ALEXIS Biochemicals: PD 150,606

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ALX-430-014

Revised 13-May-08

DETA NONOate
SYNONYMS	NOC-18 DETA/NO (Z)-1-[2-(2-Aminoethyl)-N-(2-ammonioethyl)amino]diazen-1-ium-1,2-diolate
PRODUCT LINE	Nitric Oxide Pathway
PRODUCT CATEGORY	Nitric Oxide Donors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-014-M005		5 mg	30.00 USD
ALX-430-014-M025		25 mg	100.00 USD
ALX-430-014-5005		5x5 mg	120.00 USD

Product Specification

FORMULA:	C₄H₁₃N₅O₂
MW:	163.2
CAS NUMBER:	146724-94-9
RTECS:	KH2502500
PURITY:	≥97% (¹H-NMR)
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	Soluble in water or methanol.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Relatively stable in alkaline solution.
HANDLING:	Protect from light and moisture.
HAZARD:	IRRITANT.

Product Description

Nitric oxide (NO) donor. Induces apoptosis in macrophages. The half-life time of DETA NONOate is 20 hours at 37°C and 56 hours at 22-25°C in 0.1M phosphate buffer, pH 7.4. Decomposition of NONOates is nearly instantaneous at pH 5.0. DETA NONOate liberates 2 mol of NO per mol of parent compound.

Product Specific Literature References

New nitric oxide-releasing zwitterions derived from polyamines: J.A. Hrabie, et al.; J. Org. Chem. 58, 1472 (1993)
NOC, a nitric-oxide-releasing compound, induces dose dependent apoptosis in macrophages: M. Shimaoka, et al.; BBRC 209, 519 (1995) Abstract
Schedule and concentration-dependent induction of apoptosis in leukemia cells by nitric oxide: P.J. Shami, et al.; Leukemia 12, 1461 (1998) Abstract
In vitro cytotoxicity of the nitric oxide donor, S-nitroso-N-acetyl-penicillamine, towards cells from human oral tissue: H. Babich, et al.; Pharmacol. Toxicol. 84, 218 (1999) Abstract
Expression and release of chemokines associated with apoptotic cell death in human promonocytic U937 cells and peripheral blood mononuclear cells: H. Muhl, et al.; Eur. J. Immunol. 29, 3225 (1999) Abstract
Resistance to nitric oxide-mediated apoptosis in HL-60 variant cells is associated with increased activities of Cu,Zn-superoxide dismutase and catalase: M. Yabuki, et al.; Free Radic. Biol. Med. 26, 325 (1999) Abstract
Protective effect of thioredoxin upon NO-mediated cell injury in THP1 monocytic human cells: P.J. Ferret, et al.; Biochem. J. 346, 759 (2000) Abstract
In vitro cytotoxicity of glyco-S-nitrosothiols. a novel class of nitric oxide donors: H. Babich & H.L. Zuckerbraun; Toxicol. In Vitro 15, 181 (2001) Abstract
The selective pulmonary vasodilatory effect of inhaled DETA/NO, a novel nitric oxide donor, in ARDS-a pilot human trial: C.F. Lam, et al.; J. Crit. Care 19, 48 (2004) Abstract
Endogenous NO regulates superoxide production at low oxygen concentrations by modifying the redox state of cytochrome c oxidase: M. Palacios-Callender, et al.; PNAS 101, 7630 (2004) Abstract; Full Text
Hemodynamic effects of the nitric oxide donor DETA/NO in mice: C.G. Schyvens, et al.; Clin. Exp. Hypertens. 26, 525 (2004) Abstract
The nitric oxide donor DETA-NONOate decreases matrix metalloproteinase-9 expression and activity in rat aortic smooth muscle and abdominal aortic explants: I. Sinha, et al.; Ann. Vasc. Surg. 20, 92 (2006) Abstract
Inflammatory cytokines induce MAdCAM-1 in murine hepatic endothelial cells and mediate alpha-4 beta-7 integrin dependent lymphocyte endothelial adhesion in vitro: T. Ando, et al.; BMC Physiol. 7, 10 (2007) Abstract; Full Text

