(-)-JQ1

Catalog #

27334

$190 *

Size: 5 mg

Qty

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Description

(-)-JQ1 is the inactive stereoisomer of the potent, cell-permeable, small molecule bromodomain inhibitor (+)-JQ1 that competitively binds to acetyl-lysine recognition motifs. (+)-JQ1 competitively binds to the bromodomain displacing the BRD4 fusion oncoprotein from chromatin, which induces squamous differentiation and specific anti-proliferative effect in BRD4-dependent cell lines and patient-derived xenograft models. However, study results have shown that (-)-JQ1 fails to significantly interact with any bromodomain tested and exhibits inhibition against BRD4(1) with and IC₅₀ of 10,000 nM.

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Synonyms

(R)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate

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Product Data Gallery

Product Info

Storage and Usage

Citations

Purity

≥98%

Format

Yellowish, white crystalline powder

Formula

C₂₃H₂₅ClN₄O₂S

456.99

Solubility

Soluble in DMSO or ethanol at 100 mM

Biological Activity

(-)-JQ1 showed no inhibition of BRD4-dependent NMC cells.

CAS Registry #

1268524-71-5

Background

References

Filippakopoulos, P., et al. Nature. 2010 Dec 23;468(7327):1067-73.

Application Reference:
1. BET bromodomain inhibitors block growth of pancreatic cancer cells in three-dimensional collagen (2014)
2. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (2014)

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(-)-JQ1

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