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(+)-JQ1 PA

Names

[ CAS No. ]:
2115701-93-2

[ Name ]:
(+)-JQ1 PA

Biological Activity

[Description]:

(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
Research Areas >> Cancer

[Target]

10.4 nM (BET)[1].


[In Vitro]

(+)-JQ1 PA is a derivative of JQ1, which is the inhibitor of BET. The IC50 of (+)-JQ1 PA for BET is 10.4 nM, and the IC50 of JQ1 is 14.3 nM in MV4;11 cells[1].

[Cell Assay]

Proliferation of MV4;11 cells after 72 hours of treatment, comparing JQ1 versus JQ1-PA are tested. Cell cycle profile of MV4;11 cells after 48 hours of treatment with DMSO, JQ1, JQ1-PA, or JQ1-TCO (all compounds used at 500 nM) are tested[1].

[References]

[1]. Tyler DS, et al. Click chemistry enables preclinical evaluation of targeted epigenetic therapies. Science. 2017 Jun 30;356(6345):1397-1401.


[Related Small Molecules]

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15

Chemical & Physical Properties

[ Molecular Formula ]:
C22H20ClN5OS

[ Molecular Weight ]:
437.95


Related Compounds