ALEXIS Biochemicals: Bafilomycin A1

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Antibiotics - ATPase Inhibitors

Antibiotics - NF-kB Inhibitors

Antibiotics - Protein Kinase Inhibitors

Staurosporine / Related Products

Antibiotics - Other Signal Transduction Pathway Modulators

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-270-111

Revised 31-Jul-08

Patulin
SYNONYMS	4-Hydroxy-4H-furo[3,2-c]pyran-2(6H)-one Clairformin Clavacin Clavatin Claviformin Leucopin Mycoin C3 Mycosin Penicidin Terinin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-111-M001		1 mg	20.00 USD
ALX-270-111-M005		5 mg	80.00 USD
ALX-270-111-M025		25 mg	320.00 USD

Product Specification

FORMULA:	C₇H₆O₄
MW:	154.1
CAS NUMBER:	149-29-1
MERCK INDEX:	14: 7053
RTECS:	LV2625000
SOURCE/HOST:	Isolated from Penicillium expansum.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water, 100% ethanol, ethyl acetate or DMSO (10mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	MAY BE CARCINOGENIC. TOXIC.

Product Description

Inhibitor of protein farnesylation in a cell free assay. Inhibits incorporation of tritiated mevalonate into proteins in whole cells. Mycotoxin with anti-bacterial, potassium uptake inhibitory and possibly carcinogenic activities. Known contaminant of spoiled apples.

Product Specific Literature References

M. Birkinshaw, et al.; Lancet 245, 625 (1943)
J. Kahn; J. Pharmacol. Exp. Ther. 121, 234 (1957)
IARC Monographs 10, 205 (1976)
Chronology of patulin-induced alterations in membrane function of cultured renal cells, LLC-PK: R.T. Riley, et al.; Toxicol. Appl. Pharmacol. 102, 128 (1990) Abstract
Inhibition of protein prenylation by patulin: S. Miura, et al.; FEBS Lett. 318, 88 (1993) Abstract
Aneuploidogenic and clastogenic potential of the mycotoxins citrinin and patulin: E. Pfeiffer, et al.; Carcinogenesis 19, 1313 (1998) Abstract
Hplc detection of patulin in apple juice with GC/MS confirmation of patulin identity: J.A. Roach, et al.; Adv. Exp. Med. Biol. 504, 135 (2002), Review Abstract

Further Categories Containing This Product:

Mycotoxins • Farnesylation / Isoprenylation Reagents

ALX-350-029

Revised 07-Oct-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.

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. Neurotoxic.

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-350-106

Revised 29-Nov-07

Ampullosporin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-106-M001		1 mg	50.00 USD

Product Specification

SEQUENCE:	Ac-Trp-Ala-Aib-Aib-Leu-Aib-Gln-Aib-Aib-Aib-Gln-Leu-Aib-Gln-Leucinol
FORMULA:	C₇₇H₁₂₇N₁₉O₁₉
MW:	1623.0
SOURCE/HOST:	Antibiotic isolated from Sepedonium ampullosporum.
PURITY:	≥98% (HPLC)
SOLUBILITY:	Soluble in alcohols, chloroform or dichloromethane. Insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	TOXIC.

Product Description

Peptaibol-type polypeptide. Induces pigment formation by the fungus Phoma destructiva, causes hypothermia in mice, displays neuroleptic activity in rats and forms instable pores in artificial bilayer membranes.

Product Specific Literature References

Ampullosporin, a new peptaibol-type antibiotic from Sepedonium ampullosporum HKI-0053 with neuroleptic activity in mice: M. Ritzau, et al.; J. Antibiot. 50, 722 (1997) Abstract
Differences in ion permeability of an artificial bilayer membrane caused by ampullosporin and bergofungin, new 15-membered peptaibol-type antibiotics: P. Grigoriev, et al.; Bioelectrochemistry 44, 155 (1997)
Differences in ion-channel formation by ampullosporins B, C, D and semisynthetic desacetyltryptophanyl ampullosporin A: P. Grigoriev, et al.; Bioelectrochemistry 57, 119 (2002) Abstract
Synthesis and biological evaluation of analogues of the peptaibol ampullosporin A: H.H. Nguyen, et al.; J. Med. Chem. 45, 2781 (2002) Abstract
Crystal structure and conformational analysis of ampullosporin A: M. Kronen, et al.; J. Pept. Sci. 9, 729 (2003) Abstract
Membrane association and activity of 15/16-membered peptide antibiotics: zervamicin IIB, ampullosporin A and antiamoebin I: T.N. Kropacheva, et al.; Biochim. Biophys. Acta 1715, 6 (2005) Abstract
Transcriptional response to the neuroleptic-like compound Ampullosporin A in the rat ketamine model: H. Krugel, et al.; J. Neurochem. 97, Suppl. 1, 74 (2006) Abstract

