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MPTP [Mitochondrial Transition Pore] / Related Products
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Items 15 of 15
ALX-430-064 Revised 15-Sep-08
Auranofin
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Lipoxygenases / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-064-M025   25 mg 35.00 USD Add To Cart
ALX-430-064-M100   100 mg 68.00 USD Add To Cart
Product Specification
FORMULA: C20H34AuO9PS
MW: 678.5
CAS NUMBER: 34031-32-8
MERCK INDEX: 14: 878
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (5mg/ml) or 100% ethanol (4mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions are stable for up to 3 months when stored at -20 °C.
HAZARD: TOXIC.

Product Description
Gold derivative in clinical use as an anti-arthritic. Acts as an inhibitor of several leukocyte activation pathways. Inhibits release of inflammatory mediators from human macrophages, pulmonary mast cell and basophils. Also inhibits human neutrophil 5-lipoxygenase. Efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions, potentially referable to its inhibition of mitochondrial thioredoxin reductase.
Product Specific Literature References
Antiarthritic gold compounds effectively quench electronically excited singlet oxygen: E.J. Corey, et al.; Science 236, 68 (1987) Abstract
Modulation of mediator release from human basophils and pulmonary mast cells and macrophages by auranofin: M. Columbo, et al.; Biochem. Pharmacol. 39, 285 (1990) Abstract
Auranofin stimulates LTA hydrolase and inhibits 5-lipoxygenase/LTA synthase activity of isolated human neutrophils: W.H. Betts, et al.; Biochem. Pharmacol. 39, 1233 (1990) Abstract
Auranofin inhibits the activation pathways of polymorphonuclear leukocytes at multiple sites: R. Rudkowski, et al.; Biochem. Pharmacol. 41, 1921 (1991) Abstract
Induction of mitochondrial permeability transition by auranofin, a Gold(I)-phosphine derivative: M.P. Rigobello, et al.; Br. J. Pharmacol. 136, 1162 (2002) Abstract
General Literature References
Auranofin: W.F. Kean, et al.; Br. J. Theumatol. 36, 560 (1997), (Review) Abstract; Full Text
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products • TLRs Other Products • Anti-inflammatory Agents Other Products
 
 
ALX-350-277 Revised 03-Apr-08
Betulinic acid (high purity)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-277-M005   5 mg 32.00 USD Add To Cart
ALX-350-277-M025   25 mg 95.00 USD Add To Cart
ALX-350-277-M100   100 mg 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane) tree bark.
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: IRRITANT.

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo: T. Syrovets, et al.; J. Biol. Chem. 280, 6170 (2005) Abstract
Induction of central signalling pathways and select functional effects in human platelets by beta-boswellic acid: D. Poeckel, et al.; Br. J. Pharmacol. 146, 514 (2005) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari and D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid and its derivatives, potent DNA topoisomerase II inhibitors, from the bark of Bischofia javanica: S. Wada & R. Tanaka; Chem. Biodivers. 2, 689 (2005) Abstract
Betulinic acid as new activator of NF-kappaB: molecular mechanisms and implications for cancer therapy: H. Kasperczyk, et al.; Oncogene 24, 6945 (2005) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
Further Categories Containing This Product:
Other Natural Products - DNA Regulation / Transcription • Natural Products - NF-kB Pathway Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors • Natural Products - Antiviral / anti-HIV Agents • Antitumor Agents (Apoptosis Inducers) • HIV / AIDS / Related Products
 
 
ALX-350-298 Revised 03-Apr-08
Betulinic acid (~95%)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-298-M100   100 mg 55.00 USD Add To Cart
ALX-350-298-M500   500 mg 180.00 USD Add To Cart
ALX-350-298-G001   1 g 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane tree) bark.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • NF-kB Pathway Inhibitors • Other Natural Products - DNA Regulation / Transcription • Natural Products - NF-kB Pathway Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Ubiquitin & Proteasome Other Products • Antitumor Agents (Apoptosis Inducers) • HIV / AIDS / Related Products
 
 
ALX-380-002 Revised 03-Apr-08
Cyclosporin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-002-M100   100 mg 46.00 USD Add To Cart
ALX-380-002-5100   5x100 mg 190.00 USD Add To Cart
ALX-380-002-G001   1 g 290.00 USD Add To Cart
ALX-380-002-5001   5x1 g 1'150.00 USD Add To Cart
Product Specification
FORMULA: C62H111N11O12
MW: 1202.6
CAS NUMBER: 59865-13-3
MERCK INDEX: 14: 2752
RTECS: GZ4120000
SOURCE/HOST: Isolated from Fusarium solani.
PURITY: ≥99% (Assay)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol, 100% ethanol, acetone or petroleum ether; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE TERATOGENIC. TOXIC. MAY BE CARCINOGENIC.

