| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H26N4O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK-5959 is a potent, selective, and cell-permeable BRPF1 bromodomain inhibitor with an IC50 of approximately 80 nM[1]. It is supplied as a light yellow to yellow solid (C22H26N4O3, MW 394.47) at 99.73% purity.
Physical & Chemical Properties
| CAS Number | 901245-65-6 |
|---|---|
| Molecular Formula | C22H26N4O3 |
| Molecular Weight | 394.47 g/mol |
| Purity | 99.73% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC |
| Signaling Pathway | Epigenetics |
| Solubility | In Vitro: DMSO: 13 mg/mL (32.96 mM; Requires sonication and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 80 nM (BRPF1)[1].
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Wylie S.Palmer, et al. Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains Discovery Today: Technologies Volume 19, March 2016, Pages 65-71.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 13 mg/mL (32.96 mM) | requires sonication and warming; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
GSK-5959 (3a) is also selective over the closely related family members BRPF2 (100-fold) and BRPF3 (>1000-fold)[2]. In a cellular NanoBRET assay, GSK-5959 (3a) has an EC50 = 0.98 μM[2]. GSK-5959 does not affect TRIM24 SUMOylation[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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