ALEXIS Biochemicals: Doxycycline . hyclate

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ALX-350-029

Revised 05-Apr-08

Herbimycin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-029-C100		100 µg	110.00 USD
ALX-350-029-M001		1 mg	560.00 USD

Product Specification

FORMULA:	C₃₀H₄₂N₂O₉
MW:	574.7
CAS NUMBER:	70563-58-5
RTECS:	LX8930000
SOURCE/HOST:	Isolated from Streptomyces sp.
PURITY:	≥97%
APPEARANCE:	Yellow powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.
HAZARD:	NEUROTOXIN.

Product Description

Antibiotic. Cell permeable tyrosine kinase inhibitor. Inhibitor of HSP90, NF-κB activation and angiogenesis. Increases the sensitivity of certain cancer cells to chemotherapeutic agents. Blocks mitotic activity.

Product Specific Literature References

Herbimycin, a new antibiotic produced by a strain of Streptomyces: S. Omura, et al.; J. Antibiot. (Tokyo) 32, 255 (1979) Abstract
A new activity of herbimycin A: inhibition of angiogenesis: T. Yamashita, et al.; J. Antibiot. (Tokyo) 42, 1015 (1989) Abstract
Stimulation by Bt2cAMP of epidermal mucous metaplasia in retinol- pretreated chick embryonic cultured skin, and its inhibition by herbimycin A, an inhibitor for protein-tyrosine kinase: A. Obinata, et al.; Exp. Cell. Res. 193, 36 (1991) Abstract
IgE-induced tyrosine phosphorylation of phospholipase C-gamma 1 in rat basophilic leukemia cells: D.J. Park, et al.; J. Biol. Chem. 266, 24237 (1991) Abstract; Full Text
Bacterial lipopolysaccharide stimulates protein tyrosine phosphorylation in macrophages: S.L. Weinstein, et al.; PNAS 88, 4148 (1991) Abstract
Inhibition of interleukin 3 and granulocyte-macrophage colony- stimulating factor stimulated increase of active ras.GTP by herbimycin A, a specific inhibitor of tyrosine kinases: T. Satoh, et al.; J. Biol. Chem. 267, 2537 (1992) Abstract; Full Text
New insight into oncoprotein-targeted antitumor effect: herbimycin A as an antagonist of protein tyrosine kinase against Ph1-positive leukemia cells: M. Okabe and M. Uehara; Leuk. Lymphoma 12, 41 (1993) Abstract
Prevention of anti-CD3 monoclonal antibody-induced thymic apoptosis by protein tyrosine kinase inhibitors: K. Migita, et al.; J. Immunol. 153, 3457 (1994) Abstract
Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation: L. Whitesell, et al.; PNAS 91, 8324 (1994) Abstract; Full Text
Inhibition of PDGF-induced phospholipase D but not phospholipase C activation by herbimycin A: B.Y. Kim; BBRC 212, 1061 (1995) Abstract
Controlling the vasculature: angiogenesis, anti-angiogenesis and vascular targeting of gene therapy: T.-P.D. Fan, et al.; TIPS 16, 57 (1995), (Review) Abstract
Herbimycin A enhances apoptotic effect of chemotherapeutic drugs on K562 cells: H. Ren, et al.; Chin. Med. J. (Engl.) 111, 678 (1998) Abstract
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002) Abstract; Full Text
Geldanamycin and herbimycin A induce apoptotic killing of B chronic lymphocytic leukemia cells and augment the cells’ sensitivity to cytotoxic drugs: D.T. Jones, et al.; Blood 103, 1855 (2004) Abstract; Full Text
Herbimycin A abrogates nuclear factor-kappaB activation by interacting preferentially with the IkappaB kinase beta subunit: S. Ogino, et al.; Mol. Pharmacol. 65, 1344 (2004) Abstract; Full Text
Herbimycin A suppresses mitotic activity and egg production of female Schistosoma mansoni: J. Knobloch, et al.; Int. J. Parasitol. 36, 1261 (2006) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Neurotoxins • Phospholipase D/Related Products • Antibiotics for Angiogenesis Research • HSP90/HtpG/Related Products

ALX-350-119

Revised 20-Feb-08

Fumagillin
SYNONYMS	Fumidil B Fumadil B TNP-470
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics for Angiogenesis Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-119-MC05		0.5 mg	65.00 USD
ALX-350-119-M001		1 mg	105.00 USD

Product Specification

FORMULA:	C₂₆H₃₄O₇
MW:	458.6
CAS NUMBER:	23110-15-8
MERCK INDEX:	14: 4286
SOURCE/HOST:	Isolated from Aspergillus fumigatus.
PURITY:	≥95%
APPEARANCE:	Light yellow solid
SOLUBILITY:	Soluble in chloroform or diluted aqueous bases. Slightly soluble in methanol and other alcoholic solvents. Insoluble in water.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Unstable in aqueous solutions with pH >9.0 or pH <5.0.
HANDLING:	Packaged under inert gas. Protect from light.
HAZARD:	HARMFUL.

