Replaces Prod. #: ALX-350-095
Potent inhibitor of histone deacetylase (HDAC). Inhibits proliferation. Induces cell cycle arrest at the G1 phase. At 100nM it induces a long lasting hyperacetylation of histone H4 while that induced by trichostatin is transient. Stimulates apoptosis. Apoptosis is induced via induction of Fas/Fas ligand. Displays potent antiangiogenic effects and dramatically decreases HIF-1α protein levels and transcriptional activity in human and mouse tumor cell lines. Antiprotozoal.
Product Details
| Alternative Name: | cyclo-L-(2-Amino-8-oxodecanoyl)-L-(N-methoxy-tryptophan)-L-isoleucyl-D-pipecolinyl, Cyclo(N-O-methyl-L-tryptophanyl-L-isoleucinyl-D-pipecolinyl-L-2-amino-8-oxodecanoyl) |
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| Formula: | C34H49N5O6 |
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| MW: | 623.8 |
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| CAS: | 183506-66-3 |
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| Purity: | ≥99% (HPLC) |
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| Appearance: | White powder. |
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| Solubility: | Soluble in DMSO or 100% ethanol. |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
HDAC8 regulates protein kinase D phosphorylation in skeletal myoblasts in response to stress signaling: J.S. Habibian, et al.; Biochem. Biophys. Res. Commun.
650, 81 (2023),
Abstract;
Histone deacetylase (HDAC) 1 controls the expression of beta defensin 1 in human lung epithelial cells: K. Kallsen, et al.; PLoS One
7, e50000 (2012),
Abstract;
Full Text
Inhibitors of histone deacetylases: correlation between isoform specificity and reactivation of HIV type 1 (HIV-1) from latently infected cells: K. Huber, et al.; J. Biol. Chem.
286, 22211 (2011),
Abstract;
Full Text
Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells: T. Ueda, et al.; Int. J. Mol. Med.
19, 301 (2007),
Abstract;
Regulation of the HIF-1alpha stability by histone deacetylases: S.H. Kim, et al.; Oncol. Rep.
17, 647 (2007),
Abstract;
Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis: Y.K. Kim, et al.; Cell Death Differ.
13, 2033 (2006),
Abstract;
Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells: J. Hong, et al.; Cancer Lett.
189, 197 (2003),
Abstract;
Apicidin, a histone deacetylase inhibitor, induces apoptosis and Fas/Fas ligand expression in human acute promyelocytic leukemia cells: S.H. Kwon, et al.; J. Biol. Chem.
277, 2073 (2002),
Abstract;
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities: S.B. Singh, et al.; J. Org. Chem.
67, 815 (2002),
Abstract;
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett.
11, 107 (2001),
Abstract;
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett.
11, 113 (2001),
Abstract;
Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor: J.S. Kim, et al.; BBRC
281, 866 (2001),
Abstract;
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin: J.W. Han, et al.; Cancer Res.
60, 6068 (2000),
Abstract;
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase: S.J. Darkin-Rattray, et al.; PNAS
93, 13143 (1996),
Abstract;
