PFI-4 is cell permeable, and acts by displacing the BRPF1 bromodomain from Histone H3.3.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 17 mg/mL warmed|
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Demont EH,et.al. ACS Med Chem Lett. 2014 Sep 10;1190-5. PMID: 25408830.
|Related Epigenetic Reader Domain Products|
|AZD-5153 HNT salt
AZD-5153 HNT salt is a potent, selective and orally available BET/BRD4 bromodomain inhibitor, disrupts BRD4 with an IC50 of 1.7 nM.
BI-7273 is a potent and selective BRD9 inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7, respectively.
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
|JQ-1 carboxylic acid
(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.
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