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Gliotoxin

Proteasome inhibitor
 
BML-PI129-0002 2 mg 133.00 USD
 
BML-PI129-0010 10 mg 415.00 USD
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Replaces Prod. #: ALX-350-239

Immunomodulating mycotoxin which acts by blocking membrane thiol groups. Inhibits the chymotrypsin-like activity of the 20S proteasome in a non-competitive manner. Causes apoptotic cell death in macrophages and thymocytes. Induces Ca2+ release from intact rat liver mitochondria. Inhibits the activation of transcription factor NF-κB in response to a variety of stimuli in T and B cells. Displays anti-inflammatory activity in vivo. Antioxidant. Inhibitor of farnesyltransferase and geranylgeranyltransferase I. A negative control analog is available (Prod. No. BML-L122). Displays anti-tumor activity against breast cancer in vivo.

Product Specification

Alternative Name:[3R-(3α, 5aβ,6β,10aα)]-2,3,5a,6-Tetrahydro-6-hydroxy-3-(hydroxymethyl)-2-methyl-10H-3,10a-epi-dithiopyrazino[1,2-a]indole-1,4-dione
 
Formula:C13H14N2O4S2
 
MW:326.4
 
Source:Isolated from Gladiocladium fimbriatum.
 
CAS:67-99-2
 
MI:14: 4441
 
RTECS:KB4725000
 
Purity:≥97% (HPLC, TLC)
 
Appearance:White to yellow crystalline solid.
 
Solubility:Soluble in DMSO or methanol (10mg/ml).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stock solutions are stable for up to 3 months when stored at -20°C.
 
ALX-350-239
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ALX-350-239

Product Literature References

Discovery of gliotoxin as a new small molecule targeting thioredoxin redox system: H.S. Choi, et al.; BBRC 359, 523 (2007), Abstract;
Aspergillus fumigatus suppresses the human cellular immune response via gliotoxin-mediated apoptosis of monocytes: M. Stanzani, et al.; Blood 105, 2258 (2005), Abstract;
Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivo: D.M. Vigushin, et al.; Med. Oncol. 21, 21 (2004), Abstract;
Nuclear factor-kappa B activity and intestinal inflammation in dextran sulphate sodium (DSS)-induced colitis in mice is suppressed by gliotoxin: H. Herfarth, et al.; Clin. Exp. Immunol. 120, 59 (2000), Abstract;
NF-kappaB activation is a critical regulator of human granulocyte apoptosis in vitro: C. Ward, et al.; J. Biol. Chem. 274, 4309 (1999), Abstract;
The secondary fungal metabolite gliotoxin targets proteolytic activities of the proteasome: M. Kroll, et al.; Chem. Biol. 6, 689 (1999), Abstract;
Gliotoxin and related epipolythiodioxopiperazines: P. Waring & J. Beaver; Gen. Pharmacol. 27, 1311 (1996), Review, Abstract;
The immunosuppressive fungal metabolite gliotoxin specifically inhibits transcription factor NF-kappaB: H.L. Pahl, et al.; J. Exp. Med. 183, 1829 (1996), Abstract;
Extracellular calcium is not required for gliotoxin or dexamethasone- induced DNA fragmentation: a reappraisal of the use of EGTA: P. Waring & A. Sjaarda; Int. J. Immunopharmacol. 17, 403 (1995), Abstract;
Gliotoxin stimulates Ca2+ release from intact rat liver mitochondria: M. Schweizer & C. Richter; Biochemistry 33, 13401 (1994), Abstract;
Mechanism of Gliotoxin Action and Factors Mediating Gliotoxin Sensitivity: R.W. Jones & J.G. Hancock; J. Gen. Microbiol. 134, 2067 (1988), Abstract;
Identification of an agent in cultures of Aspergillus fumigatus displaying anti-phagocytic and immunomodulating activity in vitro: A. Müllbacher, et al.; J. Gen. Microbiol. 131, 1251 (1985), Abstract;

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BML-L122-0001 1 mg 145.00 USD
 
BML-L122-0005 5 mg 395.00 USD
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