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ALX-270-444

Revised 07-Apr-08

ABT-888
SYNONYMS	2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide . dihydrochloride
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-444-M001		1 mg	50.00 USD
ALX-270-444-M005		5 mg	150.00 USD

Product Specification

FORMULA:	C₁₃H₁₆N₄O . 2HCl
MW:	244.3 . 73.0
CAS NUMBER:	912445-05-7
PURITY:	≥98% (HPLC)
APPEARANCE:	Colorless to white crystalline solid.
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Potent inhibitor of PARP-1 and PARP-2 (potency ≤5nM in vitro). Does not inhibit other NAD-binding enzymes. Has minimal CYP450 inhibition and induction. Shows broad spectrum of chemo- and radiopotentiation. Enantiomeric purity ≥97% suitable for in vivo studies. Does not show inherent cytotoxicity and shows no single agent activity in tumor models. Has excellent bioavailability and good blood-brain permeation. Increases tumor growth delay resulting from radiation and DNA-damaging agents.

Product Specific Literature References

Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models: J.M. Albert, et al.; Clin. Cancer Res. 13, 3033 (2007) Abstract
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models: C.K. Donawho, et al.; Clin. Cancer Res. 13, 2728 (2007) Abstract

ALX-270-285

Revised 20-Oct-08

5-AIQ . hydrochloride
SYNONYMS	5-Aminoisoquinolinone . HCl
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	DNA Repair Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-285-M001		1 mg	50.00 USD
ALX-270-285-M005		5 mg	175.00 USD

Product Specification

FORMULA:	C₉H₈N₂O . HCl
MW:	160.2 . 36.5
PURITY:	≥97%
APPEARANCE:	Beige to brown powder.
SOLUBILITY:	Soluble in water (warm).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from moisture.
HAZARD:	IRRITANT.

Product Description

Water-soluble, potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1).

Product Specific Literature References

Effects of 5-aminoisoquinolinone, a water-soluble, potent inhibitor of the activity of poly (ADP-ribose) polymerase on the organ injury and dysfunction caused by haemorrhagic shock: M.C. McDonald, et al.; Br. J. Pharmacol. 130, 843 (2000) Abstract
Effects of 5-aminoisoquinolinone, a water-soluble, potent inhibitor of the activity of poly (ADP-ribose) polymerase, in a rodent model of lung injury: S. Cuzzocrea, et al.; Biochem. Pharmacol. 63, 293 (2002) Abstract
Substrate-assisted catalysis by PARP10 limits its activity to mono-ADP-ribosylation: H. Kleine, et al.; Mol. Cell 32, 57 (2008) Abstract

Further Categories Containing This Product:

PARP Inhibitors

ALX-270-044

Revised 20-Oct-08

3-Aminobenzamide
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-044-G001		1 g	50.00 USD
ALX-270-044-G005		5 g	190.00 USD

Product Specification

FORMULA:	C₇H₈N₂O
MW:	136.2
CAS NUMBER:	3544-24-9
RTECS:	CU8992000
PURITY:	≥97%
APPEARANCE:	White to tan powder.
SOLUBILITY:	Soluble in DMSO or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
HAZARD:	IRRITANT. MAY BE MUTAGENIC.

Product Description

Inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1). Has minimal effect on bacterial toxin-mediated ADP-ribosylation. Apoptosis inhibitor.

Product Specific Literature References

Signal transduction in Coprinus congregatus: evidence for the involvement of G proteins in blue light photomorphogenesis: K.R. Kozak and I.A. Ross; BBRC 179, 1225 (1991) Abstract
Cell death protection by 3-aminobenzamide and other poly(ADP- ribose)polymerase inhibitors: different effects on human natural killer and lymphokine activated killer cell activities: D. Monti, et al.; BBRC 199, 525 (1994) Abstract
Cell death protection by 3-aminobenzamide: impairment of cytoskeleton function in human NK cell-mediated killing: W. Malorni, et al.; BBRC 199, 1250 (1994) Abstract
3-Aminobenzamide protects cells from UV-B-induced apoptosis by acting on cytoskeleton and substrate adhesion: W. Malorni, et al.; BBRC 207, 715 (1995) Abstract
Inactivation of the poly(ADP-ribose) polymerase gene affects oxygen radical and nitric oxide toxicity in islet cells: B. Heller, et al.; J. Biol. Chem. 270, 11176 (1995) Abstract
Inhibitors of poly(ADP-ribose) polymerase block nitric oxide-induced apoptosis but not differentiation in human leukemia HL-60 cells: M.L. Kuo, et al.; BBRC 219, 502 (1996) Abstract
Substrate-assisted catalysis by PARP10 limits its activity to mono-ADP-ribosylation: H. Kleine, et al.; Mol. Cell 32, 57 (2008) Abstract

Further Categories Containing This Product:

Apoptosis Inducers & Inhibitors Other Products • DNA Repair Other Products

ALX-270-250

Revised 18-Jan-06

4-Amino-1,8-naphthalimide
SYNONYMS	4-ANI
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-250-M010		10 mg	35.00 USD

Product Specification

FORMULA:	C₁₂H₈N₂O₂
MW:	212.2
CAS NUMBER:	1742-95-6
RTECS:	DE4081000
PURITY:	≥95%
APPEARANCE:	Yellow to orange solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
USE/STABILITY:	Stock solutions are stable for 3 months when stored at –20°C.
HAZARD:	IRRITANT.

