ALEXIS Biochemicals: Aaptamine

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ALX-270-047

Revised 26-Sep-07

Aristolochic acid
SYNONYMS	8-Methoxy-6-nitrophenanthrol(3,4-d)-1,3-dioxide-5-carboxylic acid
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-047-M025		25 mg	25.00 USD
ALX-270-047-M100		100 mg	90.00 USD

Product Specification

FORMULA:	C₁₇H₁₁NO₇
MW:	341.3
CAS NUMBER:	313-67-7
MERCK INDEX:	14: 786
RTECS:	CF3325000
SOURCE/HOST:	Isolated from Aristolochia clematis.
PURITY:	≥97% (~1:1 mixture of aristolochic acids I (A) and II (B))
APPEARANCE:	Yellow solid.
SOLUBILITY:	Soluble in DMSO or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
HAZARD:	MAY BE CARCINOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description

Phospholipase A₂(PLA₂) inhibitor active against the enzymes found in many snake venoms as well as those of human platelets and synovial fluids. Inhibits ionophore-stimulated PLA₂activity in human neutrophils. Has been shown to be nephropathic and carcinogenic.

Product Specific Literature References

Characterization of three edema-inducing phospholipase A2 enzymes from habu (Trimeresurus flavoviridis) venom and their interaction with the alkaloid aristolochic acid: B.S. Vishwanath, et al.; Toxicon 25, 501 (1987) Abstract
Interaction of aristolochic acid with Vipera russelli phospholipase A2: its effect on enzymatic and pathological activities: B.S. Vishwanath & T.V. Gowda; Toxicon 25, 929 (1987) Abstract
Interaction of phospholipase A2 from Vipera russelli venom with aristolochic acid: a circular dichroism study: B.S. Vishwanath, et al.; Toxicon 25, 939 (1987) Abstract
Edema-inducing activity of phospholipase A2 purified from human synovial fluid and inhibition by aristolochic acid: B.S. Vishwanath, et al.; Inflammation 12, 549 (1988) Abstract
Effects of aristolochic acid on phospholipase A2 activity and arachidonate metabolism of human neutrophils: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1001, 3 (1989) Abstract
Suramin alters phosphoinositide synthesis and inhibits growth factor receptor binding in HT-29 cells: R. Kopp & A. Pfeiffer; Cancer Res. 50, 6490 (1990) Abstract
The effects of the phospholipase A2 inhibitors aristolochic acid and PGBx on A23187-stimulated mobilization of arachidonate in human neutrophils are overcome by diacylglycerol or phorbol ester: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1126, 319 (1992) Abstract
Evidence for different mechanisms involved in the formation of lyso platelet-activating factor and the calcium-dependent release of arachidonic acid from human neutrophils: J.D. Winkler, et al.; Biochem. Pharmacol. 44, 2055 (1992) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Detection of DNA adducts formed by aristolochic acid in renal tissue from patients with Chinese herbs nephropathy: H.H. Schmeiser, et al.; Cancer Res. 56, 2025 (1996) Abstract
Aristolochic acid and ’Chinese herbs nephropathy’: a review of the evidence to date: J.P. Cosyns; Drug Saf. 26, 33 (2003), Review Abstract
Effect of aristolochic acid on intracellular calcium concentration and its links with apoptosis in renal tubular cells: Y.H. Hsin, et al.; Apoptosis 11, 2167 (2006) Abstract

Further Categories Containing This Product:

PLA2 Inhibitors • Carcinogens & Tumor Promoters Other Products • Natural Products - Other Tumor Promoters • Other Toxins • Alkaloids

ALX-270-075

Revised 08-Oct-08

KT5720
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-075-C100		100 µg	110.00 USD
ALX-270-075-C500		500 µg	330.00 USD
ALX-270-075-M001		1 mg	590.00 USD

Product Specification

FORMULA:	C₃₂H₃₁N₃O₅
MW:	537.6
CAS NUMBER:	108068-98-0
SOURCE/HOST:	Semisynthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in methanol (5mg/ml) or DMSO (1mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.

