ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM. ACY-738 has a selectivity of 60- to 1500-fold over class I HDACs. ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228.
In vivo, ACY-738 induces dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors in novel, but not familiar environments. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels.
|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|
|Related HDAC Products|
Givinostat is an HDAC inhibitor with IC50s of 198 and 157 nM for HDAC1 and HDAC3, respectively.
Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
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.
Valproic acid is an HDAC inhibitor with IC50 in the range of 0.5~2 mM.
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