ALEXIS Biochemicals: UK-1

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ALX-380-224

Revised 09-Jun-08

21-Hydroxyoligomycin A
SYNONYMS	Nemadectin ω Antibiotic LL-F28249 ω
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antitumor Antibiotics

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-224-M001		1 mg	360.00 USD

Product Specification

FORMULA:	C₄₅H₇₄O₁₂
MW:	807.1
CAS NUMBER:	102042-09-1
SOURCE/HOST:	Isolated from Streptomyces sp. AS5351.
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Co-metabolite of nemadectin. Antitumor agent with weak antifungal and nematocidal activity.

Product Specific Literature References

Plasmid effects on secondary metabolite production by a streptomycete synthesizing an anthelmintic macrolide: D.I. Thomas, et al.; J. Gen. Microbiol. 137, 2331 (1991) Abstract
Structure and absolute stereochemistry of 21-hydroxyoligomycin A: M.M. Wagenaar, et al.; J. Nat. Prod. 70, 367 (2007) Abstract

ALX-380-116

Revised 07-Apr-08

Hypothemycin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Antifungal

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-116-C250		250 µg	140.00 USD
ALX-380-116-M001		1 mg	420.00 USD

Product Specification

FORMULA:	C₁₉H₂₂O₈
MW:	378.4
CAS NUMBER:	76958-67-3
SOURCE/HOST:	Isolated from Phoma sp.
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white solid.
SOLUBILITY:	Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.

Product Specific Literature References

Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors • Tyrosine Kinase Inhibitors • Antibiotics - Protein Kinase Inhibitors • Antibiotics - Proteasome / Ubiquitin Modulators • Antitumor Antibiotics • Ras Signalling Pathway Other Products • Ubiquitination Other Products • Antitumor Agents (DNA Interaction & Gene Regulation) • CDKs & Cyclins Other Products

ALX-380-260

Revised 07-Apr-08

Idarubicin . hydrochloride
SYNONYMS	Idamycin DMDR 4-Demethoxydaunorubicin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Apoptosis Inducers & Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-260-M001		1 mg	45.00 USD
ALX-380-260-M005		5 mg	180.00 USD

Product Specification

FORMULA:	C₂₆H₂₇NO₉ . HCl
MW:	497.5 . 36.5
CAS NUMBER:	57852-57-0
MERCK INDEX:	14: 4886
RTECS:	HB7877000
SOURCE/HOST:	Synthetic.
PURITY:	≥98%
APPEARANCE:	Orange crystalline solid.
SOLUBILITY:	Soluble in water or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	VERY TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

More potent, lipophilic and antineoplastic analog of daunorubicin. DNA-damaging effect includes DNA oxidation and methylation, DNA intercalation, inhibition of DNA synthesis, induction of DNA strand breaks and delay of cell cycle progression. Inhibitor of topoisomerase IIα. Produces endonucleolytic cleavage and is a marker of apoptosis.

Product Specific Literature References

Idarubicin (4-demethoxydaunorubicin). A preliminary overview of preclinical and clinical studies: F. Ganzina, et al.; Invest. New Drugs 4, 85 (1986), Review Abstract
Antitumor activity of idarubicin, a derivative of daunorubicin, against drug sensitive and resistant P388 leukemia: T. Tsuruo, et al.; Anticancer Res. 13, 357 (1993) Abstract
Study of apoptosis-related responses of leukemic blast cells to in vitro anthracycline treatment: M.A. Belaud-Rotureau, et al.; Leukemia 14, 1266 (2000) Abstract
A comparison of the in vitro genotoxicity of anticancer drugs idarubicin and mitoxantrone: J. Blasiak, et al.; Acta Biochim. Pol. 49, 145 (2002) Abstract; Full Text
Repair of idarubicin-induced DNA damage: A cause of resistance?: D.C. Dartsch & F. Gieseler; DNA Repair (Amst) 6, 1618 (2007) Abstract

Further Categories Containing This Product:

Antibiotics - Topoisomerase Inhibitors • Antitumor Agents (Apoptosis Inducers) • Antitumor Antibiotics • Antitumor Agents (DNA Interaction & Gene Regulation)

ALX-380-230

Revised 07-Apr-08

Kazusamycin A
SYNONYMS	Kazusamycin Hydroxyleptomycin B Antibiotic CL 1957B Hydroxyelactocin PD 114,721
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antitumor Antibiotics

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-230-MC01		0.1 mg	460.00 USD

Product Specification

FORMULA:	C₃₃H₄₈O₇
MW:	556.7
CAS NUMBER:	92090-94-3
RTECS:	OA0550000
SOURCE/HOST:	Isolated from Streptomyces sp. MST-AS4898.
PURITY:	≥95% (HPLC)
APPEARANCE:	Colorless film.
SOLUBILITY:	Soluble in 100% ethanol (recommended) or methanol. Unstable in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Shows potent antitumor activity in vitro and in vivo against several tumor cell lines. Has antibacterial and antifungal activities. Inhibitor of nuclear export.

