ALEXIS Biochemicals: WP631 . dimethanesulfonate

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ALX-380-047

Revised 20-Feb-08

Tunicamycin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Apoptosis Inducers & Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-047-M010		10 mg	82.00 USD
ALX-380-047-M050		50 mg	350.00 USD

Product Specification

CAS NUMBER:	11089-65-9
MERCK INDEX:	14: 9819
RTECS:	YO7980200
SOURCE/HOST:	Isolated from Streptomyces lysosuperficus.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
PURITY DETAIL:	Mixture of tunicamycin A, B, C and D.
SOLUBILITY:	Soluble in methanol or DMSO (50mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	VERY TOXIC.

Product Description

Nucleoside antibiotic that blocks the formation of protein N-glycosidic linkages by inhibiting the transfer of N-acetylglucosamine 1-phosphate to dolichol monophosphate. Induces ER-stress following the inhibition of N-linked glycosylation.

Product Specific Literature References

Isolation and structures of components of Tunicamycin: T. Ito, et al.; Agric. Biol. Chem. 44, 695 (1980)
Separation of tunicamycin homologues by reversed-phase high-performance liquid chromatography: W.C. Mahoney & D. Duksin; J. Chromatogr. 198, 506 (1980) Abstract
Relationship of the structure and biological activity of the natural homologues of tunicamycin: D. Duksin & W.C. Mahoney; J. Biol. Chem. 257, 3105 (1982) Abstract; Full Text
Tunicamycin inhibits the expression of functional thrombin receptors on human T-lymphoblastoid cells: A. Tordai, et al.; BBRC 206, 857 (1995) Abstract
Tunicamycin, a new antibiotic. I. Isolation and characterization of tunicamycin: A. Takatsuki, et al.; J. Antibiot. (Tokyo) 24, 215 (1971) Abstract
Tunicamycin inhibits NMDA and AMPA receptor responses independently of N-glycosylation: K. Maruo, et al.; Brain Res. 977, 294 (2003) Abstract
Tunicamycin enhances tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in human prostate cancer cells: T. Shiraishi, et al.; Cancer Res. 65, 6364 (2005) Abstract
Novel potential of tunicamycin as an activator of the aryl hydrocarbon receptor -- dioxin responsive element signaling pathway: K. Horikawa, et al.; FEBS Lett. 580, 3721 (2006) Abstract
Tunicamycin sensitizes human melanoma cells to tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis by up-regulation of TRAIL-R2 via the unfolded protein response: C.C. Jiang, et al.; Cancer Res. 67, 5880 (2007) Abstract
Glycosylation modulates TRAIL-R1/death receptor 4 protein: different regulations of two pro-apoptotic receptors for TRAIL by tunicamycin: T. Yoshida, et al.; Oncol. Rep. 18, 1239 (2007) Abstract

Further Categories Containing This Product:

Endoplasmatic Reticulum Stress • Autophagy Other Products

ALX-380-222

Revised 19-Aug-08

UCN-01
SYNONYMS	7-Hydroxystaurosporine Staurosporine, 7-Hydroxy-
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Staurosporine / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-222-MC25		0.25 mg	85.00 USD
ALX-380-222-M001		1 mg	265.00 USD

Product Specification

FORMULA:	C₂₈H₂₆N₄O₄
MW:	482.5
CAS NUMBER:	112953-11-4
RTECS:	KC6600010
SOURCE/HOST:	Isolated from Streptomyces sp. MST-AS5345.
PURITY:	≥98% (HPLC)
APPEARANCE:	Light tan to light yellow solid.
SOLUBILITY:	Soluble in methanol, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibitor of protein kinase C (PKC) and cyclin-dependent kinases (CDKs) resulting in accumulation of cells in the G1 phase and induction of apoptosis. Enhances the cytotoxicity of other anticancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by these agents.

Product Specific Literature References

[1] UCN-01, a selective inhibitor of protein kinase C from Streptomyces: I. Takahashi, et al.; J. Antibiot. (Tokyo) 40, 1782 (1987) Abstract
[2] UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract
[3] UCN-01, 7-hydroxyl-staurosporine, inhibits kinase activity of cyclin-dependent kinases and reduces the phosphorylation of the retinoblastoma susceptibility gene product in A549 human lung cancer cell line: K. Kawakami, et al.; BBRC 219, 778 (1996) Abstract
[4] UCN-01 (7-hydroxystaurosporine) and other indolocarbazole compounds: a new generation of anti-cancer agents for the new century?: S. Akinaga, et al.; Anticancer Drug Des. 15, 43 (2000) Abstract
[5] UCN-01-induced cell cycle arrest requires the transcriptional induction of p21(waf1/cip1) by activation of mitogen-activated protein/extracellular signal-regulated kinase kinase/extracellular signal-regulated kinase pathway: M.M. Facchinetti, et al.; Cancer Res. 64, 3629 (2004) Abstract; Full Text

General Information

BACKGROUND/TECHNICAL INFORMATION

Note: Some interconversion of UCN-01 to UCN-02 may occur under acidic HPLC conditions (see [2]).

