GSK 2801

CAS NO.：1619994-68-1
Empirical Formula: C20H21NO4S
Molecular Weight: 371.45
MDL number: MFCD26142953
Update Date: 2024-11-17 08:48:38

What is GSK 2801?

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.

The Uses of GSK 2801

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.

Properties of GSK 2801

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 for GSK 2801

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral
Precautionary Statement Codes	P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.