Product Specific Literature References

A new antitumor antibiotic, kazusamycin: I. Umezawa, et al.; J. Antibiot. (Tokyo) 37, 706 (1984) Abstract
Antitumor activity of a new antibiotic, kazusamycin: K. Komiyama, et al.; J. Antibiot. (Tokyo) 38, 224 (1985) Abstract
Novel antitumor antibiotics, CI-940 (PD 114,720) and PD 114,721. Taxonomy, fermentation and biological activity: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 38, 460 (1985) Abstract
In vivo and in vitro anticancer activity of the structurally novel and highly potent antibiotic CI-940 and its hydroxy analog (PD 114,721): B.J. Roberts, et al.; Cancer Chemother. Pharmacol. 16, 95 (1986) Abstract
Leptomycin B is an inhibitor of nuclear export: inhibition of nucleo-cytoplasmic translocation of the human immunodeficiency virus type 1 (HIV-1) Rev protein and Rev-dependent mRNA: B. Wolff, et al.; Chem. Biol. 4, 139 (1997) Abstract; Full Text

Further Categories Containing This Product:

Antibiotics - Antifungal

ALX-380-231

Revised 14-Mar-08

Kazusamycin B
SYNONYMS	Hydroxyleptomycin A Antibiotic CL 1957E PD 124,895
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antitumor Antibiotics

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-231-MC01		0.1 mg	460.00 USD

Product Specification

FORMULA:	C₃₂H₄₆O₇
MW:	542.7
CAS NUMBER:	107140-30-7
RTECS:	OA0551000
SOURCE/HOST:	Isolated from Streptomyces sp. MST-AS4898.
PURITY:	≥95% (HPLC)
APPEARANCE:	Colorless film.
SOLUBILITY:	Soluble in 100% ethanol (recommended) or methanol. Unstable in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Shows potent antitumor activity in vitro and in vivo against several tumor cell lines, including L1210 and P388 leukemia cells. Has antibacterial and antifungal activities. Inhibitor of nuclear export.

Product Specific Literature References

PD 124,895 and PD 124,966, two new antitumor antibiotics: T.R. Hurley, et al.; J. Antibiot. (Tokyo) 39, 1651 (1986) Abstract
Kazusamycin B, a novel antitumor antibiotic: K. Funaishi, et al.; J. Antibiot. (Tokyo) 40, 778 (1987) Abstract
Antitumor effect of kazusamycin B on experimental tumors: E. Yoshida, et al.; J. Antibiot. (Tokyo) 40, 1596 (1987) Abstract
The effect of kazusamycin B on the cell cycle and morphology of cultured L1210 cells: K. Takamiya, et al.; J. Antibiot. (Tokyo) 41, 1854 (1988) Abstract
Leptomycin B is an inhibitor of nuclear export: inhibition of nucleo-cytoplasmic translocation of the human immunodeficiency virus type 1 (HIV-1) Rev protein and Rev-dependent mRNA: B. Wolff, et al.; Chem. Biol. 4, 139 (1997) Abstract; Full Text

Further Categories Containing This Product:

Antibiotics - Antifungal

ALX-380-066

Revised 07-Apr-08

Kendomycin
SYNONYMS	(-)-TAN 2162
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antitumor Antibiotics

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-066-C100		100 µg	95.00 USD
ALX-380-066-C500		500 µg	370.00 USD

Product Specification

FORMULA:	C₂₉H₄₂O₆
MW:	486.6
CAS NUMBER:	59785-91-0
SOURCE/HOST:	Isolated from Streptomyces violaceoruber.
PURITY:	≥98%
APPEARANCE:	Yellow powder.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC.

Product Description

Potent endothelin receptor antagonist. Anti-osteoporotic compound. Shows remarkable antibacterial and cytotoxic activity. Mediates its cytotoxic effects, at least in part, through proteasome inhibition.

Product Specific Literature References

2000 Structure and biosynthesis of kendomycin, a carboxylic ansa-compound from Streptomyces: A.Zeeck & H.B. Bode; J. Chem. Soc. Perkin Trans. 323 (2000)
Evidence for the mode of action of the highly cytotoxic Streptomyces polyketide kendomycin: Y.A. Elnakady, et al.; Chembiochem. 8, 1261 (2007) Abstract

Further Categories Containing This Product:

Antibiotics - Other Signal Transduction Pathway Modulators • Endothelins [ETs] & Endothelin Receptors / Related Products • Antibiotics - Proteasome / Ubiquitin Modulators • Bone Metabolism Other Products

ALX-380-213

Revised 10-Dec-07

Kigamicin C
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antitumor Antibiotics

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-213-MC05		0.5 mg	320.00 USD

Product Specification

FORMULA:	C₄₁H₄₇NO₁₆
MW:	809.8
CAS NUMBER:	680571-51-1
SOURCE/HOST:	Isolated from Amycolatopsis sp. MST-AS4724.
PURITY:	≥97% (HPLC)
APPEARANCE:	Yellow powder.
SOLUBILITY:	Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Antitumor antibiotic. Inhibits the growth of Gram-positive bacteria including MRSA.