Product Description

Potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) (IC₅₀=0.18µM). About 1000-fold more potent than 3-aminobenzamide (Prod. No. ALX-270-044).

Product Specific Literature References

Specific inhibitors of poly(ADP-ribose) synthetase and mono(ADP-ribosyl)transferase: M. Banasik, et al.; J. Biol. Chem. 267, 1569 (1992) Abstract; Full Text
Nitric oxide toxicity in islet cells involves poly(ADP-ribose) polymerase activation and concomitant NAD+ depletion: J. Radons, et al.; BBRC 199, 1270 (1994) Abstract
Combination effects of poly(ADP-ribose) polymerase inhibitors and DNA-damaging agents in ovarian tumor cell lines--with special reference to cisplatin: F. Bernges & W.J. Zeller; J. Cancer Res. Clin. Oncol. 122, 665 (1996) Abstract
Inhibition of the activity of poly(ADP ribose) synthetase reduces ischemia-reperfusion injury in the heart and skeletal muscle: C. Thiemermann, et al.; PNAS 94, 679 (1997) Abstract; Full Text
Effects of inhibitors of the activity of poly (ADP-ribose) synthetase on the liver injury caused by ischaemia-reperfusion: a comparison with radical scavengers: J. Bowes & C. Thiemermann; Br. J. Pharmacol. 124, 1254 (1998) Abstract
4-Amino-1,8-naphthalimide: a novel inhibitor of poly(ADP-ribose) polymerase and radiation sensitizer: A. Schlicker, et al.; Int. J. Radiat. Biol. 75, 91 (1999) Abstract

Further Categories Containing This Product:

DNA Repair Other Products

ALX-270-174

Revised 20-Oct-08

Benzamide
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-174-G005		5 g	20.00 USD

Product Specification

FORMULA:	C₇H₇NO
MW:	121.1
CAS NUMBER:	55-21-0
MERCK INDEX:	14: 1060
RTECS:	CU8700000
PURITY:	≥99%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
HAZARD:	HARMFUL.

Product Description

Inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1). Neuroprotectant.

Product Specific Literature References

Cytotoxicity of a new IMP dehydrogenase inhibitor, benzamide riboside, to human myelogenous leukemia K562 cells: H.N. Jayaram, et al.; BBRC 186, 1600 (1992) Abstract
Nitric oxide activation of poly(ADP-ribose) synthetase in neurotoxicity: J. Zhang, et al.; Science 263, 687 (1994) Abstract
Substrate-assisted catalysis by PARP10 limits its activity to mono-ADP-ribosylation: H. Kleine, et al.; Mol. Cell 32, 57 (2008) Abstract

Further Categories Containing This Product:

DNA Repair Other Products

ALX-270-486

Revised 15-Jul-08

3-(4-Chlorophenyl)quinoxaline-5-carboxamide
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-486-M005		5 mg	230.00 USD

Product Specification

FORMULA:	C₁₅H₁₀ClN₃O
MW:	283.7
PURITY:	≥95% (HPLC)
APPEARANCE:	Light brown solid.
SOLUBILITY:	Soluble in DMSO (10mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Packaged under inert gas. Protect from light.
HAZARD:	IRRITANT.

Product Description

Potent quinoxaline-based PARP inhibitor with a 5-fold selectivity towards PARP-2 (IC₅₀=7nM) over PARP-1 (IC₅₀=33nM). Brain-permeant. Exhibits good pharmacokinetics.

Product Specific Literature References

Discovery of quinazolinone and quinoxaline derivatives as potent and selective poly(ADP-ribose) polymerase-1/2 inhibitors: A. Iwashita, et al.; FEBS Lett. 579, 1389 (2005) Abstract
Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling: J. Ishida, et al.; Bioorg. Med. Chem. 14, 1378 (2006) Abstract

Further Categories Containing This Product:

DNA Repair Other Products

ALX-270-221

Revised 23-Jul-07

DPQ
SYNONYMS	3,4-Dihydro-5-[4-(1-piperidinyl)butoxy]-1(2H)-isoquinolinone
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-221-M001		1 mg	52.00 USD
ALX-270-221-M005		5 mg	195.00 USD

Product Specification

FORMULA:	C₁₈H₂₆N₂O₂
MW:	302.4
CAS NUMBER:	129075-73-6
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white to light brown solid.
SOLUBILITY:	Soluble in DMSO; slightly soluble in 100% ethanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stock solutions in DMSO are stable for up to 1 month when stored at -20°C.
HAZARD:	HARMFUL.
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Very potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor.

