Apicidin

BML-GR340

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HDAC inhibitor

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.

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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)
Appearance	White powder.
CAS	183506-66-3
Couple Target	HDAC
Couple Type	Inhibitor
Formula	C₃₄H₄₉N₅O₆
MW	623.8
Purity	≥99% (HPLC)
Solubility	Soluble in DMSO or 100% ethanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. 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.
Long Term Storage	-20°C
Shipping	Blue Ice

Regulatory Status	RUO – Research Use Only

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
Overlapping and Divergent Actions of Structurally Distinct Histone Deacetylase Inhibitors in Cardiac Fibroblasts: Schuetze, K. B., Stratton, M. S., et al.; J. Pharmacol. Exp. Ther. 361, 140 (2017), Abstract
Histone hyperacetylation up-regulates protein kinase Cδ in dopaminergic neurons to induce cell death: relevance to epigenetic mechanisms of neurodegeneration in Parkinson disease: Jin, H., Kanthasamy, A., et al.; J. Biol. Chem. 289, 34743 (2014), 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), Application(s): In Vitro, Abstract — Full Text
Valproic acid antagonizes the capacity of other histone deacetylase inhibitors to activate the Epstein-barr virus lytic cycle: Daigle, D., Gradoville, L., et al.; J. Virol. 85, 5628 (2011), Abstract
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
Identification of four potential epigenetic modulators from the NCI structural diversity library using a cell-based assay: Best, A. M., Chang, J., et al.; J. Biomed. Biotechnol. 2011, 868095 (2011), Abstract
Enhancement of vaccinia virus based oncolysis with histone deacetylase inhibitors: MacTavish, H., Diallo, J. S., et al.; PLoS One 5, e14462 (2011), Abstract
Cardiac HDAC6 catalytic activity is induced in response to chronic hypertension: Lemon, D. D., Horn, T. R., et al.; J. Mol. Cell. Cardiol. 51, 41 (2011), Abstract
Regulation of the HIF-1alpha stability by histone deacetylases: S.H. Kim, et al.; Oncol. Rep. 17, 647 (2007), Abstract

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Apicidin

BML-GR340

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