Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
|Cell lines||normal human (i.e., H69) and rat (NRC) cholangiocyte cell lines|
|Preparation method||Proliferation assays
Proliferation assays were conducted using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay (MTS; Promega) and/or counting cells using the Cellometer Auto4 (Nexcelom Bioscience) cell counter.
|Concentrations||0, 4 µ M|
|Incubation time||3 days|
|Animal models||orthotopic, syngeneic CCA model in rats|
|Dosages||10 mg/kg daily for 7 days|
|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.
|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.
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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