Product Description

Inhibitor of angiogenesis and endothelial cell proliferation. Specific inhibitor of methionine aminopeptidase type II (MetAP-II). Antineoplastic. Anti-infective.

Product Specific Literature References

Fumagillin (H-3), a new antibiotic with amebicidal properties: C.M. Mc, et al.; Science 113, 202 (1951) Abstract
Synthetic analogues of fumagillin that inhibit angiogenesis and suppress tumour growth: D. Ingber, et al.; Nature 348, 555 (1990) Abstract
The anti-angiogenic agent fumagillin covalently modifies a conserved active-site histidine in the Escherichia coli methionine aminopeptidase: W.T. Lowther, et al.; PNAS 95, 12153 (1998) Abstract; Full Text
Molecular recognition of angiogenesis inhibitors fumagillin and ovalicin by methionine aminopeptidase 2: E.C. Griffith, et al.; PNAS 95, 15183 (1998) Abstract
Fumagillin treatment of intestinal microsporidiosis: J.M. Molina, et al.; N. Engl. J. Med. 346, 1963 (2002) Abstract
Whirling disease of salmonid fish: life cycle, biology, and disease: M.A. Gilbert & W.O. Granath, Jr.; J. Parasitol. 89, 658 (2003) Abstract
Fumagillin treatment of hepatocellular carcinoma in rats: an in vivo study of antiangiogenesis: I.S. Sheen, et al.; World J. Gastroenterol. 11, 771 (2005) Abstract
Fumagillin: an anti-infective as a parent molecule for novel angiogenesis inhibitors: B. Lefkove, et al.; Expert Rev. Anti Infect. Ther. 5, 573 (2007), Review Abstract
FGFR1/PI3K/AKT signaling pathway is a novel target for antiangiogenic effects of the cancer drug fumagillin (TNP-470): G.J. Chen, et al.; J. Cell Biochem. 101, 1492 (2007) Abstract

Further Categories Containing This Product:

Aminopeptidases/Related Products • Fibroblast Growth Factors [FGFs] & Receptors/Related Products • Natural Products - Other Anti-infective Agents • Antitumor Antibiotics • Antitumor Agents (Anti-proliferative)

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 • Proteasome/Related Products • Antibiotics for Angiogenesis Research • NF-kB Pathway Inhibitors • Antitumor Antibiotics • Antibiotics - NF-kB Inhibitors • 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 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, 113 (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. Antibiot. (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 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
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
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
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
The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form: M.C. Mutomba, et al.; Mol. Biochem. Parasitol. 93, 11 (1998) Abstract
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
Proteasome inhibitors MG132 and lactacystin hyperphosphorylate HSF1 and induce hsp70 and hsp27 expression: D. Kim, et al.; BBRC 254, 264 (1999) Abstract
Proteasome inhibitors induce mitochondria-independent apoptosis in human glioma cells: H. Kitagawa, et al.; FEBS Lett. 443, 181 (1999) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis and activates caspase-3 in cultured cerebellar granule cells: L.A. Pasquini, et al.; J. Neurosci. Res. 59, 601 (2000) Abstract
Proteasome inhibitors induce cytochrome c-caspase-3-like protease- mediated apoptosis in cultured cortical neurons: J.H. Qiu, et al.; J. Neurosci. 20, 259 (2000) Abstract
Lactacystin activates FLICE (caspase 8) protease and induces apoptosis in Fas-resistant adult T-cell leukemia cell lines: Y. Yamada, et al.; Eur. J. Haematol. 64, 315 (2000) 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:

ALX-380-062

Revised 03-Apr-08

Cytochalasin E
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics for Cytoskeletal Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-062-M001		1 mg	40.00 USD
ALX-380-062-M005		5 mg	160.00 USD

Product Specification

FORMULA:	C₂₈H₃₃NO₇
MW:	495.6
CAS NUMBER:	36011-19-5
MERCK INDEX:	14: 2790
SOURCE/HOST:	Isolated from Aspergillus clavatus.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Antibiotic. Inhibits angiogenesis and tumor growth. Depolymerizes actin filaments.

