ALEXIS Biochemicals: Reveromycin B

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Antibiotics - Apoptosis Inducers & Inhibitors

Antitumor Agents (Apoptosis Inducers)

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Apoptosis Inducers & Inhibitors Other Products

ALX-380-039

Revised 10-Dec-07

Oligomycin C
SYNONYMS	12-Deoxyoligomycin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Apoptosis Inducers & Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-039-M001		1 mg	330.00 USD

Product Specification

FORMULA:	C₄₅H₇₄O₁₀
MW:	775.1
CAS NUMBER:	11052-72-5
MERCK INDEX:	14: 6833
RTECS:	RK3335000
SOURCE/HOST:	Isolated from Streptomyces sp. MST-AS5339.
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
HAZARD:	MAY BE MUTAGENIC. HARMFUL.

Product Description

Minor component of the oligomycin complex. Macrolide antibiotic that inhibits membrane bound mitochondrial ATPase (F₁F₀), preventing phosphoryl group transfer. Induces apoptosis.

Product Specific Literature References

Production and isolation of the antibiotic, oligomycin: J. Visser, et al.; J. Biochem. Microbiol. Technol. Engr. 2, 31 (1960) Abstract
The BH3 domain is required for caspase-independent cell death induced by Bax and oligomycin: M.E. Fitch, et al.; Cell Death Differ. 7, 338 (2000) Abstract; Full Text
Oligomycin, inhibitor of the F0 part of H+-ATP-synthase, suppresses the TNF-induced apoptosis: L.A. Shchepina, et al.; Oncogene 21, 8149 (2002) Abstract; Full Text
Mitochondria-targeting drug oligomycin blocked P-glycoprotein activity and triggered apoptosis in doxorubicin-resistant HepG2 cells: Y.C. Li, et al.; Chemotherapy 50, 55 (2004) Abstract

Further Categories Containing This Product:

ALX-350-013

Revised 23-Oct-07

Olomoucine (high purity)
SYNONYMS	6-Benzylamino-2-(2-hydroxyethylamino)-9-methylpurine
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-013-M005		5 mg	65.00 USD
ALX-350-013-M025		25 mg	260.00 USD

Product Specification

FORMULA:	C₁₅H₁₈N₆O
MW:	298.4
CAS NUMBER:	101622-51-9
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in methanol or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Potent and very selective inhibitor of cdc2, CDK and other cyclin-related kinases by competing for the ATP-binding domain of the kinase. Inhibits CDK1/cyclin B (IC50=7µM), CDK2 (IC50=7µM) and CDK5/p35 (IC50=3µM). Also inhibits DNA synthesis in interleukin-2 stimulated T lymphocytes and triggers G1 arrest similar to that observed in interleukin-2 deprived cells. Can be used to synchronize cells in G1. Triggers apoptosis in target tumor cells in vitro and in vivo and in maturing cerebellar granule neurons.

Product Specific Literature References

Inhibition of cyclin-dependent kinases by purine analogues: J. Vesely, et al.; Eur. J. Biochem. 224, 771 (1994) Abstract
Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases: R.T. Abraham, et al.; Biol. Cell 83, 105 (1995) Abstract
Mitotic disassembly of the Golgi apparatus in vivo: T. Mistelli & G. Warren; J. Cell Sci. 108, 2715 (1995) Abstract
Chemical inhibitors of cyclin-dependent kinases: L. Meijer, et al.; Meth. Enzymol. 283, 113 (1997) Abstract
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem. 40, 408 (1997) Abstract
The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998) Abstract
Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) Abstract

Further Categories Containing This Product:

Cell Cycle Blockers & Inhibitors / Related Products • Antitumor Agents (Apoptosis Inducers)

ALX-270-396

Revised 07-Mar-08

Olomoucine II
SYNONYMS	6-(2-Hydroxybenzylamino)-2(R)-[[1-hydroxymethyl)propyl]amino]-9-isopropylpurine
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-396-M001		1 mg	42.00 USD
ALX-270-396-M005		5 mg	145.00 USD

Product Specification

FORMULA:	C₁₉H₂₆N₆O₂
MW:	370.5
CAS NUMBER:	500735-47-7
PURITY:	≥98%
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	Soluble in DMSO, dimethyl formamide or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Selective inhibitor of CDK1/cyclin B (IC₅₀=20nM). Potent cytotoxin in tumor cells: IC₅₀=5.3µM against MCF7 cells, IC₅₀=11.1µM against K562 cells, IC₅₀=3.0µM against CEM cells, IC₅₀=6.3µM against HOS cells, and IC₅₀=6.3µM against G361 cells.

Product Specific Literature References

Synthesis and biological activity of olomoucine II: V. Krystof, et al.; Bioorg. Med. Chem. Lett. 12, 3283 (2002) Abstract
Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor: V. Krystof, et al.; Cell Mol. Life Sci. 62, 1763 (2005) Abstract

Further Categories Containing This Product:

Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers)

ALX-270-379

Revised 04-Mar-05

Oxamflatin
SYNONYMS	(2E)-5-[3-(Phenylsulfonylamino)phenyl]pent-2-en-4-ynohydroxamic acid
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (Apoptosis Inducers)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-379-M001		1 mg	70.00 USD
ALX-270-379-M005		5 mg	275.00 USD

Product Specification

FORMULA:	C₁₇H₁₄N₂O₄S
MW:	342.4
PURITY:	≥95% (HPLC)
APPEARANCE:	Solid.
SOLUBILITY:	Soluble in DMSO, methanol or acetonitrile.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	+4°C
HANDLING:	After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas. Protect from light.

Product Description

Potent inhibitor of mammalian HDAC (IC₅₀=15.7nM). Acts as a ligand for the enzyme active site metal ion. Upregulates plasminogen activator inhibitor type 2 (PAI-2) expression with concomitant inhibition of urokinase (u-PA) gene and protein expression in HT-1080 and U-937 cells. Elevates the expression of extracellular matrix proteins fibronectin and gelsolin. Induces apoptosis in P-glyoprotein (Pgp) positive and Pgp negative multidrug resistant cells.

Product Specific Literature References

Oxamflatin: a novel compound which reverses malignant phenotype to normal one via induction of JunD: H. Sonoda, et al.; Oncogene 13, 143 (1996) Abstract
Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase: Y.B. Kim, et al.; Oncogene 18, 2461 (1999) Abstract
The novel anti-tumour agent oxamflatin differentially regulates urokinase and plasminogen activator inhibitor type 2 expression and inhibits urokinase-mediated proteolytic activity: A.E. Dear & R.L. Medcalf; Biochim. Biophys. Acta 1492, 15 (2000) Abstract
Novel mechanisms of apoptosis induced by histone deacetylase inhibitors: M.J. Peart, et al.; Cancer Res. 63, 4460 (2003) Abstract

Further Categories Containing This Product:

HDAC Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Agents (Enzyme Inhibitors)

ALX-430-146

Revised 30-Nov-06

PAC-1
SYNONYMS	4-(Phenylmethyl)[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hydrazide-1-piperazine acetic acid
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (Apoptosis Inducers)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-146-M010		10 mg	45.00 USD
ALX-430-146-M050		50 mg	180.00 USD

Product Specification

FORMULA:	C₂₃H₂₈N₄O₂
MW:	392.5
CAS NUMBER:	315183-21-2
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in acetonitrile, DMSO, dioxane or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

First molecule to directly activate procaspase-3 to caspase-3 in vitro. Has been shown to induce apoptosis in cancer cells.

Product Specific Literature References

Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy: K.S. Putt, et al.; Nat. Chem. Biol. 2, 543 (2006) Abstract

Further Categories Containing This Product:

Caspases Other Products

ALX-350-258

Revised 08-Apr-08

Parthenolide
SYNONYMS	(1aR-[1aR,4E,7aS,-10aS,-10bR])-2,3-6,7,7a,8,10a,10b-Octahydro-1a,5-dimethyl-8-methyleneoxireno[9,10]cyclo deca[1,2-b]furan-9(1aH)-one
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-350-258-M005		5 mg	15.00 USD
ALX-350-258-M025		25 mg	30.00 USD

Product Specification

FORMULA:	C₁₅H₂₀O₃
MW:	248.3
CAS NUMBER:	20554-84-1
MERCK INDEX:	14: 7048
RTECS:	LY4220000
SOURCE/HOST:	Isolated from feverfew leaves.
PURITY:	≥99% (TLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (100mg/ml), dichloromethane (50mg/ml) or 100% ethanol (20mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Sesquiterpene lactone. Anti-inflammatory compound. Specifically inhibits activation of NF-κB by preventing the degradation of IκBα and IκBβ. Inhibits activation of MAP kinase (MAPK/ERK) and generation of leukotriene B₄ and thromboxane B₂. Potent anticancer agent. Induces apoptosis in various cancer cell lines. Specifically inhibits histone deacetylase 1 (HDAC1) without affecting other class I/II HDACs. Inhibits tubulin carboxypeptidase (TCP) activity.