Product Specific Literature References

Dihydroisoquinolines: the design and synthesis of a new series of potent inhibitors of poly(ADP-ribose) polymerase: M.J. Suto, et al.; Anticancer Drug Des. 6, 107 (1991) Abstract
Poly(ADP-ribose) polymerase gene disruption renders mice resistant to cerebral ischemia: M.J.L. Eliasson, et al.; Nat. Med. 3, 1089 (1997) Abstract
Neuroprotective effects of inhibiting poly(ADP-ribose) synthetase on focal cerebral ischemia in rats: H. Takahashi, et al.; J. Cereb. Blood Flow Metab. 17, 1137 (1997) Abstract
Role of poly(ADP-ribose) synthetase in inflammation and ischaemia-reperfusion: C. Szabo & V.L. Dawson; TIPS 19, 287 (1998), (Review) Abstract
Post-treatment with an inhibitor of poly(ADP)-ribose polymerase attenuates cerebral damage in focal ischemia: K. Takahashi, et al.; Brain Res. 829, 46 (1999) Abstract; Full Text
Poly(ADP-ribose) polymerase inhibitors attenuate necrotic but not apoptotic neuronal death in experimental models of cerebral ischemia: F. Moroni, et al.; Cell Death Differ. 8, 921 (2001) Abstract
Comet assay as a novel approach for studying DNA damage in focal cerebral ischemia: differential effects of NMDA receptor antagonists and poly(ADP-ribose) polymerase inhibitors: L. Giovannelli, et al.; J. Cereb. Blood Flow Metab. 22, 697 (2002) Abstract

Further Categories Containing This Product:

DNA Repair Other Products

ALX-270-452

Revised 27-Nov-06

DR2313
SYNONYMS	2-Methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidine-4-one
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-452-M001		1 mg	20.00 USD
ALX-270-452-M005		5 mg	60.00 USD
ALX-270-452-M025		25 mg	180.00 USD

Product Specification

FORMULA:	C₈H₁₀N₂OS
MW:	182.2
CAS NUMBER:	284028-90-6
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, methanol or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:	After reconstitution, prepare aliquots and store at -20°C. Protect from light.
HAZARD:	HARMFUL.

Product Description

Potent, water soluble competitive PARP inhibitor (IC₅₀=0.20µM and 0.24µM for PARP-1 and PARP-2 respectively).

Product Specific Literature References

A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological profiles, neuroprotective effects, and therapeutic time window in cerebral ischemia in rats: H. Nakajima, et al.; Pharmacol. Exp. Ther. 312, 472 (2005) Abstract; Full Text

ALX-270-383

Revised 20-Oct-08

EB-47 . dihydrochloride . dihydrate
SYNONYMS	1-Piperazineacetamide,4-[1-(6-amino-9H-purin-9-yl)-1-deoxy-β-D-ribofuranuron]-N-(2,3-dihydro-1H-isoindol-4-yl)-1-one . 2HCl . 2H₂O
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-383-M001		1 mg	45.00 USD
ALX-270-383-M005		5 mg	180.00 USD

Product Specification

FORMULA:	C₂₄H₂₇N₉O₆ . 2HCl . 2H₂O
MW:	537.5 . 73.0 . 36.0
PURITY:	≥95% (HPLC)
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light. Packaged under inert gas.
HAZARD:	HARMFUL. MAY BE CARCINOGENIC.

Product Description

Very potent and water soluble PARP-1 inhibitor (IC₅₀=45nM, 100% inhibition at 200nM). Shows cytoprotective effects against oxidative damage in cells and in in vivo models of reperfusion injury and inflammation.

Product Specific Literature References

The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1): P.G. Jagtap, et al.; Bioorg. Med. Chem. Lett. 14, 81 (2004) Abstract
Substrate-assisted catalysis by PARP10 limits its activity to mono-ADP-ribosylation: H. Kleine, et al.; Mol. Cell 32, 57 (2008) Abstract

Further Categories Containing This Product:

DNA Repair Other Products

ALX-190-001

Revised 20-Jun-08

H-Trp-Glu-OH
SYNONYMS	H-WE-OH G3335
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	PARP Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-190-001-M050		50 mg	80.00 USD

Product Specification

FORMULA:	C₁₆H₁₉N₃O₅
MW:	333.3
CAS NUMBER:	36099-95-3
PURITY:	≥97%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water (50mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Cell permeable, s