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|
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.
ITSA-1 is a suppressor of Trichostatin A (TSA) and a molecular tool for dissecting gene regulation by distinct aceytlation events (histone and tubulin).
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.
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