Gliotoxin

Proteasome inhibitor



BML-PI129-0002	2 mg	77.00 USD

BML-PI129-0010	10 mg	330.00 USD

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 negatve control analog is available (Prod. No. BML-L122).

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

Purity:	≥98% (TLC)

Appearance:	White solid.

CAS:	67-99-2

MI:	14: 4441

RTECS:	KB4725000

Source/Host:	Isolated from Gladiocladium fimbriatum.

Solubility:	Soluble in DMSO or methanol (10mg/ml).

Long Term Storage:	-20°C

Use/Stability:	Stock solutions are stable for up to 3 months when stored at -20°C.

Hazard:	TOXIC.

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

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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;

R.J. Jones & J.G. Hancock; J. Gen. Microbiol. 134, 2067 (1988),

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;