Apicidin is a potent nonselective HDAC inhibitor with IC50 of 0.7 nM. Apicidin is a fungal metabolite, as well as a histone deacetylase inhibitor. Antiangiogenic and anti-invasive; Apicidin not only blocks proliferation of human stomach and breast cancer cells, but also induces apoptosis and autophagy in human oral squamous carcinoma 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.
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin.
Han, et al. Cancer Res. 2000 Nov 1;60(21):6068-74. PMID: 11085529.
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase.
Darkin-Rattray, et al. Proc Natl Acad Sci U S A. 1996 Nov 12;93(23):13143-7. PMID: 8917558.
|Related HDAC Products|
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.
Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
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