Further Categories Containing This Product:

Antibiotics - Apoptosis Inducers & Inhibitors • PKC Inhibitors • Antibiotics - Protein Kinase Inhibitors • CDK & Cyclin Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products • Antibiotics for Cell Cycle Research • Antitumor Antibiotics • Alkaloids

ALX-380-206

Revised 19-Aug-08

UCN-02
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Staurosporine / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-206-MC25		0.25 mg	85.00 USD
ALX-380-206-M001		1 mg	265.00 USD

Product Specification

FORMULA:	C₂₈H₂₆N₄O₄
MW:	482.5
CAS NUMBER:	121569-61-7
RTECS:	KC6600000
SOURCE/HOST:	Isolated from Streptomyces sp. MST-AS5345.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to pale yellow solid.
SOLUBILITY:	Soluble in ethyl acetate, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibitor of protein kinase C (PKC) and protein kinase A (PKA). Although less selective than its isomer UCN-01 (Prod. No. ALX-380-222), UCN-02 exhibits comparable activity and probably acts by similar mechanisms.

Product Specific Literature References

[1] UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract

General Information

BACKGROUND/TECHNICAL INFORMATION

Note: Some interconversion of UCN-02 to UCN-01 may occur under acidic HPLC conditions (see [1]).

Further Categories Containing This Product:

Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Antibiotics • PKC Inhibitors • Antibiotics - Protein Kinase Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products • CDK & Cyclin Inhibitors • Antibiotics for Cell Cycle Research • Alkaloids

ALX-450-012

Revised 24-Oct-07

Valinomycin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Ionophores

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-450-012-M005		5 mg	20.00 USD
ALX-450-012-M025		25 mg	60.00 USD

Product Specification

FORMULA:	C₅₄H₉₀N₆O₁₈
MW:	1111.4
CAS NUMBER:	2001-95-8
MERCK INDEX:	14: 9910
SOURCE/HOST:	Isolated from Streptomyces fulvissimus.
PURITY:	≥90%
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in acetic acid, chloroform, DMSO or ether.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	TOXIC.

Product Description

Potassium ionophore. Useful reagent for the measurement of K+ ions by electrode-based systems. Induces apoptosis in several cell lines.

Product Specific Literature References

Opposing interactions of ionophores (valinomycin and monensin) on calcium ion uptake in rat retinal preparations: J.B. Lombardini; Neurochem. Res. 10, 77 (1985) Abstract
Valinomycin-based K+ selective microelectrodes with low electrical membrane resistance: D. Ammann, et al.; Neurosci. Lett. 74, 221 (1987) Abstract
Alternative pathways of apoptosis induced by methylprednisolone and valinomycin analyzed by flow cytometry: C.L. Deckers, et al.; Exp. Cell. Res. 208, 362 (1993) Abstract
K+ ionophores inhibit nerve growth factor-induced neuronal differentiation in rat adrenal pheochromocytoma PC12 cells: H.Harada, et al.; Biochim. Biophys. Acta 1220, 310 (1994) Abstract
The effect of respiration on the permeability of the mitochondrial membrane to ions: S. Luvisetto, et al.; Biochim. Biophys. Acta 1186, 12 (1994) Abstract
Combination of the electrogenic ionophores, valinomycin and CCCP, can lead to non-electrogenic K+/H+ exchange on bilayer lipid membranes: V.N. Orlov, et al.; FEBS Lett. 345, 104 (1994) Abstract
Valinomycin induces apoptosis of ascites hepatoma cells (AH-130) in relation to mitochondrial membrane potential: Y. Inai, et al.; Cell Struct. Funct. 22, 555 (1997) Abstract
Induction of apoptosis by valinomycin: mitochondrial permeability transition causes intracellular acidification: I.J. Furlong, et al.; Cell Death Differ 5, 214 (1998) Abstract
Valinomycin-induced apoptosis of human NK cells is predominantly caspase independent: A. Paananen, et al.; Toxicology 212, 37 (2005) Abstract

Further Categories Containing This Product:

Antibiotics - Apoptosis Inducers & Inhibitors

ALX-380-064

Revised 08-Oct-08

WP631 . dihydrochloride
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Other Antibiotics - DNA Regulation / Transcription

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-064-C100		100 µg	60.00 USD
ALX-380-064-M001		1 mg	240.00 USD

Product Specification

FORMULA:	C₆₂H₆₄O₂₀N₂ . 2HCl
MW:	1157.2 . 73.0
PURITY:	≥95%
APPEARANCE:	Off-white to red powder.
SOLUBILITY:	Soluble in DMSO or dimethyl formamide.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Dissolve the compound in DMSO or dimethyl formamide at 20mg/ml, then add water (or 5% dextrose, PBS, etc.) to bring it to a final concentration of 1mg/ml (5% DMSO or dimethyl formamide).
HANDLING:	Keep cool and dry.
HAZARD:	HARMFUL. MAY BE CARCINOGENIC.

