A PCAF/GCN5 bromodomain inhibitor
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GSK4027

Item No. 23421

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-3(2H)-pyridazinone
CAS Number
2079896-25-4
Molecular Formula
C17H21BrN4O
Formula Weight
377.3
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
228, 292 nm
SMILES
CN1C[C@@H](C2=CC=CC=C2)C[C@@H](NC(C=NN3C)=C(Br)C3=O)C1
InChi Code
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
InChi Key
VZAFGXCWAWRULT-UONOGXRCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $154

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    10 mg

    $283

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    Product Description

    GSK4027 is a p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain inhibitor (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).1 It is greater than 18,000-fold selective for PCAF and GCN5 over BET family bromodomains and greater than 70-fold selective over other bromodomain families in a BROMOscan assay. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Humphreys, P.G., Bamborough, P., Chung, C.W., et al. Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probe. J. Med. Chem. 60(2), 695-709 (2017).