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.
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Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM.
HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs.
HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines.
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