Product Description

Potent, reversible, cell permeable and selective inhibitor of cAMP-dependent protein kinase (PKA).

Product Specific Literature References

K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; BBRC 142, 436 (1987) Abstract
Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells: D.M. Gadbois, et al.; PNAS 89, 8626 (1992) Abstract
Effects of selective inhibition of protein kinase C, cyclic AMP- dependent protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons: L. Cabell and G. Audesirk; Int. J. Dev. Neurosci. 11, 357 (1993), (Review) Abstract

Further Categories Containing This Product:

Staurosporine / Related Products • Alkaloids

ALX-270-087

Revised 12-Mar-08

KT5823
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKG Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-087-C100		100 µg	110.00 USD
ALX-270-087-C500		500 µg	330.00 USD
ALX-270-087-M001		1 mg	590.00 USD

Product Specification

FORMULA:	C₂₉H₂₅N₃O₅
MW:	495.5
CAS NUMBER:	126643-37-6
SOURCE/HOST:	Semisynthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, dimethyl formamide or ethyl acetate.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.

Product Description

Potent and selective inhibitor of cGMP-dependent protein kinase (PKG).

Product Specific Literature References

K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; BBRC 142, 436 (1987) Abstract

Further Categories Containing This Product:

Staurosporine / Related Products • Alkaloids

ALX-270-110

Revised 20-Jun-08

Papaverine . hydrochloride
SYNONYMS	1-[(3',4'-Dimethoxyphenyl)methyl]-6,7-dimethoxyisoquinoline . HCl
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-110-G005		5 g	22.00 USD

Product Specification

FORMULA:	C₂₀H₂₁NO₄ . HCl
MW:	339.4 . 36.5
CAS NUMBER:	61-25-6
MERCK INDEX:	14: 7019
RTECS:	NW8575000
PURITY:	≥98%
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in 100% ethanol; slightly soluble in water (25mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	HARMFUL.

Product Description

Originally isolated from opium. Alkaloid with smooth muscle relaxing activity. Inhibits phosphodiesterases.

Product Specific Literature References

Papaverine-induced inhibition of phosphodiesterase activity in various mammalian tissues: G. Poch & W.R. Kukovetz; Life Sci. I 10, 133 (1971) Abstract
Effects of papaverine on smooth muscle and their mechanisms: M. Ferrari; Pharmacol. res. Commun. 6, 97 (1974) Abstract
The effect of papaverine on ion channels in rat basilar smooth muscle cells: D. Han, et al.; Neurol. Res. 29, 544 (2007) Abstract

Further Categories Containing This Product:

Phosphodiesterases / Related Products • Alkaloids

ALX-270-157

Revised 03-Apr-08

Australine . hydrochloride
SYNONYMS	(1R,2R,3R,7S,7aR)-3-Hydroxymethyl-1,2,7-trihydroxypyrrolizidine . HCI
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-157-M001		1 mg	180.00 USD

Product Specification

FORMULA:	C₈H₁₅NO₄. HCl
MW:	189.2 . 36.5
CAS NUMBER:	186766-07-4
SOURCE/HOST:	Isolated from Castanospermum australe seeds.
PURITY:	≥95%
APPEARANCE:	Crystalline solid.
SOLUBILITY:	Soluble in water, methanol and 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	After reconstitution, prepare aliquots and store at -20°C.
HAZARD:	HARMFUL.

Product Description

Alkaloid. Inhibitor of α-glucosidase, amyloglucosidase and glucosidase I. Does not inhibit glucosidase II, and is reported to be the first glucosidase inhibitor which differentiates glucosidase I from glucosidase II. Does not inhibit α-galactosidase, β-galactosidase, β-glucosidase, α-mannosidase and β-mannosidase.

