[CAS NO. 901245-65-6] GSK-5959
PRODUCTS SPECIFICATIONS [901245-65-6]
DESCRIPTION [901245-65-6]
Overview
| MDL | MFCD14744183 |
|---|---|
| Molecular Weight | 394.47 |
| Molecular Formula | C22H26N4O3 |
| SMILES | O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC |
Summary
IC50 & Target
IC50: 80 nM (BRPF1) [1] .
In Vitro
GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold)
[2]
.
GSK-5959 (3a) exhibits an EC
50
= 0.98 μM) in cellular NanoBRET assay
[2]
.
GSK-5959 has no effect on TRIM24 SUMOylation
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 13 mg/mL ( 32.96 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL |
References
- [1] Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195.
- [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.
- [3] Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11;293(19):7476-7485.