Product Specific Literature References

Inhibition of actin polymerization in blood platelets by cytochalasins: J.E. Fox & D.R. Phillips; Nature 292, 650 (1981) Abstract
Cytochalasin-E-Resistant Mutants of Coprinus cinereus: Isolation and Genetic, Biochemical, and Cytological Analyses: M. Tsukamoto, et al.; Fungal Genet. Biol. 20, 52 (1996) Abstract
Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth: T. Udagawa, et al.; J. Pharmacol. Exp. Ther. 294, 421 (2000) Abstract
Depolymerization of actin filament by cytochalasin E induces interleukin-8 production and up-regulates CD54 in the HeLa epithelial cell line: N. Ikewaki, et al.; Microbiol. Immunol. 47, 775 (2003) Abstract

Further Categories Containing This Product:

Interleukins Other Products • Actin/Related Products • Antibiotics for Angiogenesis Research • Antitumor Antibiotics • Microtubule Modulators • Alkaloids

ALX-380-092

Revised 03-Jul-08

Radicicol
SYNONYMS	Monorden 1aS-(1aR,2Z,4E,14,15aR*)]-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Antifungal

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-092-M001		1 mg	75.00 USD
ALX-380-092-M005		5 mg	295.00 USD

Product Specification

FORMULA:	C₁₈H₁₇ClO₆
MW:	364.8
CAS NUMBER:	12772-57-5
MERCK INDEX:	14: 6253
RTECS:	RR1105000
SOURCE/HOST:	Isolated from Humicola fuscoatra.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to light yellow powder.
SOLUBILITY:	Soluble in DMSO, methanol or acetone.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	MAY BE CARCINOGENIC. HARMFUL.

Product Description

Antifungal macrocyclic lactone antibiotic with antimalarial activity. Potent inhibitor of HSP90. Binds more strongly to HSP90 (nanomolar affinity) than to Grp94. Also binds to yeast HSP90, E. coli HtpG and TRAP-1. Non-competitive inhibitor of ATP citrate lyase. Anti-angiogenic. Specifically inhibits the interaction between HIF-1α/Arnt heterodimer and the hypoxia-responsive element (HRE), reducing VEGF expression. Protein tyrosine kinase inhibitor, e.g. p60^v-src(IC₅₀=0.27nM). Inhibitor of cyclooxygenase-2 (COX-2) expression (IC₅₀=27nM) without affecting COX-1 expression in LPS-stimulated macrophages. Induces the differentiation of HL-60 cells into macrophages, blocking cell cycle at G1 and G2. Suppressor of NIH 3T3 cell transformation by diverse oncogenes such as mos, ras and src in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Inhibitor of AP-1-, NF-κB- and serum response factor (SRF)-mediated transcription (e.g. expression of iNOS). Represses the transcriptional function of the estrogen receptor. Inhibits archeal growth and DNA topoisomerase VI (a Topo IIB family topoisomerase). Blocks replication of negative-strand RNA viruses.

