GSK2801 (GSK-2801)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$620	Check With Us
500mg	$999	Check With Us
1g	$1495	Check With Us

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Cat #: V0419 CAS #: 1619994-68-1 Purity ≥ 98%

Description: GSK2801 (GSK-2801) is a novel, orally bioavailable, selective, cell bioactive and acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains, which are 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.

References: Chen P, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2016 Feb 25;59(4):1410-24.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	371.45
Molecular Formula	C20H21NO4S
CAS No.	1619994-68-1
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 74 mg/mL (199.2 mM)r
	Water: <1 mg/mLr
	Ethanol: 7 mg/mL (18.8 mM)
Solubility In Vivo	0.5% CMC+1% Tween 80: 30mg/mL
SMILES Code	CC(C1=CC(C2=CC=CC=C2S(=O)(C)=O)=C3C=C(OCCC)C=CN13)=O
Synonyms	GSK-2801; GSK 2801; GSK2801

Protocol	In Vitro	GSK2801 binds TAF1L(2) with an affinity KB of 0.31μM (KD: 3.2 μM) and a binding enthalpy change ΔH of −8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity KB of 0.826 μM (KD: 1.1 μM) and ΔH of −9.8 kcal/mol.
Protocol	In Vivo	In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.6922 mL	13.4608 mL	26.9215 mL	53.8430 mL
5mM	0.5384 mL	2.6922 mL	5.3843 mL	10.7686 mL
10mM	0.2692 mL	1.3461 mL	2.6922 mL	5.3843 mL
20mM	0.1346 mL	0.6730 mL	1.3461 mL	2.6922 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.