Further Categories Containing This Product:

Apoptosis Inducers & Inhibitors Other Products

ALX-420-036

Revised 21-Jul-05

DICA
SYNONYMS	2-(2,4-Dichlorophenoxy)-N-(2-mercaptoethyl)acetamide
PRODUCT LINE	Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY	Caspase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-420-036-M005		5 mg	40.00 USD
ALX-420-036-M025		25 mg	160.00 USD

Product Specification

FORMULA:	C₁₀H₁₁Cl₂NO₂S
MW:	280.2
CAS NUMBER:	613665-26-2
PURITY:	≥98% (TLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in methanol or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Do not store DMSO solutions for more than 1 day.
HANDLING:	Keep under inert gas. Protect from oxygen.

Product Description

Inhibitor of caspase-3 and caspase-7 binding to an allosteric site and not to the active site.

Product Specific Literature References

Discovery of an allosteric site in the caspases: J.A. Hardy, et al.; PNAS 101, 12461 (2004) Abstract; Full Text

Further Categories Containing This Product:

Apoptosis Inducers & Inhibitors Other Products

ALX-420-027

Revised 26-Mar-08

DMNQ
SYNONYMS	2,3-Dimethoxy-1,4-naphthoquinone
PRODUCT LINE	Oxidative Stress
PRODUCT CATEGORY	Oxidative Stress Markers & Reagents / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-420-027-M005		5 mg	68.00 USD
ALX-420-027-M010		10 mg	115.00 USD
ALX-420-027-M025		25 mg	225.00 USD

Product Specification

FORMULA:	C₁₂H₁₀O₄
MW:	218.2
CAS NUMBER:	6956-96-3
PURITY:	≥99%
APPEARANCE:	Yellow crystalline solid.
SOLUBILITY:	Soluble in acetone, DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	IRRITANT.

Product Description

Redox-cycling agent that induces intracellular superoxide anion formation and, depending on the concentration, induces cell proliferation, apoptosis or necrosis. DMNQ does not react with free thiol groups, is non-alkylating and adduct-forming in contrast to other quinones. Thus, DMNQ is a valuable tool for the generation of reactive oxygen species (ROS) in order to study the role of ROS in cell toxicity, apoptosis and necrosis.

Product Specific Literature References

Different prooxidant levels stimulate growth, trigger apoptosis, or produce necrosis of insulin-secreting RINm5F cells: J.M. Dypbukt, et al.; J. Biol. Chem. 269, 30553 (1994) Abstract; Full Text
DNA single-strand breakage in mammalian cells induced by redox cycling quinones in the absence of oxidative stress: W.A. Morgan; J. Biochem. Toxicol. 10, 227 (1995) Abstract
Potentiation of nitric oxide synthase expression by superoxide in interleukin 1 beta-stimulated rat mesangial cells: K.F. Beck, et al.; FEBS Lett. 435, 35 (1998) Abstract
The relative importance of oxidative stress versus arylation in the mechanism of quinone-induced cytotoxicity to platelets: S.A. Seung, et al.; Chem. Biol. Interact. 113, 133 (1998) Abstract

Further Categories Containing This Product:

Apoptosis Inducers & Inhibitors Other Products • Non-apoptotic Cell Death / Necrosis

ALX-270-098

Revised 16-Nov-06

Erbstatin analog
SYNONYMS	Methyl 2,5-dihydroxycinnamate
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	EGFR Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-098-M005		5 mg	55.00 USD

Product Specification

FORMULA:	C₁₀H₁₀O₄
MW:	194.2
CAS NUMBER:	63177-57-1
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white to light brown crystalline solid.
SOLUBILITY:	Soluble in methanol, DMSO or dilute aqueous base.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Considerably longer half-life in aqueous solution than erbstatin itself. Induces apoptosis.