Product Specific Literature References

Potent and specific inhibition of p60v-src protein kinase both in vivo and in vitro by radicicol: H.J. Kwon, et al.; Cancer Res. 52, 6926 (1992) Abstract
Radicicol, a microbial cell differentiation modulator, inhibits in vivo angiogenesis: T. Oikawa, et al.; Eur. J. Pharmacol. 241, 221 (1993) Abstract
Radicicol, a protein tyrosine kinase inhibitor, suppresses the expression of mitogen-inducible cyclooxygenase in macrophages stimulated with lipopolysaccharide and in experimental glomerulonephritis: P. Chanmugam, et al.; J. Biol. Chem. 270, 5418 (1995) Abstract; Full Text
Suppression of RAS and MOS transformation by radicicol: J.F. Zhao, et al.; Oncogene 11, 161 (1995) Abstract
Induction of differentiation of HL-60 cells by the anti-fungal antibiotic, radicicol: Y. Shimada, et al.; J. Antibiot. 48, 824 (1995) Abstract
Radicicol inhibits tyrosine phosphorylation of the mitotic Src substrate Sam68 and retards subsequent exit from mitosis of Src-transformed cells: I. Pillay, et al.; Cell Growth Differ. 7, 1487 (1996) Abstract
Radicicol leads to selective depletion of Raf kinase and disrupts K-Ras-activated aberrant signaling pathway: S. Soga, et al.; J. Biol. Chem. 273, 822 (1998) Abstract; Full Text
Antimalarial activity of radicicol, heptelidic acid and other fungal metabolites: Y. Tanaka, et al.; J. Antibiot. 51, 153 (1998) Abstract
Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol: S.V. Sharma, et al.; Oncogene 16, 2369 (1998) Abstract
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin: S.M. Roe, et al.; J. Med. Chem. 42, 260 (1999) Abstract
T.W. Schulte, et al.; Mol. Endocrinol. 13, 1435 (1999) Abstract; Full Text
Radicicol suppresses expression of inducible nitric-oxide synthase by blocking p38 kinase and nuclear factor-kappaB/Rel in lipopolysaccharide-stimulated macrophages: Y.J. Jeon, et al.; J. Pharmacol. Exp. Ther. 294, 548 (2000) Abstract; Full Text
Radicicol binds and inhibits mammalian ATP citrate lyase: S.W. Ki, et al.; J. Biol. Chem. 275, 39231 (2000) Abstract; Full Text
Radicicol suppresses transformation and restores tropomyosin-2 expression in both ras- and MEK-transformed cells without inhibiting the Raf/MEK/ERK signaling cascade: P.N. Kim, et al.; Cell Growth Differ. 12, 543 (2001) Abstract; Full Text
Radicicol-sensitive peptide binding to the N-terminal portion of GRP94: S. Vogen, et al.; J. Biol. Chem. 277, 40742 (2002) Abstract; Full Text
Reduction of hypoxia-induced transcription through the repression of hypoxia-inducible factor-1alpha/aryl hydrocarbon receptor nuclear translocator DNA binding by the 90-kDa heat-shock protein inhibitor radicicol: E. Hur, et al.; Mol. Pharmacol. 62, 975 (2002) Abstract; Full Text
Radicicol represses the transcriptional function of the estrogen receptor by suppressing the stabilization of the receptor by heat shock protein 90: M.O. Lee, et al.; Mol. Cell Endocrinol. 188, 47 (2002) Abstract
Development of radicicol analogues: S. Soga, et al.; Curr. Cancer Drug Targets 3, 359 (2003) Abstract
Heat shock protein 90 (Hsp90) chaperone complex inhibitor, radicicol, potentiated radiation-induced cell killing in a hormone-sensitive prostate cancer cell line through degradation of the androgen receptor: K. Harashima, et al.; Int. J. Radiat. Biol. 81, 63 (2005) Abstract
Inhibition of archaeal growth and DNA topoisomerase VI activities by the Hsp90 inhibitor radicicol: D. Gadelle, et al.; Nucleic Acid Res. 33, 2310 (2005) Abstract
Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site: M.K. Hadden, et al.; Curr. Top. Med. Chem. 6, 1173 (2006), Review Abstract
The topoisomerase II-Hsp90 complex: a new chemotherapeutic target?: C.R. Barker, et al.; Int. J. Cancer 118, 2685 (2006) Abstract
Structural basis for topoisomerase VI inhibition by the anti-Hsp90 drug radicicol: K.D. Corbett & J.M. Berger; Nucleic Acids Res. 34, 4269 (2006) Abstract
Chemistry and biology of resorcylic acid lactones: N. Winssinger & S. Barluenga; Chem. Commun. (Camb.) 22 (2007) Abstract
Antiviral activity and RNA polymerase degradation following Hsp90 inhibition in a range of negative strand viruses: J.H. Connor, et al.; Virology 362, 109 (2007) Abstract

Further Categories Containing This Product:

NF-kB Pathway Inhibitors • Cell Cycle Blockers & Inhibitors/Related Products • Tyrosine Kinase Inhibitors • Estrogen & Estrogen Receptors/Related Products • Antibiotics - Nitric Oxide Pathway Modulators • Antitumor Agents (Hormone-related) • Malaria/Related Products • Antibiotics - Antimalarial • Antibiotics - Protein Kinase Inhibitors • Antibiotics - NF-kB Inhibitors • Antibiotics for Angiogenesis Research • Antibiotics for Cell Cycle Research • HSP90/HtpG/Related Products •