Product Specific Literature References

Australine, a pyrrolizidine alkaloid that inhibits amyloglucosidase and glycoprotein processing: J.E. Tropea, et al.; Biochemistry 28, 2027 (1989) Abstract
Calystegins, a novel class of alkaloid glycosidase inhibitors: R.J. Molyneux, et al.; Arch. Biochem. Biophys. 304, 81 (1993) Abstract
Stereoselective synthesis of the glycosidase inhibitor australine through a one-pot, double-cyclization strategy: C. Ribes, et al.; Org. Lett. 9, 77 (2007) Abstract

Further Categories Containing This Product:

Glycosidases / Related Products • Alkaloids

ALX-270-160

Revised 27-Sep-07

Castanospermine
SYNONYMS	(1S,6S,7R,8R,8aR)-1,6,7,8-Tetrahydroxyoctahydroindolizine
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-160-M010		10 mg	60.00 USD
ALX-270-160-M050		50 mg	180.00 USD

Product Specification

FORMULA:	C₈H₁₅NO₄
MW:	189.2
CAS NUMBER:	79831-76-8
MERCK INDEX:	14: 1896
SOURCE/HOST:	Isolated from Castanospermum australe seeds.
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from moisture.

Product Description

Plant alkaloid. Potent inhibitor of α- and β-glucosidase activity in fibroblast extracts; inhibits the glycoprotein processing cycle. Exhibits antiviral properties. Prevents angiogenesis.

Product Specific Literature References

Castanospermine inhibits the processing of the oligosaccharide portion of the influenza viral hemagglutinin: Y.T. Pan, et al.; Biochemistry 22, 3975 (1983) Abstract
Glycoproteins: their structure, biosynthesis and possible clinical implications: H. Schachter; Clin. Biochem. 17, 3 (1984) Abstract
The effects of processing inhibitors of N-linked oligosaccharides on the intracellular migration of glycoprotein E2 of mouse hepatitis virus and the maturation of coronavirus particles: R. Repp, et al.; J. Biol. Chem. 260, 15873 (1985) Abstract; Full Text
Effects of the anti-inflammatory compounds castanospermine, mannose-6- phosphate and fucoidan on allograft rejection and elicited peritoneal exudates: M.R. Bartlett, et al.; Immunol. Cell Biol. 72, 367 (1994) Abstract
Antiviral activity and metabolism of the castanospermine derivative MDL 28,574, in cells infected with herpes simplex virus type 2: S.P. Ahmed, et al.; BBRC 208, 267 (1995) Abstract
The alpha-glucosidase I inhibitor castanospermine alters endothelial cell glycosylation, prevents angiogenesis, and inhibits tumor growth: R. Pili, et al.; Cancer Res. 55, 2920 (1995) Abstract
Perturbation of free oligosaccharide trafficking in endoplasmic reticulum glucosidase I-deficient and castanospermine-treated cells: C. Durrant & S.E. Moore; Biochem. J. 365, 239 (2002) Abstract

Further Categories Containing This Product:

Glycosidases / Related Products • Natural Products - Antiviral / anti-HIV Agents • Natural Products for Angiogenesis Research • Alkaloids

ALX-270-300

Revised 05-Apr-08

Fascaplysin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products for Cell Cycle Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-300-M001		1 mg	60.00 USD
ALX-270-300-M005		5 mg	240.00 USD

Product Specification

FORMULA:	C₁₈H₁₁N₂OCl
MW:	306.8
SOURCE/HOST:	Synthetic.
PURITY:	≥98%
APPEARANCE:	Brown powder.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
HANDLING:	Keep under inert gas. Protect from light.
HAZARD:	TOXIC.

Product Description

Originally isolated from a marine sponge. Selective CDK4/cyclin D1 (IC₅₀=350nM) inhibitor (in an ATP competitive manner).

Product Specific Literature References

Fascaplysin, an unusual antimicrobial pigment from the marine sponge Fascaplysinopsis sponge: D.M. Roll, et al.; J. Org. Chem. 53, 3276 (1988)
A new bioactive sesterterpene and antiplasmodial alkaloids from the marine sponge hyrtios cf. erecta: G. Kirsch, et al.; J. Nat. Prod. 63, 825 (2000) Abstract
Inhibition of cyclin-dependent kinase 4 (Cdk4) by fascaplysin, a marine natural product: R. Soni, et al.; BBRC 275, 877 (2000) Abstract
DNA binding properties of the marine sponge pigment fascaplysin: A. Hormann, et al.; Bioorg. Med. Chem. 9, 917 (2001) Abstract