Product Specific Literature References

A comparison of the effects of an extract of feverfew and parthenolide, a component of feverfew, on human platelet activity in-vitro: W.A. Groenewegen & S. Heptinstall; J. Pharm. Pharmacol. 42, 553 (1990) Abstract
Feverfew extracts and parthenolide irreversibly inhibit vascular responses of the rabbit aorta: R.W. Barsby, et al.; J. Pharm. Pharmacol. 44, 737 (1992) Abstract
Inhibition of 5-lipoxygenase and cyclo-oxygenase in leukocytes by feverfew. Involvement of sesquiterpene lactones and other components: H. Sumner, et al.; Biochem. Pharmacol. 43, 2313 (1992) Abstract
Inhibition of the expression of inducible cyclooxygenase and proinflammatory cytokines by sesquiterpene lactones in macrophages correlates with the inhibition of MAP kinases: D. Hwang, et al.; BBRC 226, 810 (1996) Abstract
Sesquiterpene lactones specifically inhibit activation of NF-kappa B by preventing the degradation of I kappa B-alpha and I kappa B-beta: S.P. Hehner, et al.; J. Biol. Chem. 273, 1288 (1998) Abstract
Sesquiterpene lactones inhibit inducible nitric oxide synthase gene expression in cultured rat aortic smooth muscle cells: H.R. Wong & I.Y. Menendez; BBRC 262, 375 (1999) Abstract
The antiinflammatory sesquiterpene lactone parthenolide inhibits NF- kappa B by targeting the I kappa B kinase complex: S.P. Hehner, et al.; J. Immunol. 163, 5617 (1999) Abstract
Paclitaxel sensitivity of breast cancer cells with constitutively active NF-kappaB is enhanced by IkappaBalpha super-repressor and parthenolide: N.M. Patel, et al.; Oncogene 19, 4159 (2000) Abstract
Antitumor agent parthenolide reverses resistance of breast cancer cells to tumor necrosis factor-related apoptosis-inducing ligand through sustained activation of c-Jun N-terminal kinase: H. Nakshatri, et al.; Oncogene 23, 7330 (2004) Abstract
Involvement of proapoptotic Bcl-2 family members in parthenolide-induced mitochondrial dysfunction and apoptosis: S. Zhang, et al.; Cancer Lett. 211, 175 (2004) Abstract
Parthenolide-induced apoptosis in multiple myeloma cells involves reactive oxygen species generation and cell sensitivity depends on catalase activity: W. Wang, et al.; Apoptosis 11, 2225 (2006) Abstract
Parthenolide inhibits tubulin carboxypeptidase activity: X. Fonrose, et al.; Cancer Res. 67, 3371 (2007) Abstract
Parthenolide specifically depletes histone deacetylase 1 protein and induces cell death through ataxia telangiectasia mutated: Y.N. Gopal, et al.; Chem. Biol. 14, 813 (2007) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors • COX Inhibitors • Other Natural Products for Inflammation Research

ALX-270-234

Revised 29-Jan-05

PD 150,606
SYNONYMS	3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic acid
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Calpains / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-234-M005		5 mg	65.00 USD

Product Specification

FORMULA:	C₉H₇IO₂S
MW:	306.1
PURITY:	≥95%
APPEARANCE:	Off-white solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light. Keep under inert gas.

Product Description

Cell permeable, selective, and non-peptide calpain inhibitor directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases such as cathepsin B and cathepsin L. Prevents dexamethasone-induced apoptosis in thymocytes.

Product Specific Literature References

Modulation of hypoxia-induced calpain activity in rat renal proximal tubules: C.L. Edelstein, et al.; Kidney Int. 50, 1150 (1996) Abstract
An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective: K.K. Wang, et al.; PNAS 93, 6687 (1996) Abstract
Alpha-mercaptoacrylic acid derivatives as novel selective calpain inhibitors: K.K. Wang, et al.; Adv. Exp. Med. Biol. 389, 95 (1996) Abstract
Crystal structure of calcium bound domain VI of calpain at 1.9A resolution and its role in enzyme assembly, regulation, and inhibitor binding: G.D. Lin, et al.; Nat. Struct. Biol. 4, 539 (1997) Abstract
Calpains mediate calcium and chloride influx during the late phase of cell injury: S.L. Waters, et al.; J. Pharmacol. Exp. Ther. 283, 1177 (1997) Abstract

Further Categories Containing This Product:

