| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
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. GSK2801 inhibits BAZ2A and BAZ2B with Kd of 257 nM and 136 nM, respectively. It has the potential to be used as a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.
| ln 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 tests employing the bromodomain of BRD9 results in the measurement of an affinity KB of 0.826 μM (KD: 1.1 μM) and ΔH of −9.8 kcal/mol[1]. GSK2801 or RNAi suppression of BAZ2A/B with JQ1 selectively displaced BRD2 to promoters/enhancers of ETS-regulated genes. In 2D cells, enhanced displacement of BRD2 from chromatin by combined pharmacological therapy triggered senescence. In spheroid cultures, combined therapy produces cleaved caspase-3 and cleavage PARP typical of apoptosis in tumor cells. Thus, GSK2801 suppresses BRD2-driven transcription in conjunction with BET inhibitor and promotes apoptosis of TNBC[2] .
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| ln Vivo |
After oral and intraperitoneal dosing to male CD1 mice, the pharmacokinetic characteristics are assessed to assess the appropriateness of GSK2801 for in vivo investigations. Following oral dosage, GSK2801 exhibits a decent in vivo exposure, mild clearance, and reasonable plasma stability[1].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C20H21NO4S
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| Molecular Weight |
371.45
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| Exact Mass |
371.119
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| CAS # |
1619994-68-1
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| Related CAS # |
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| PubChem CID |
73010930
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| Appearance |
Light yellow to khaki solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.596
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| LogP |
2.95
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
599
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KHWCPNJRJCNVRI-UHFFFAOYSA-N
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| 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
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| Chemical Name |
1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone
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| Synonyms |
GSK-2801; GSK 2801; GSK2801
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.73 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (6.73 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC+1% Tween 80: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6922 mL | 13.4608 mL | 26.9215 mL | |
| 5 mM | 0.5384 mL | 2.6922 mL | 5.3843 mL | |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6922 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
Chemoproteomic profiling of BAZ inhibitor selectivity to endogenous bromodomain proteins. J Med Chem. 2016 Feb 25; 59(4): 1410–1424. |
BAZ2A fluorescence recovery after photobleaching assay. J Med Chem. 2016 Feb 25; 59(4): 1410–1424. |
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