Product Specific Literature References

Kigamicins, novel antitumor antibiotics. I. Taxonomy, isolation, physico-chemical properties and biological activities: S. Kunimoto, et al.; J. Antibiot. (Tokyo) 56, 1004 (2003) Abstract
Kigamicins, novel antitumor antibiotics. II. Structure determination: S. Kunimoto, et al.; J. Antibiot. (Tokyo) 56, 1012 (2003) Abstract

ALX-350-245

Revised 07-Apr-08

Lactacystin (native)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Proteasome / Ubiquitin Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-245-MC01		0.1 mg	60.00 USD
ALX-350-245-MC05		0.5 mg	250.00 USD
ALX-350-245-M001		1 mg	445.00 USD

Product Specification

FORMULA:	C₁₅H₂₄N₂O₇S
MW:	376.4
CAS NUMBER:	133343-34-7
SOURCE/HOST:	Isolated from Streptomyces sp.
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING:	Protect from light.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation by inhibiting IκB degradation. Inhibits the ubiquitin proteasome pathway in cell culture (IC₅₀=10µM). Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Product Specific Literature References

Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura, et al.; J. Antibiot. 44, 116 (1991) Abstract
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany, et al.; PNAS 91, 3358 (1994) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajo-Ohmi, et al.; BBRC 217, 1070 (1995) Abstract
The neuritogenesis inducer lactacystin arrests cell cycle at both G0/G1 and G2 phases in neuro 2a cells: M. Katagiri, et al.; J. Antibiotics (Tokyo) 48, 344 (1995) Abstract
Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori, et al.; J. Biol. Chem. 270, 29447 (1995) Abstract; Full Text
Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu, et al.; J. Antibiotics (Tokyo) 48, 747 (1995) Abstract
Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka, et al.; BBRC 216, 291 (1995) Abstract
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny, et al.; BBRC 227, 564 (1996) Abstract
Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita, et al.; BBRC 224, 74 (1996) Abstract
Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee, et al.; J.Biol. Chem. 271, 25630 (1996) Abstract; Full Text
Lactacystin increases LDL receptor level on HepG2 cells: H. Miura, et al.; BBRC 227, 684 (1996) Abstract
Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami, et al.; Biochem. J. 317, 77 (1996) Abstract; Full Text
Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda, et al.; BBRC 219, 800 (1996) Abstract
Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu, et al.; J. Biol. Chem. 271, 22791 (1996) Abstract; Full Text
Accelerated degradation of PML-retinoic acid receptor alpha (PML-RARA) oncoprotein by all-trans-retinoic acid in acute promyelocytic leukemia: possible role of the proteasome pathway: H. Yoshida, et al.; Cancer Res. 56, 2945 (1996) Abstract
The proteasome inhibitor lactacystin induces apoptosis and sensitizes chemo- and radioresistant human chronic lymphocytic leukaemia lymphocytes to TNF-alpha-initiated apoptosis: J. Delic, et al.; Br. J. Cancer 77, 1103 (1998) Abstract
Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998), (Review) Abstract; Full Text
Proteasome inhibitors prevent the degradation of familial Alzheimer's disease-linked presenilin 1 and potentiate A beta 42 recovery from human cells: P. Marambaud, et al.; Mol. Med. 4, 147 (1998) Abstract
The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form: M.C. Mutomba & C.C. Wang; Mol. Biochem. Parasitol. 93, 11 (1998) 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
Proteasome inhibition by lactacystin in primary neuronal cells induces both potentially neuroprotective and pro-apoptotic transcriptional responses: a microarray analysis: E.H. Yew, et al.; J. Neurochem. 94, 943 (2005) Abstract

Further Categories Containing This Product:

Heat Shock Proteins Other Products • Antibiotics for Angiogenesis Research • Antibiotics - NF-kB Inhibitors • NF-kB Pathway Inhibitors • Antitumor Antibiotics • Proteasome / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors

ALX-350-260

Revised 11-Aug-08

Lactacystin (synthetic)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Proteasome / Ubiquitin Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-260-MC01		0.1 mg	95.00 USD
ALX-350-260-M001		1 mg	730.00 USD

Product Specification

FORMULA:	C₁₅H₂₄N₂O₇S
MW:	376.4
CAS NUMBER:	133343-34-7
SOURCE/HOST:	Synthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
ACTIVITY:	k_obs/[I]=4’000M^-1sec^-1 versus 20S:PA28 complex.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing aqueous solutions for more than one day.
HANDLING:	Protect from light. Avoid freeze/thaw cycles.
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasom