GSK2801

inhibitor of BAZ2A and BAZ2B bromodomains CAS# 1619994-68-1

GSK2801

Catalog No. BCC6498----Order now to get a substantial discount!

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Quality Control of GSK2801

Number of papers citing our products

Chemical structure

GSK2801

3D structure

Chemical Properties of GSK2801

Cas No. 1619994-68-1 SDF Download SDF
PubChem ID 73010930 Appearance Powder
Formula C20H21NO4S M.Wt 371.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (134.61 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 1-[1-(2-methylsulfonylphenyl)-7-propoxyindolizin-3-yl]ethanone
SMILES CCCOC1=CC2=C(C=C(N2C=C1)C(=O)C)C3=CC=CC=C3S(=O)(=O)C
Standard InChIKey KHWCPNJRJCNVRI-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GSK2801

DescriptionSelective BAZ2A and BAZ2B inhibitor (IC50 values are 0.40 and 0.43 μM, respectively). Selective for BAZ2A/B over TAF1L and BRD9. Cell permeable and orally available.

GSK2801 Dilution Calculator

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GSK2801 Molarity Calculator

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Preparing Stock Solutions of GSK2801

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6922 mL 13.4608 mL 26.9215 mL 53.843 mL 67.3038 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL 10.7686 mL 13.4608 mL
10 mM 0.2692 mL 1.3461 mL 2.6922 mL 5.3843 mL 6.7304 mL
50 mM 0.0538 mL 0.2692 mL 0.5384 mL 1.0769 mL 1.3461 mL
100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.5384 mL 0.673 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GSK2801

GSK2801, as an inhibitor of BAZ2A and BAZ2B bromodomains, is potent, selective and cell active acetyl-lysine competitive, with dissociation constants (KD) of 136 and 257 nM for binding to BAZ2B and BAZ2A, respectively [1].

Bromodomains, as protein interaction domains, are acetyl-lysine specific. Bromodomain containing proteins BAZ2A and BAZ2B are closely related. The nucleolar remodeling complex (NoRC) regulates the expression of noncoding RNAs. BAZ2A and BAZ2B constitute the central scaffolding protein of NoRC [1].

In U2OS cells, treatment with the SAHA induced hyperacetylated chromatin. In a GFP-BAZ2A fusion construct, the conserved asparagines that are essential for recognizing the acetylated lysine has been mutated. When a GFP-BAZ2A fusion construct was transfected into SAHA-treated U2OS cells, the mutant construct accelerated FRAP half-recovery time. Treatment with GSK2801 alone in U2OS cells also accelerated FRAP half-recovery time. Both acceleration extents are the same. This meant that GSK2801 can displace BAZ2A from chromatin [1].

Pharmacokinetic parameters of GSK2801 after intraperitoneal and oral dosing to male CD1 mice were measured. Data showed that after oral dosing in vivo, GSK2801 has reasonable exposure, reasonable plasma stability and modest clearance. GSK2801 can be used as an inhibitor of BAZ2A/B bromodomain in vivo [1]. No more in vivo data of the treatment with GSK2801 are found.

Reference:
[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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References on GSK2801

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.[Pubmed:25799074]

J Med Chem. 2016 Feb 25;59(4):1410-24.

Bromodomains are acetyl-lysine specific protein interaction domains that have recently emerged as a new target class for the development of inhibitors that modulate gene transcription. The two closely related bromodomain containing proteins BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. However, BAZ2 bromodomains have low predicted druggability and so far no selective inhibitors have been published. Here we report the development of GSK2801, a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains as well as the inactive control compound GSK8573. GSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively. Crystal structures demonstrated a canonical acetyl-lysine competitive binding mode. Cellular activity was demonstrated using fluorescent recovery after photobleaching (FRAP) monitoring displacement of GFP-BAZ2A from acetylated chromatin. A pharmacokinetic study in mice showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. Thus, GSK2801 represents a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.

Description

GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.

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