GSK 2801 Chemical Properties

Density 

1.23±0.1 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥2.82 mg/mL in EtOH with gentle warming and ultrasonic

form 

solid

color 

Light yellow to khaki

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

GSK 2801 Usage And Synthesis

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. 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). It binds to BAZ2A and BAZ2B with K_d 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. See the Structural Genomics Consortium (SGC) website for more information.

Uses

GSK2801 is a selective cell-permeable inhibitor of the BAZ2 (bromodomain-containing protein) interfering with nucleosome spacing during chromatin assembly.

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. journal of medicinal chemistry, 2015.

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