A probe for BAZ2A/B bromodomains
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GSK2801

Item No. 14120

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
1-[1-[2-(methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]-ethanone
CAS Number
1619994-68-1
Molecular Formula
C20H21NO4S
Formula Weight
371.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
λmax
210, 257, 372 nm
SMILES
CCCOC1=CC2=C(C3=C(S(C)(=O)=O)C=CC=C3)C=C(C(C)=O)N2C=C1
InChi Code
InChI=1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3,23)24/h5-10,12-13H,4,11H2,1-3H3
InChi Key
KHWCPNJRJCNVRI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    Product Description

    GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen).1,2 It binds to BAZ2A and BAZ2B with Kd values of 0.26 and 0.14 µM, respectively, and does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2.1,2 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. Chen, P., Chaikuad, A., Bamborough, P., et al. Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B. J. Med. Chem. 59(4), 1410-1424 (2015).

    2. Gallenkamp, D., Gelato, K.A., Haendler, B., et al. Bromodomains and their pharmacological inhibitors. Chem. Med. Chem. 9(3), 438-464 (2014).