Apoptosis Inducers & Inhibitors Other Products

ALX-445-004

Revised 08-Oct-08

Phorbol 12-myristate 13-acetate
SYNONYMS	PMA 12-O-Tetradecanoylphorbol 13-acetate TPA
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Phorbols / Phorbol Esters

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-445-004-M001		1 mg	18.00 USD
ALX-445-004-M005		5 mg	60.00 USD
ALX-445-004-M010		10 mg	110.00 USD
ALX-445-004-M025		25 mg	210.00 USD

Product Specification

FORMULA:	C₃₆H₅₆O₈
MW:	616.8
CAS NUMBER:	16561-29-8
MERCK INDEX:	14: 7332
RTECS:	QH4377000
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, methanol, 100% ethanol, acetone, ether or dimethylformamide; almost insoluble in aqueous buffers.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Dissolve in an organic solvent prior to dilution into aqueous buffers. Add calculated volume of organic solvent to vial to prepare concentrated stock solution. Intermediate dilutions into the same organic solvent are recommended prior to final dilution into aqueous buffer.
HANDLING:	Protect from light.
HAZARD:	MAY BE CARCINOGENIC. HARMFUL. MAY BE MUTAGENIC.

Product Description

Most commonly used phorbol ester. Binds to and activates protein kinase C (PKC). Causes an extremely wide range of effects in cells and tissues. Very potent mouse skin tumor promoter. Inhibits apoptosis induced by Fas, but induces apoptosis in HL-60 promyelocytic leukemia cells.

Product Specific Literature References

Autoxidation of phorbol esters under normal storage conditions: R. Schmidt & E. Hecker; Cancer Res. 35, 1375 (1975) Abstract
Phorbol esters as signal transducers and tumor promoters: M. Castagna; Biol. Cell 59, 3 (1987), Review Abstract
P.M. Blumberg; CRC Crit. Rev. Toxicol 8, 153 (1988)
Differential irreversible insertion of protein kinase C into phospholipid vesicles by phorbol esters and related activators: M.G. Kazanietz, et al.; J. Biol. Chem. 267, 20878 (1992) Abstract
Phorbol esters induce nitric oxide synthase activity in rat hepatocytes. Antagonism with the induction elicited by lipopolysaccharide: S. Hortelano, et al.; J. Biol. Chem. 267, 24937 (1992) Abstract; Full Text
Phorbol ester induces apoptosis in HL-60 promyelocytic leukemia cells but not in HL-60 PET mutant: D.E. Macfarlane & P.S. O'Donnel; Leukemia 7, 1846 (1993) Abstract
Effect of phorbol 12-myristate 13-acetate on Ca2+-ATPase activity in rat liver nuclei: K. Oishi & M. Yamaguchi; J. Cell. Biochem. 55, 168 (1994) Abstract
Role for ceramide as an endogenous mediator of Fas-induced cytotoxicity: C.G. Tepper, et al.; PNAS 92, 8443 (1995) Abstract
Evidence for different mechanisms of growth inhibition of T-cell lymphoma by phorbol esters and concanavalin A: S. Desrivieres, et al.; J. Biol. Chem. 272, 2470 (1997) Abstract
Phorbol esters and synthetic diacylglycerols inhibit gamma-aminobutyric acid uptake in human spermatozoa: an effect mediated by protein kinase C?: A. Aanesen, et al.; Mol. Hum. Reprod. 4, 339 (1998) Abstract
Gene expression of TPA induced differentiation in HL-60 cells by DNA microarray analysis: X. Zheng, et al.; Nucleic Acids Res. 30, 4489 (2002) Abstract; Full Text
Phorbol esters and neurotransmitter release: more than just protein kinase C?: E.M. Silinsky and T.J. Searl; Br. J. Pharmacol. 138, 1191 (2003), Review Abstract
Characterization of phorbol esters activity on individual mammalian protein kinase C isoforms, using the yeast phenotypic assay: L. Saraiva, et al.; Eur. J. Pharmacol. 491, 101 (2004) Abstract

Further Categories Containing This Product:

PKC Activators • Natural Products - Apoptosis Inducers & Inhibitors

ALX-106-017

Revised 04-Mar-05

L-Pipecolic acid . hydrochloride
SYNONYMS	L-(-)-Pipecolinic acid . HCl
PRODUCT LINE	Combinatorial Chemistry
PRODUCT CATEGORY	Special Amino Acids

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-106-017-M050		50 mg	30.00 USD

Product Specification

FORMULA:

C₆H₁₁NO₂