GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
| Molecular Weight | 394.47 |
| Formula | C22H26N4O3 |
| CAS Number | 901245-65-6 |
| Solubility (25°C) | DMSO 6 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Goutham Atla, et al. Genome Biol. Genetic regulation of RNA splicing in human pancreatic islets
| Related Epigenetic Reader Domain Products |
|---|
| Phoenixin-20
Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. |
| Menin-MLL inhibitor 31
Menin-MLL inhibitor 31 is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM. |
| OPN-2853
OPN-2853 is a bromodomain protein-4 (BRD4) inhibitor that can be used in studies related to hematologic and lymphatic disorders. |
| HDAC/JAK/BRD4-IN-1
HDAC/JAK/BRD4-IN-1 is a potent HDAC/JAK/BRD4 triple inhibitor. |
| VYN-201
VYN-201 is a novel pan-BET inhibitor for studies related to idiopathic pulmonary fibrosis. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
