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GSK2801

Item № 14120
CAS № 1619994-68-1
Purity ≥98%
product image
                (CAS 1619994-68-1)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $25.00 0.00
     5 mg $88.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description

BAZ2A/B are bromodomain-containing proteins whose biological function is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.1,2 BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen).3,4 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 ATAD2.3,4 See the Structural Genomics Consortium (SGC) website for more information.

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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
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

Download SGC Epigenetic Chemical Probe Guide

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Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data pack, and GC-MS data.

References & Product Citations
Product Description References

1. Clapier, C.R., and Cairns, B.R. The biology of chromatin remodeling complexes Annual Reviews of Biochemistry 78, 273-304 (2009).

2. He, X., Fan, H.Y., Garlick, J.D., et al. Diverse regulation of SNF2h chromatin remodeling by noncatalytic subunits Biochemistry 47, 7025-7033 (2008).

3. Chen, P., Chaikuad, A., Bamborough, P., et al. Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B Journal of Medicinal Chemistry (2015).

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

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