BRD73954 does not only retained HDAC6 inhibitory activity (IC50 = 0.036 μM) but resulted in a 10-fold increase in potency for HDAC8 (IC50 = 0.12 μM) with a concomitant reduction in potency for HDAC2.
In vitro: While treatment BRD73954 with resulted in a robust increase in α-tubulin acetylation, no change in the acetylation state of H3 was observed, which is consistent with the ability of these compounds to inhibit HDAC6 but not HDACs 1, 2, or 3 in the biochemical assay in HeLa cells.
|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 30 mg/mL|
Discovery of the first histone deacetylase 6/8 dual inhibitors.
Olson DE, et al. J Med Chem. 2013 Jun 13;56(11):4816-20. PMID: 23672185.
|Related HDAC Products|
Valproic acid is an HDAC inhibitor with IC50 in the range of 0.5~2 mM.
Chidamide is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.