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MMP Inhibitors
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ALX-260-165 Revised 10-Nov-08
MMP-3 Inhibitor
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SYNONYMS Ac-RCGVPD-NH2
Stromelysin-1 Inhibitor
PRODUCT LINE Cytoskeleton
PRODUCT CATEGORY MMP Inhibitors
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ALX-260-165-M001   1 mg 45.00 USD Add To Cart
ALX-260-165-M005   5 mg 180.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Arg-Cys-Gly-Val-Pro-Asp-NH2
FORMULA: C27H46N10O9S
MW: 686.8
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Inhibitor of matrix metalloproteinase 3 (MMP-3) (IC50=5µM).
Product Specific Literature References
Peptides based on the conserved predomain sequence of matrix metalloproteinases inhibit human stromelysin and collagenase: A.C. Hanglow, et al.; Agents Actions 39, C148 (1993) Abstract
Potent peptide inhibitors of stromelysin based on the prodomain region of matrix metalloproteinases: N. Fotouhi, et al.; J. Biol. Chem. 269, 30227 (1994) Abstract
 
 
ALX-270-280 Revised 07-Apr-08
clasto-Lactacystin β-lactone (synthetic)
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SYNONYMS Omuralide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-270-280-C200   200 µg 280.00 USD Add To Cart
ALX-270-280-M001   1 mg 1'295.00 USD Add To Cart
Product Specification
FORMULA: C10H15NO4
MW: 213.2
CAS NUMBER: 155975-72-7
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 20mg/ml soluble in DMSO or acetonitrile.
ACTIVITY: Kobs/[I]=20’000M-1s-1 versus 20S:PA28 complex.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR.

Product Description
Highly specific, cell permeable, and irreversible 20S proteasome inhibitor. Inhibits ubiquitin proteasome pathway in cell culture (IC50=1µM). It has been suggested that the natural product lactacystin acts as a precursor for clasto-lactacystin β-lactone and that the latter is the sole species that interacts with the proteasome. Inhibits cathepsin A. Leads to a reduction of adipogenesis.
Product Specific Literature References
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Mechanistic studies on the inactivation of the proteasome by lactacystin: a central role for clasto-lactacystin beta-lactone: L.R. Dick, et al.; J. Biol. Chem. 271, 7273 (1996) Abstract
Mechanistic studies on the inactivation of the proteasome by lactacystin in cultured cells: L.R. Dick, et al.; J. Biol. Chem. 272, 182 (1997) Abstract; Full Text
Lactacystin and clasto-lactacystin beta-lactone modify multiple proteasome beta-subunits and inhibit intracellular protein degradation and major histocompatibility complex class I antigen presentation: A. Craiu, et al.; J. Biol. Chem. 272, 13437 (1997) Abstract; Full Text
Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998) Abstract; Full Text
Total synthesis and biological activity of lactacystin, omuralide and analogs: E.J. Corey & W.D. Li; Chem. Pharm. Bull. 47, 1 (1999) Abstract
Lactacystin, a proteasome inhibitor: discovery and its application in cell biology: H. Tomoda & S. Omura; Yakugaku Zasshi 120, 935 (2000), Review Abstract
Lactacystin inhibits cathepsin A activity in melanoma cell lines: L. Kozlowski, et al.; Tumour Biol. 22, 211 (2001) Abstract
Inhibition of human preadipocyte proteasomal activity by HIV protease inhibitors or specific inhibitor lactacystin leads to a defect in adipogenesis, which involves matrix metalloproteinase-9: S. De Barros, et al.; J. Pharmacol. Exp. Ther. 320, 291 (2007) Abstract
Effect of proteasome inhibitor clasto-lactacystin-beta-lactone on the proteome of the haloarchaeon Haloferax volcanii: P.A. Kirkland, et al.; Microbiology 153, 2271 (2007) Abstract
Further Categories Containing This Product:
Cathepsin InhibitorsProteasome / Related ProductsMMP Inhibitors
 
 
ALX-270-337 Revised 04-Mar-05
3-(4-Phenoxyphenylsulfonyl)propylthiirane
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SYNONYMS MMP-2/MMP-9 Inhibitor
PRODUCT LINE Cytoskeleton
PRODUCT CATEGORY MMP Inhibitors
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ALX-270-337-M005   5 mg 50.00 USD Add To Cart
ALX-270-337-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H14O3S2
MW: 306.4
PURITY: ≥98%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in DMSO, chloroform, acetone, methanol and other organic solvents.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Potent and selective inhibitor of matrix metalloproteinases 2 and 9.
Product Specific Literature References
Potent and selective mechanism-based inhibition of Gelatinases: S. Brown, et al.; JACS 122, 6799 (2000)
Tissue inhibitor of metalloproteinase (TIMP)-2 acts synergistically with synthetic matrix metalloproteinase (MMP) inhibitors but not with TIMP-4 to enhance the (Membrane type 1)-MMP-dependent activation of pro-MMP-2: M. Toth, et al.; J. Biol. Chem. 275, 41415 (2000) Abstract; Full Text
X-ray absorption studies of human matrix metalloproteinase-2 (MMP-2) bound to a highly selective mechanism-based inhibitor. comparison with the latent and active forms of the enzyme: O. Kleifeld, et al.; J. Biol. Chem. 276, 17125 (2001) Abstract; Full Text
 
 
ALX-350-145 Revised 28-Mar-07
Isobavachalcone
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SYNONYMS 2’,4’,4-Trihydroxy-3’-[3’’-methylbut-3’’-enyl]chalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-145-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C20H20O4
MW: 324.4
CAS NUMBER: 20784-50-3
SOURCE/HOST: Isolated from plant Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Inhibits platelet aggregation. Inhibitor of Epstein-Barr virus early antigen (EBV-EA) induction. Exhibits potent inhibitory effect on skin tumor promotion. Potent inhibitor of MMP-2. Displays DNA strand-scission (cleaving) activity. Shows antifungal activity.
Product Specific Literature References
Antiplatelet flavonoids from seeds of Psoralea corylifolia: W.J. Tsai, et al.; J. Nat. Prod. 59, 671 (1996) Abstract
Antioxidative components of Psoralea corylifolia (Leguminosae): H. Haraguchi, et al.; Phytother. Res. 16, 539 (2002) Abstract
Chalcones, coumarins, and flavanones from the exudate of Angelica keiskei and their chemopreventive effects: T. Akihisa, et al.; Cancer Lett. 201, 133 (2003) Abstract
Antitrichomonal and antioxidant activities of Dorstenia barteri and Dorstenia convexa: N.O. Omisore, et al.; Braz. J. Med. Biol. Res. 38, 1087 (2005) Abstract
Chalcones and other compounds from the exudates of Angelica keiskei and their cancer chemopreventive effects: T. Akihisa, et al.; J. Nat. Prod. 69, 38 (2006) Abstract
Inhibition of matrix metalloproteinase-2 secretion by chalcones from the twigs of Dorstenia barteri Bureau.: B. Ngameni, et al.; Arkivoc ix, 91 (2007) Full Text
 
