GSK-340( GSK340 | GSK 340 )

Catalog No. M13548 CAS No. 2222509-79-5

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK-340
Note

Research use only, not for human use.
Brief Description

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2).
Description

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2) with pKd of 8.18, 7.49, 7.72 and 7.68 for BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2, respectively; displays 229-, 40-, 48- and 91-fold selectivity over the responding BD1, >100-fold selectivity over TAF1, WRD9, ATAD2A/B and other bromodomains (pKd<5.0); inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2 with pIC50 of 7.2, 6.5, 7.3 and 6.7, respectively; inhibits release of the MCP-1 cytokine in human PBMCs (pIC50=7.4) and whole blood; GSK-340 is an useful in vitro tool molecule for investigation into the biological role of the BD2 domains.
In Vitro

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In Vivo

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Synonyms

GSK340 | GSK 340
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

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Indication

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CAS Number

2222509-79-5
Formula Weight

417.553
Molecular Formula

C26H31N3O2
Purity

>98% (HPLC)
Solubility

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SMILES

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Chemical Name

(S)-1-(2-cyclopropyl-4-(2-(hydroxymethyl)benzyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-3,4-dihydroquinoxalin-1(2H)-yl)ethan-1-one

1. Law RP, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.7b01666.

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