Product Specific Literature References

Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors: K. Umezawa, et al.; FEBS Lett. 260, 198 (1990) Abstract
Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T3 cells: K. Umezawa, et al.; FEBS Lett. 314, 289 (1992) Abstract
Induction of mouse thymocyte apoptosis by inhibitors of tyrosine kinases is associated with dephosphorylation of nuclear proteins: Y. Azuma, et al.; Cell Immunol. 152, 271 (1993) Abstract
Inhibition of Abelson oncogene function by erbstatin analogues: M. Kawada, et al.; Drugs Exp. Clin. Res. 19, 235 (1993) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Apoptosis Inducers & Inhibitors Other Products

ALX-155-037

Revised 21-Oct-08

Extracellular Death Factor
SYNONYMS	EDF
PRODUCT LINE	Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY	Apoptosis Inducers & Inhibitors Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-155-037-M001		1 mg	40.00 USD
ALX-155-037-M005		5 mg	120.00 USD

Product Specification

SEQUENCE:	H-Asn-Asn-Trp-Asn-Asn-OH
FORMULA:	C₂₇H₃₆N₁₀O₁₀
MW:	660.6
SOURCE/HOST:	Synthetic.
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white powder.
FORMULATION:	Lyophilized.
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Programmed cell death (PCD) in E. coli depends on cell-to-cell communication, a process known as quorum sensing. The communicating cells produce and emit the extracellular death factor (EDF). After reaching a sufficent concentration, EDF activates the cell death pathway in a subset of cells.

Product Specific Literature References

A linear pentapeptide is a quorum-sensing factor required for mazEF-mediated cell death in Escherichia coli: I. Kolodkin-Gal, et al.; Science 318, 652 (2007) Abstract

Further Categories Containing This Product:

Peptides

ALX-480-059

Revised 09-Mar-06

Guanosine 3',5'-cyclic Monophosphate . sodium salt
SYNONYMS	cGMP . Na
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	cGMP Derivatives

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-480-059-M025		25 mg	25.00 USD
ALX-480-059-M100		100 mg	95.00 USD

Product Specification

FORMULA:	C₁₀H₁₁N₅O₇P . Na
MW:	344.2 . 23.0
CAS NUMBER:	40732-48-7
MERCK INDEX:	14: 2709
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Intracellular messenger implicated in mediating action of nitric oxide (NO) in many cell types. Target receptors for the second messenger guanosine 3',5'-cyclic monophosphate (cGMP) include protein kinase G (PKG) isozymes, cGMP-dependent ion channels as well as cGMP-responsive phosphodiesterases. In presence of corresponding phosphodiesterases cGMP is metabolized rapidly. Suppresses apoptosis.

Product Specific Literature References

Cyclic GMP metabolism and involvement in biological regulation: N.D. Goldberg & M.K. Haddox; Ann. Rev. Biochem. 46, 823 (1977) Abstract
Interleukin-1 beta suppresses apoptosis in rat ovarian follicles by increasing nitric oxide production: S.Y. Chun, et al.; Endocrinology 136, 3120 (1995) Abstract

Further Categories Containing This Product:

Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products • Apoptosis Inducers & Inhibitors Other Products

ALX-270-016

Revised 05-May-08

H-7 . dihydrochloride
SYNONYMS	(±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-016-M010		10 mg	60.00 USD
ALX-270-016-M025		25 mg	120.00 USD

Product Specification

FORMULA:	C₁₄H₁₇N₃O₂S . 2 HCl
MW:	291.4 . 73.0
CAS NUMBER:	108930-17-2
PURITY:	≥98%
APPEARANCE:	White to light yellow solid.
SOLUBILITY:	Soluble in water, 100% ethanol or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibitor of protein kinase C (PKC), cAMP- and cGMP-dependent protein kinase (PKA and PKG). Also inhibits myosin light chain kinase. Induces apoptotic DNA fragmentation and cell death. Inhibits telomerase activity in treated NPC-076 cells.