 
ALX-350-334 Revised 03-Apr-08
Ascochlorin
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SYNONYMS LL-Z 1272 γ
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-350-334-MC05   0.5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C23H29ClO4
MW: 404.9
CAS NUMBER: 26166-39-2
RTECS: VH3707560
SOURCE/HOST: Isolated from Acremonium sp. MST-FP1890.
PURITY: ≥95% (HPLC)
APPEARANCE: White to light grey powder.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Antitumor antibiotic. Shows antiviral activity. Inhibitor or matrix metalloproteinase 9 (MMP-9). Reduces the inflammatory response to TNF-α in rat vascular smooth muscle cells. May be useful as an antiatherogenic agent.
Product Specific Literature References
Ascochlorin, a new antibiotic, found by the paper-disc agar-diffusion method. I. Isolation, biological and chemical properties of ascochlorin. (Studies on antiviral and antitumor antibiotics. I): G. Tamura, et al.; J. Antibiot. (Tokyo) 21, 539 (1968) Abstract
Ascochlorin derivatives as ligands for nuclear hormone receptors: M. Togashi, et al.; J. Med. Chem. 46, 4113 (2003) Abstract
Ascochlorin inhibits matrix metalloproteinase-9 expression by suppressing activator protein-1-mediated gene expression through the ERK1/2 signaling pathway: inhibitory effects of ascochlorin on the invasion of renal carcinoma cells: S. Hong, et al.; J. Biol. Chem. 280, 25202 (2005) Abstract; Full Text
Selective cytotoxicity of ascochlorin in ER-negative human breast cancer cell lines: K. Sakaguchi, et al.; BBRC 329, 46 (2005) Abstract
Ascochlorin suppresses oxLDL-induced MMP-9 expression by inhibiting the MEK/ERK signaling pathway in human THP-1 macrophages: J.H. Kang, et al.; J. Cell. Biochem. 102, 506 (2007) Abstract
 
 
ALX-380-273 Revised 03-Apr-08
Doxycycline . hyclate
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SYNONYMS Doxycycline . hydrochloride . hemiethanolate . hemihydrate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
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ALX-380-273-G001   1 g 20.00 USD Add To Cart
ALX-380-273-G005   5 g 60.00 USD Add To Cart
Product Specification
FORMULA: C22H24N2O8 . HCl . 0.5C2H6O . 0.5H2O
MW: 444.4 . 36.5 . 23.0 . 9.0
CAS NUMBER: 24390-14-5
MERCK INDEX: 14: 3440
RTECS: QI8925000
SOURCE/HOST: Semisynthetic from oxytetracycline.
PURITY: ≥98% (Assay on dry basis)
APPEARANCE: Yellow crystalline solid.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: HARMFUL. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description
Broad spectrum antibiotic and bacteriostatic. Shows antiprotozoal properties. Potent inhibitor of MMPs (matrix metalloproteinases) in vivo. Inhibits collagen synthesis.
Product Specific Literature References
Alpha-6-deoxyoxytetracycline. I. Some biological properties: A.R. English; Proc. Soc. Exp. Biol. Med. 122, 1107 (1966) Abstract
A compilation of LD50 values in newborn and adult animals: E.I. Goldenthal; Toxicol. Appl. Pharmacol. 18, 185 (1971) Abstract
An efficacy trial of doxycycline chemoprophylaxis against leptospirosis: E.T. Takafuji, et al.; N. Engl. J. Med. 310, 497 (1984) Abstract
Specificity of the anticollagenase action of tetracyclines: relevance to their anti-inflammatory potential: K. Suomalainen, et al.; Antimicrob. Agents Chemother. 36, 227 (1992) Abstract
Matrix metalloproteinase-8 is expressed in rheumatoid synovial fibroblasts and endothelial cells. Regulation by tumor necrosis factor-alpha and doxycycline: R. Hanemaaijer, et al.; J. Biol. Chem. 272, 31504 (1997) Abstract; Full Text
Doxycycline and tissue repair in rats: S. Lamparter, et al.; J. Lab. Clin. Med. 139, 295 (2002) Abstract
Molecular interactions between matrilysin and the matrix metalloproteinase inhibitor doxycycline investigated by deuterium exchange mass spectrometry: R.A. Garcia, et al.; Mol. Pharmacol. 67, 1128 (2005) Abstract; Full Text
Doxycycline alters vascular smooth muscle cell adhesion, migration, and reorganization of fibrillar collagen matrices: C. Franco, et al.; Am. J. Pathol. 168, 1697 (2006) Abstract; Full Text
Doxycycline inhibits MMPs via modulation of plasminogen activators in focal cerebral ischemia: D. Burggraf, et al.; Neurobiol. Dis. 25, 506 (2007) Abstract
 
 

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