GSK4027

Size	Price	Stock	Quantity
--	$--	In stock

Size

Price

Stock

Quantity

$--

In stock

Purity

≥95%

Appearance

Crystalline Solid

IUPACName

4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenylpiperidin-3-yl]amino]pyridazin-3-one

Synonyms

4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-3(2H)-pyridazinone

InChI Key

VZAFGXCWAWRULT-UONOGXRCSA-N

InChI

InChI=1S/C17H21BrN4O/c1-21-10-13(12-6-4-3-5-7-12)8-14(11-21)20-15-9-19-22(2)17(23)16(15)18/h3-7,9,13-14,20H,8,10-11H2,1-2H3/t13-,14+/m0/s1

Canonical SMILES

CN1CC(CC(C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3

1. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe

Jameed Hussain, Jessica F Renaux, Anne-Marie Michon, Thomas G Hayhow, Peter D Craggs, David F Tough, Philip G Humphreys, Laurie Gordon, Katherine L Jones, Matthew Lindon, Rab K Prinjha, Chun-Wa Chung, Colin J Suckling, Paola Grandi, Paul Bamborough J Med Chem . 2017 Jan 26;60(2):695-709. doi: 10.1021/acs.jmedchem.6b01566.

p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. However, outside of viral replication, little is known about the dependence of these effects on the C-terminal bromodomain. Herein, we report GSK4027 as a chemical probe for the PCAF/GCN5 bromodomain, together with GSK4028 as an enantiomeric negative control. The probe was optimized from a weakly potent, nonselective pyridazinone hit to deliver high potency for the PCAF/GCN5 bromodomain, high solubility, cellular target engagement, and ≥18000-fold selectivity over the BET family, together with ≥70-fold selectivity over the wider bromodomain families.

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	2.6506 mL	13.2528 mL	26.5055 mL
5 mM	0.5301 mL	2.6506 mL	5.3011 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 mL

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