Further Categories Containing This Product:

Peptides • Alzheimer Research Other Products • Ion Channels & Transporters Other Products

ALX-350-233

Revised 30-Oct-07

Gramicidin A (high purity)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-233-M001		1 mg	25.00 USD
ALX-350-233-M005		5 mg	70.00 USD

Product Specification

SEQUENCE:	HCO-Val-Gly-Ala-D-Leu-Ala-D-Val-Val-D-Val-Trp-D-Leu-Trp-D-Leu-Trp-D-Leu-Trp-NHCH₂CH₂OH
FORMULA:	C₉₉H₁₄₀N₂₀O₁₇
MW:	1882.3
CAS NUMBER:	11029-61-01
MERCK INDEX:	14: 4532
SOURCE/HOST:	Isolated from Bacillus brevis.
PURITY:	≥95%
APPEARANCE:	Off-white solid.
PURITY DETAIL:	Contaminants: gB and gC isomers: <1% (HPLC).
SOLUBILITY:	Soluble in DMSO, in the lower alcohols or in acetic acid.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Naturally occurring ion channel forming pentadecapeptide. Causes K⁺/H⁺-exchange in mitochondria in a non-voltage dependent manner.

Product Specific Literature References

Purification of gramicidin A: C.J. Stankovic, et al.; Anal. Biochem. 184, 100 (1990) Abstract
The permeation properties of small organic cations in gramicidin A channels: S.A. Seoh & D. Busath; Biophys. J. 64, 1017 (1993) Abstract
Palmitoylation-induced conformational changes of specific side chains in the gramicidin transmembrane channel: R.E. Koeppe, 2nd, et al.; Biochemistry 34, 9299 (1995) Abstract
Two mechanisms of H+/OH- transport across phospholipid vesicular membrane facilitated by gramicidin A: B.S. Prabhananda & M.H. Kombrabail; Biophys. J. 71, 3091 (1996) Abstract
Effects of gramicidin-A on the adsorption of phospholipids to the air-water interface: S.C. Biswas, et al.; Biochim. Biophys. Acta 1717, 41 (2005) Abstract

Further Categories Containing This Product:

Peptides • K+ Channels Other Products

ALX-350-241

Revised 07-Dec-07

Manumycin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-241-M001		1 mg	58.00 USD
ALX-350-241-M005		5 mg	170.00 USD
ALX-350-241-M010		10 mg	260.00 USD

Product Specification

FORMULA:	C₃₁H₃₈N₂O₇
MW:	550.7
CAS NUMBER:	52665-74-4
SOURCE/HOST:	Isolated from Streptomyces parvulus.
PURITY:	≥96% (HPLC)
APPEARANCE:	Yellow to brown powder.
SOLUBILITY:	Soluble in methanol or DMSO; insoluble in water.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
IDENTITY:	Determined by ¹H-NMR.

Product Description

Potent, selective and competitive inhibitor of Ras farnesyltransferase. Does not affect geranylgeranyltransferase. Inhibition is competitive with respect to farnesyl pyrophosphate and non-competitive with respect to Ras. Inhibits neutral sphingomyelinase.

Product Specific Literature References

Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994) Abstract
Manumycin inhibits ras signal transduction pathway and induces apoptosis in COLO320-DM human colon tumour cells: A. Di Paolo, et al.; Br. J. Cancer 82, 905 (2000) Abstract
Manumycin A and its analogues are irreversible inhibitors of neutral sphingomyelinase: C. Arenz, et al.; ChemBioChem 2, 141 (2001) Abstract
Enhancement of manumycin A-induced apoptosis by methoxyamine in myeloid leukemia cells: M. She, et al.; Leukemia 19, 595 (2005) Abstract
Binding of manumycin A inhibits IkappaB kinase beta activity: M. Bernier, et al.; J. Biol. Chem. 281, 2551 (2006) Abstract

Further Categories Containing This Product:

Farnesylation / Isoprenylation Reagents • Ceramides / Cerebrosides / Sphingolipids / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors

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)