Product Description

Synthetic fluorescent bisintercalating anthracycline antibiotic with ultratight binding properties to DNA. Inhibits Sp1-initiated transcription at nanomolar concentrations. Appears to overcome MRP-mediated multidrug resistance. Induces apoptosis. Licenced product covered by US Patent 5,874,412. Sold with permission of Houston Pharmaceuticals, Inc.

Product Specific Literature References

Structure-based design of a new bisintercalating anthracycline antibiotic: J.B. Chaires, et al.; J. Med. Chem. 40, 261 (1997) Abstract
Structure of a DNA-bisdaunomycin complex: G.G. Hu, et al.; Biochemistry 36, 5940 (1997) Abstract
Bisanthracycline WP631 inhibits basal and Sp1-activated transcription initiation in vitro: B. Martin, et al.; Nucl. Acids Res. 27, 3402 (1999) Abstract; Full Text
Analysis of the effects of Daunorubicin and WP631 on transcription: J. Portugal, et al.; Curr. Med. Chem. 8, 1 (2001), (Review) Abstract
Identification of a critical Sp1 site within the endoglin promoter and its involvement in the transforming growth factor-beta stimulation: L.M. Botella, et al.; J. Biol. Chem. 276, 34486 (2001) Abstract; Full Text
Exploiting anthracycline scaffold for designing DNA-targeting agents: W. Priebe; Methods Enzymol. 340, 529 (2001) Abstract
Induction of G(2)/M arrest and inhibition of c-myc and p53 transcription by WP631 in Jurkat T lymphocytes: S. Villamarin, et al.; Biochem. Pharmacol. 63, 1251 (2002) Abstract
Evidence that activation of nuclear factor-kappaB is essential for the cytotoxic effects of doxorubicin and its analogues: K. Ashikawa, et al.; Biochem. Pharmacol. 67, 353 (2004) Abstract
Bis-anthracycline antibiotics inhibit human immunodeficiency virus type 1 transcription: O. Kutsch, et al.; Antimicrob. Agents. Chemother. 48, 1652 (2004) Abstract
Circumvention of the multidrug-resistance protein (MRP-1) by an antitumor drug through specific inhibition of gene transcription in breast tumor cells: S. Mansilla, et al.; Biochem. Pharmacol. 73, 934 (2007) Abstract

Further Categories Containing This Product:

MDR Inhibitors • Antibiotics - Apoptosis Inducers & Inhibitors • Sp Protein Family / Related Products • DNA Intercalators & Crosslinkers

ALX-380-074

Revised 12-Oct-07

WP631 . dimethanesulfonate
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Other Antibiotics - DNA Regulation / Transcription

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-074-C500		500 µg	150.00 USD

Product Specification

FORMULA:	C₆₂H₆₄N₂O₂₀ . 2CH₃SO₃
MW:	1157.2 . 191.2
PURITY:	≥95%
APPEARANCE:	Red powder.
SOLUBILITY:	Soluble in DMSO (10mg/ml) or water (1mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	HARMFUL. MAY BE CARCINOGENIC.

Product Description

Synthetic fluorescent bisintercalating anthracycline antibiotic with ultratight binding properties to DNA. Inhibits Sp1-initiated transcription at nanomolar concentrations. Appears to overcome multidrug resistance protein (MRP) mediated multidrug resistance (MDR). More water soluble than WP631 . dihydrochloride (Prod. No. ALX-380-064). Licenced product covered by US Patent 5,874,412. Sold with permission of Houston Pharmaceuticals, Inc.

Product Specific Literature References

Structure-based design of a new bisintercalating anthracycline antibiotic: J.B. Chaires, et al.; J. Med. Chem. 40, 261 (1997) Abstract
Structure of a DNA-bisdaunomycin complex: G.G. Hu, et al.; Biochemistry 36, 5940 (1997) Abstract
Binding of two novel bisdaunorubicins to DNA studied by NMR spectroscopy: H. Robinson, et al.; Biochemistry 36, 8663 (1997) Abstract
Ultratight DNA binding of a new bisintercalating anthracycline antibiotic: F. Leng, et al.; Biochemistry 37, 1743 (1998) Abstract
Drug-DNA interactions: J.B. Chaires; Curr. Opin. Struct. Biol. 8, 314 (1998) Abstract
Bisanthracycline WP631 inhibits basal and Sp1-activated transcription initiation in vitro: B. Martin, et al.; Nucleic Acids Res. 27, 3402 (1999) Abstract
Analysis of the effects of daunorubicin and WP631 on transcription: J. Portugal, et al.; Curr. Med. Chem. 8, 1 (2001) Abstract
Inhibition of basal and transforming growth factor-beta-induced stimulation of COL1A1 transcription by the DNA intercalators, mitoxantrone and WP631, in cultured human dermal fibroblasts: S. Gaidarova and S.A. Jimenez; J. Biol. Chem. 277, 38737 (2002) Abstract
Sequence selective binding of bis-daunorubicin WP631 to DNA: K.R. Fox, et al.; Eur. J. Biochem. 271, 3556 (2004) Abstract

Further Categories Containing This Product:

DNA Intercalators & Crosslinkers • MDR Inhibitors • Sp Protein Family / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors

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