Product Specific Literature References

1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets: S. Kawamoto & H. Hidaka; BBRC 125, 258 (1984) Abstract
Stimulus-dependent inhibition of platelet aggregation by the protein kinase C inhibitors polymyxin B, H-7 and staurosporine: C. Schächtele, et al.; BBRC 151, 542 (1988) Abstract
Blockade of the spinal excitatory effect of cAMP on the startle reflex by intrathecal administration of the isoquinoline sulfonamide H-8: comparison to the protein kinase C inhibitor H-7: N.M. Boulis & M. Davis; Brain Res. 525, 198 (1990) Abstract
Potent selective inhibition of 7-O-methyl UCN-01 against protein kinase C: I. Takahashi, et al.; J. Pharmacol. Exp. Ther. 255, 1218 (1990) Abstract
The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source: J. Quick, et al.; BBRC 187, 657 (1992) Abstract
Modulation of neutrophil superoxide generation by inhibitors of protein kinase C, calmodulin, diacylglycerol and myosin light chain kinases, and peptidyl prolyl cis-trans isomerase: H. Bergstrand, et al.; J. Pharmacol. Exp. Ther. 263, 1334 (1992) Abstract
C. Gimond and M. Aumailley; Exp. Cell Res. 203, 365 (1992) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; Biochem. Biophys. Res. Commun. 241, 730 (1997) Abstract

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • PKA Inhibitors

ALX-270-017

Revised 27-Apr-06

H-89 . dihydrochloride
SYNONYMS	N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-017-M001		1 mg	22.00 USD
ALX-270-017-M005		5 mg	55.00 USD

Product Specification

FORMULA:	C₂₀H₂₀BrN₃O₂S . 2HCl
MW:	446.4 . 73.0
CAS NUMBER:	127243-85-0
PURITY:	≥97% (¹H-NMR)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO or methanol; also soluble in ethanol: water (1:1).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stock solutions are stable for at least 3-4 weeks when stored at +4°C. We recommend using a fresh solution each day.

Product Description

Cell permeable potent and selective inhibitor of cAMP- and cGMP-dependent protein kinases (PKA and PKG) and protein kinase Cµ (PKCµ). In contrast, most other protein kinase C (PKC) isotypes are much more weakly inhibited. Also inhibits Ca²⁺/calmodulin-dependent protein kinase II, casein kinase I and myosin light chain kinase. Induces apoptosis.

Product Specific Literature References

Polyamines differentially inhibit cyclic AMP-dependent protein kinase- mediated phosphorylation in the brain of the tobacco hornworm, Manduca sexta: W.L. Combest, et al.; J. Neurochem. 51, 1581 (1988) Abstract
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5- isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma: T. Chijiwa, et al.; J. Biol. Chem. 265, 5267 (1990) Abstract; Full Text
A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2- bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells: C.C. Geilen; FEBS Lett. 309, 381 (1992) Abstract
Protein kinase A inhibitors enhance radiation-induced apoptosis: D. Findik, et al.; J. Cell. Biochem. 57, 12 (1995) Abstract
Characterization of activators and inhibitors of protein kinase C mu: F.-J. Johannes, et al.; Eur. J. Biochem. 227, 303 (1995) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells: T. Bouschet, et al.; J. Biol. Chem. 278, 4778 (2003) Abstract; Full Text

Further Categories Containing This Product:

CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Casein Kinase Inhibitors

ALX-430-101

Revised 08-Aug-08

HA14-1
SYNONYMS	Ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
PRODUCT LINE	Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY	Bcl-2 Family Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-101-M005		5 mg	40.00 USD
ALX-430-101-M025		25 mg	160.00 USD

Product Specification

FORMULA:	C₁₇H₁₇N₂O₅Br
MW:	409.2
CAS NUMBER:	65673-63-4
PURITY:	≥95% (¹H-NMR)
APPEARANCE:	Off-white to light yellow powder.
SOLUBILITY:	Soluble in DMSO, dimethyl formamide or halogenated solvents; also soluble in 100% ethanol (hot).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Unstable in solution. Prepare fresh solution for each application.
HANDLING:	Keep cool and dry.
IDENTITY: