor growth in NMC xenograft models in vivo. Exhibits reversible contraceptive effects in germ cells from male mice. Inactive analog (-)-JQ1 available.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the (+)-JQ1 probe summary on the SGC website.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of (+)-JQ1 is reviewed on the chemical probes website.

Compound Libraries

(+)-JQ1 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	456.99
Formula	C₂₃H₂₅ClN₄O₂S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1268524-70-4
PubChem ID	46907787
InChI Key	DNVXATUJJDPFDM-KRWDZBQOSA-N
Smiles	O=C(OC(C)(C)C)C[C@@H]1N=C(C4=CC=C(Cl)C=C4)C3=C(SC(C)=C3C)N2C1=NN=C2C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	45.7	100
	ethanol	45.7	100

Preparing Stock Solutions

The following data is based on the product molecular weight 456.99. 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	2.19 mL	10.94 mL	21.88 mL
5 mM	0.44 mL	2.19 mL	4.38 mL
10 mM	0.22 mL	1.09 mL	2.19 mL
50 mM	0.04 mL	0.22 mL	0.44 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Filippakopoulos et al (2010) Selective inhibition of BET bromodomains. Nature 468 1067 PMID: 20871596

Herrmann et al (2012) Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML. Oncotarget. [Epub ahead of print] 3 1588 PMID: 23249862

Matzuk et al (2012) Small-molecule inhibition of BRDT for male contraception. Cell 150 673 PMID: 22901802

Keywords: (+)-JQ1, supplier, BET, bromodomains, inhibitors, inhibits, potent, selective, high, affinity, NUT, midline, carcinomas, antitumor, male, contraceptive, BRD2, BRD3, BRD4, BRDT, sgc, Bromodomains, Bromodomains, Tocris Bioscience

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