Product Description
Antibiotic. Potent immunosuppressor. Widely used after organ transplantation. Binds to cytosolic proteins of the cyclophilin family. Cyclosporin A-cyclophilin complexes block protein phosphatase 2B (PP2B; calcineurin), a key enzyme in T cell activation. As a result of the calcineurin inhibition, cyclosporine A blocks various cellular processes such as activation of T cells and expression of several lymphokines (especially IL-2). Inhibits cytochrome c release from mitochondria. Inhibits nitric oxide (NO) synthesis.
Product Specific Literature References
Cyclosporin A and C-New metabolites from Trichodermapolysporum (Link ex Pers.) Rifai: Dreyfuss M., et al.; Europ. J. appl. Microbiol. 3, 125 (1976)
Immunosuppression for organ grafting - observations on cyclosporin A: R. Y. Calne; Immunol. Rev. 46, 113 (1976), Review Abstract
Immunological actions of cyclosporin A in rheumatoid arthritis: D. Yocum; Br. J. Rheumatol. 32, 38 (1993), Review Abstract
Cyclosporin A binding to mitochondrial cyclophilin inhibits the permeability transition pore and protects hearts from ischaemia/reperfusion injury: A.P. Halestrap, et al; Mol. Cell. Biochem. 174, 167 (1997), Review Abstract
New aspects of cyclosporin a mode of action: from gene silencing to gene up-regulation: L. Mascarell & P. Truffa-Bachi; Mini Rev. Med. Chem. 3, 205 (2003), Review Abstract
Rationale for T cell inhibition by cyclosporin A in major autoimmune diseases: G.F. Ferraccioli, et al.; Ann. N. Y. Acad. Sci. 1051, 658 (2005), Review Abstract
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products • Antibiotics - Nitric Oxide Pathway Modulators • Antibiotics - Apoptosis Inducers & Inhibitors • Non-apoptotic Cell Death / Necrosis
 
 
ALX-380-284 Revised 08-Apr-08
Cyclosporin D
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SYNONYMS Val2-cyclosporin
7-L-Valine-cyclosporin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-284-M001   1 mg 80.00 USD Add To Cart
ALX-380-284-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C63H113N11O12
MW: 1216.6
CAS NUMBER: 63775-96-2
MERCK INDEX: 14: 2752
SOURCE/HOST: Isolated from Fusarium solani.
PURITY: ≥95% (HPLC)
APPEARANCE: Colorless to off-white crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, acetone or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE TERATOGENIC. TOXIC. MAY BE CARCINOGENIC.

Product Description
Weak immunosuppressor. Potent inhibitor of tumor promoting phorbol ester TPA/PMA (Prod. No. ALX-445-004) in vivo. Potent inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro.
Product Specific Literature References
The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro: M. Gschwendt, et al.; BBRC 150, 545 (1988) Abstract
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products • CAM Kinase Inhibitors
 
 
ALX-380-286 Revised 08-Apr-08
Cyclosporin H
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SYNONYMS Csh-cyclosporin
5-(N-Methyl-D-valine)-cyclosporin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-286-M001   1 mg 80.00 USD Add To Cart
ALX-380-286-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C62H111N11O12
MW: 1202.6
CAS NUMBER: 83602-39-5
SOURCE/HOST: Isolated from Fusarium solani.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, acetone or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE TERATOGENIC. TOXIC. MAY BE CARCINOGENIC.

Product Description

Immunologically inactive. Does not bind to immunophilin. Potent inhibitor of tumor promoting phorbol ester TPA/PMA (Prod. No. ALX-445-004) in mouse skin in vivo. Potent inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro. Potent and selective antagonist of formyl peptide receptor. Inhibits formyl peptide-induced superoxide formation.

Product Specific Literature References
The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro: M. Gschwendt, et al.; BBRC 150, 545 (1988) Abstract
Differential inhibition of human neutrophil activation by cyclosporins A, D, and H. Cyclosporin H is a potent and effective inhibitor of formyl peptide-induced superoxide formation: K. Wenzel-Seifert, et al.; J. Immunol. 147, 1940 (1991) Abstract
Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E: K. Wenzel-Seifert & R. Seifert; J. Immunol. 150, 4591 (1993) Abstract
Cyclosporin H is a potent and selective competitive antagonist of human basophil activation by N-formyl-methionyl-leucyl-phenylalanine: A. de Paulis, et al.; J. Allergy Clin. Immunol. 98, 152 (1996) Abstract
Cyclosporin H, Boc-MLF and Boc-FLFLF are antagonists that preferentially inhibit activity triggered through the formyl peptide receptor: A.L. Stenfeldt, et al.; Inflammation 30, 224 (2007) Abstract
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors • CAM Kinase Inhibitors • Antibiotics - Nitric Oxide Pathway Modulators • Non-apoptotic Cell Death / Necrosis
 
 
ALX-270-293 Revised 28-Mar-08
Decylubiquinone
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SYNONYMS 2,3-Dimethoxy-5-methyl-6-decyl-1,4-benzoquinone
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Coenzymes & Vitamins Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-293-M010   10 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C19H30O4
MW: 322.4
CAS NUMBER: 55486-00-5
PURITY: ≥97% (TLC)
APPEARANCE: Clear orange to red liquid.
SOLUBILITY: Soluble in DMSO (10mg/ml) or TRIS buffer.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions in DMSO are stable for up to 3 months when stored at -20°C.
HAZARD: IRRITANT.

Product Description
Inhibitor of the mitochondrial permeability transition pore (MPTP). This inhibitory effect can be counteracted by ubiquinone-5 (Prod. No. ALX-270-294).
Product Specific Literature References
A ubiquinone-binding site regulates the mitochondrial permeability transition pore: E. Fontaine, et al.; J. Biol. Chem. 273, 25734 (1998) Abstract; Full Text
The course of etoposide-induced apoptosis from damage to DNA and p53 activation to mitochondrial release of cytochrome c: N.O. Karpinich, et al.; J. Biol. Chem. 277, 16547 (2002) Abstract; Full Text
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products
 
 
ALX-350-098 Revised 05-Apr-08
Ferutinin (high purity)
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SYNONYMS Tefestrol (high purity)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-098-M001   1 mg 35.00 USD Add To Cart
ALX-350-098-M005   5 mg 100.00 USD Add To Cart
ALX-350-098-M010   10 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5