Further Categories Containing This Product:

CDK & Cyclin Inhibitors • Marine Natural Products • Alkaloids

ALX-350-008

Revised 02-Oct-07

Chelerythrine chloride
SYNONYMS	1,2-Dimethoxy-N-methyl-[1,3]benzodioxolo[5,6-c]phenanthridinium chloride
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-008-M001		1 mg	25.00 USD
ALX-350-008-M005		5 mg	75.00 USD
ALX-350-008-M025		25 mg	300.00 USD

Product Specification

FORMULA:	C₂₁H₁₈NO₄Cl
MW:	383.8
CAS NUMBER:	3895-92-9
MERCK INDEX:	14: 2051
RTECS:	FL9200000
SOURCE/HOST:	Synthetic.
PURITY:	≥97% (completely free of biologically active impurities, such as sanguinarine)
APPEARANCE:	Yellow to orange solid.
SOLUBILITY:	Soluble in DMSO, water, 100% ethanol or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Heating to 40-50°C with gentle agitation may support complete solubilization. Further dilute with buffer just prior to use. Stock solutions should be refrigerated or frozen between for storage.
HAZARD:	HARMFUL.

Product Description

Potent, selective and cell permeable protein kinase C (PKC) inhibitor. Induces apoptosis. BH3 mimetic which inhibits Bcl-X_L function.

Product Specific Literature References

Antiplatelet effects of chelerythrine chloride isolated from Zanthoxylum simulans: F.-N. Ko, et al.; Biochim. Biophys. Acta 1052, 360 (1990) Abstract
Chelerythrine is a potent and specific inhibitor of protein kinase C: J.M. Herbert, et al.; BBRC 172, 993 (1990) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Identification of chelerythrine as an inhibitor of BclXL function: S.L. Chan, et al.; J. Biol. Chem. 278, 20453 (2003) Abstract
Chelerythrine and sanguinarine dock at distinct sites on BclXL that are not the classic BH3 binding cleft: Y.H. Zhang, et al.; J. Mol. Biol. 364, 536 (2006) Abstract
The effect of chelerythrine on cell growth, apoptosis, and cell cycle in human normal and cancer cells in comparison with sanguinarine: J. Malikova, et al.; Cell Biol. Toxicol. 22, 439 (2006) Abstract

Further Categories Containing This Product:

Bcl-2 Family Modulators • PKC Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Alkaloids

ALX-350-015

Revised 02-Dec-08

(S)-(+)-Camptothecin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Topoisomerase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-015-M050		50 mg	40.00 USD
ALX-350-015-M250		250 mg	150.00 USD
ALX-350-015-G001		1 g	295.00 USD

Product Specification

FORMULA:	C₂₀H₁₆N₂O₄
MW:	348.4
CAS NUMBER:	7689-03-4
MERCK INDEX:	14: 1735
RTECS:	UQ0492000
SOURCE/HOST:	Isolated from Mappia foetida Miers (Nothapodytes foetida (Wt.) Sleumer).
PURITY:	≥98% (HPLC)
APPEARANCE:	Pale yellow powder.
SOLUBILITY:	Soluble in DMSO (10mg/ml), methanol (40mg/ml) or 0.1N sodium hydroxide (50mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light and moisture. After reconstitution, prepare aliquots and store at -20°C.
HAZARD:	TOXIC.

Product Description

Potent antitumor agent. Inhibitor of DNA-topoisomerase I. Activates p53 resulting in upregulated expression of TRAIL-R2 (DR5) and Bak to overcome TRAIL resistance in Bax-deficient human colon carcinoma cells. Suppresses nitric oxide (NO) biosynthesis.

Product Specific Literature References

M.E. Wall, et al.; JACS 88, 3888 (1966)
The current status of camptothecin analogues as antitumor agents: W.J. Slichenmyer, et al.; J. Natl. Cancer Inst. 85, 271 (1993), (Review) Abstract
RNA synthesis inhibitors increase melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; Mol. Brain Res. 23, 47 (1994)