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United States 

Actinonin

Protease inhibitor
 
ALX-260-128-M005 5 mg 138.00 USD
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Replaces Prod. #: BML-PI114

Antibiotic. Inhibitor of aminopeptidase M, N and leucine and alanyl aminopeptidase and peptide deformylase (PDF). Inhibits MMP-1 (Ki=300nM), MMP-2 (IC50~90nM at MMP-2=5nM), MMP-3 (Ki=1’700nM), MMP-7 (IC50~3’500nM at MMP-7=19nM), MMP-8 (Ki=160nM), MMP-9 (Ki=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. Apoptosis inducer.

Product Details

Alternative Name:3[[1-[[2-(Hydroxymethyl)-1-pyrrolidinyl]-carbonyl]-2-methylpropyl]-carbamoyl]-octanohydroxamic acid
 
Formula:C19H35N3O5
 
MW:385.5
 
Source:Synthetic.
 
CAS:13434-13-4
 
Purity:≥98% (HPLC)
 
Appearance:White to off-white powder.
 
Solubility:Soluble in 100% ethanol (20mg/ml) or DMSO (>20mg/ml).
 
Shipping:Ambient Temperature
 
Long Term Storage:-20°C
 
Regulatory Status:RUO - Research Use Only
 
ALX-260-128
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ALX-260-128

Product Literature References

Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation: E.L. Orth-He, et al.; Cell Rep. 42, 111965 (2023), Abstract;
Age-associated decline of MondoA drives cellular senescence through impaired autophagy and mitochondrial homeostasis: H.Y. Imoto, et al.; Cell Rep. 38, 110444 (2022), Abstract;
Parkin-independent mitophagy via Drp1-mediated outer membrane severing and inner membrane ubiquitination: Y. Oshima, et al.; J. Cell Biol. 220, 202006043 (2021), Abstract;
Formyl-methionine as a degradation signal at the N-termini of bacterial proteins: K.I. Piatkov, et al. ; Microb. Cell 2, 376 (2015), Application(s): Cell Culture, Abstract; Full Text
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;