Actinonin

Protease inhibitor



ALX-260-128-M005	5 mg	86.00 USD

Replaces Prod. #: BML-PI114

Antibiotic. Inhibitor of aminopeptidase M, N and leucine and alanyl aminopeptidase and peptide deformylase (PDF). Inhibits MMP-1 (K_i=300nM), MMP-2 (IC₅₀~90nM at MMP-2=5nM), MMP-3 (K_i=1’700nM), MMP-7 (IC₅₀~3’500nM at MMP-7=19nM), MMP-8 (K_i=160nM), MMP-9 (K_i=330nM), MMP-10 (IC₅₀~500nM at MMP-10=22nM), MMP-12 (IC₅₀~350nM at MMP-12=4nM), and MMP-13 (IC₅₀~100nM at MMP-13=13nM), but not MMP-14 (IC₅₀>1mM at MMP-14=13.6nM). Shows antitumor activity in vitro and in vivo.

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Product Specification

Alternative Name:	3[[1-[[2-(Hydroxymethyl)-1-pyrrolidinyl]-carbonyl]-2-methylpropyl]-carbamoyl]-octanohydroxamic acid

Formula:	C₁₉H₃₅N₃O₅

MW:	385.5

Purity:	≥98%

Appearance:	White to off-white powder.

CAS:	13434-13-4

Source/Host:	Synthetic.

Solubility:	Soluble in 100% ethanol (20mg/ml) or DMSO (>20mg/ml).

Long Term Storage:	-20°C

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Product Literature References

Actinonin induces apoptosis in U937 leukemia cells: M. Grujic, et al.; Cancer Lett. 223, 211 (2005), Abstract;

Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics: M.D. Lee, et al.; J. Clin. Invest. 114, 1107 (2004), Abstract;

Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor: D.Z. Chen, et al.; Biochemistry 39, 1256 (2000), Abstract;

Antitumor activity of actinonin in vitro and in vivo: Y. Xu, et al.; Clin. Cancer Res. 4, 171 (1998), Abstract;

Inhibition of alanyl aminopeptidase induces MAP-kinase p42/ERK2 in the human T cell line KARPAS-299: U. Lendeckel, et al.; BBRC 252, 5 (1998), Abstract;

Effects of an antibiotic protease inhibitor, actinonin on the growth within collagen gels of non-metastatic and metastatic mouse mammary tumors of the same origin: K. Sayama, et al.; Cancer Lett 94, 171 (1995), Abstract;

Gene expression, purification and characterization of recombinant human neutrophil collagenase: T.F. Ho, et al.; Gene 146, 297 (1994), Abstract;

Analgesic effect of actinonin, a new potent inhibitor of multiple enkephalin degrading enzymes: M. Hachisu, et al.; Life Sci. 41, 235 (1987), Abstract;

Production of actinonin, an inhibitor of aminopeptidase M, by actinomycetes: H. Umezawa, et al.; J. Antibiot. (Tokyo) 38, 1629 (1985), Abstract;