Apicidin

HDAC inhibitor



BML-GR340-0001	1 mg	59.00 USD

BML-GR340-0005	5 mg	239.00 USD

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 Specification

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)

Formula:	C₃₄H₄₉N₅O₆

MW:	623.8

Purity:	≥99% (HPLC, TLC)

CAS:	183506-66-3

Solubility:	Soluble in DMSO or 100% ethanol.

Long Term Storage:	-20°C

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.

Hazard:	VERY TOXIC.

Background / Technical Information:	Please click here for the comprehensive product datasheet.

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Product Literature References

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;