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ALX-270-270 Revised 17-Mar-08
Pifithrin-α . hydrobromide
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SYNONYMS 1-(4-Methylphenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)ethanone . HBr
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-270-M005   5 mg 50.00 USD Add To Cart
ALX-270-270-M010   10 mg 85.00 USD Add To Cart
ALX-270-270-M025   25 mg 200.00 USD Add To Cart
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Product Specification
FORMULA: C16H18N2OS . HBr
MW: 286.4 . 80.9
CAS NUMBER: 63208-82-2
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.
IDENTITY: Determined by 1H-NMR.

Product Description
Chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Reversibly blocks p53-dependent transcriptional activation and apoptosis.
Product Specific Literature References
Cancer research. A new way to combat therapy side effects: D. Ferber; Science 285, 1651 (1999) Abstract
A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy: P.G. Komarov, et al.; Science 285, 1733 (1999) Abstract
Suppression of p53: a new approach to overcome side effects of antitumor therapy: E.A. Komarova & A.V. Gudkov; Biochemistry (Mosc) 65, 41 (2000), (Review) Abstract; Full Text
Neurons are protected from excitotoxic death by p53 antisense oligonucleotides delivered in anionic liposomes: A. Lakkaraju, et al.; J. Biol. Chem. 276, 32000 (2001) Abstract; Full Text
Wild-type and mutated presenilins 2 trigger p53-dependent apoptosis and down-regulate presenilin 1 expression in HEK293 human cells and in murine neurons: C. Alves da Costa, et al.; PNAS 99, 4043 (2002) Abstract
Inactivation of p21WAF1 sensitizes cells to apoptosis via an increase of both p14ARF and p53 levels and an alteration of the Bax/Bcl-2 ratio: D. Javelaud & F. Besancon; J. Biol. Chem. 277, 37949 (2002) Abstract; Full Text
Transcription factor AP-2alpha triggers apoptosis in cardiac myocytes: F.U. Muller, et al.; Cell Death Differ. 11, 485 (2004) Abstract
Pifithrin-alpha inhibits p53 signaling after interaction of the tumor suppressor protein with hsp90 and its nuclear translocation: P.J. Murphy, et al.; J. Biol. Chem. 279, 30195 (2004) Abstract
 
 
ALX-270-287 Revised 26-Jun-08
Pifithrin-α (cyclic) . hydrobromide
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SYNONYMS 2-(4-Methylphenyl)imidazo[2,1-b]-5,6,7,8-tetrahydrobenzothiazole . HBr
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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ALX-270-287-M010   10 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C16H16N2S . HBr
MW: 268.4 . 80.9
CAS NUMBER: 60477-34-1
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (100mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and moisture. Keep under inert gas.

Product Description
Stable analog of pifithrin-α (Prod. No. ALX-270-270), with biological properties similar to its parent compound, but with reduced cytotoxicity. Inhibitor of p53. Reversibly inhibits p53-dependent transactivation of p53-responsive genes and reversibly blocks p53-mediated apoptosis. Potent STAT6 transcriptional inhibitor.
Product Specific Literature References
Cancer research. A new way to combat therapy side effects: D. Ferber; Science 285, 1651 (1999) Abstract
A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy: P.G. Komarov, et al.; Science 285, 1733 (1999) Abstract
Suppression of p53: a new approach to overcome side effects of antitumor therapy: E.A. Komarova, et al.; Biochemistry 65, 41 (2000) Abstract; Full Text
Pifithrin-alpha inhibits p53 signaling after interaction of the tumor suppressor protein with hsp90 and its nuclear translocation: P.J. Murphy, et al.; J Biol Chem 279, 30195 (2004) Abstract
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ALX-270-310 Revised 10-Jul-08
PRIMA-1
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SYNONYMS 2,2-bis(Hydroxymethyl)-3-quinuclidinone
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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ALX-270-310-M001   1 mg 23.00 USD Add To Cart
ALX-270-310-M005   5 mg 101.00 USD Add To Cart
Product Specification
FORMULA: C9H15NO3
MW: 185.2
CAS NUMBER: 5608-24-2
PURITY: ≥95%
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: 25mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; 2.5mg/ml soluble in PBS, pH 7.2 .
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Restores sequence-specific DNA binding and the active conformation to mutant p53 proteins in vitro and in vivo, thus triggering apoptosis of cancer cells.
Product Specific Literature References
Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound: V.J. Bykov, et al.; Nat. Med. 8, 282 (2002) Abstract
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers)
 
 
ALX-270-437 Revised 04-Jun-08
6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins/Related Products
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ALX-270-437-M001   1 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C13H13ClN2O
MW: 248.7
CAS NUMBER: 49843-98-3
PURITY: ≥95%
APPEARANCE: White to beige powder.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months when stored at -20°C in the dark.
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Specific cell permeable inhibitor. Potent cell permeable and metabolically stable specific inhibitor of hSIRT1 (IC50=98nM in vivo / IC50=38nM in vitro; compared to hSIRT2: IC50=19µM and hSIRT3: IC50=48µM) with no effect on human histone deacetylases (HDACs) class I and class II, nor NAD glycohydrolase (IC50>100µg). Inhibits the deacetylation of p53 (IC50=1µM).
Product Specific Literature References
Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1: A.D. Napper, et al.; J. Med. Chem. 48, 8045 (2005) Abstract
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes: J.C. Milne, et al.; Nature 450, 712 (2007) Abstract
Further Categories Containing This Product:
p53 Other Products
 
 
ALX-350-015 Revised 03-Apr-08
(S)-(+)-Camptothecin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-015-M050   50 mg 40.00 USD Add To Cart
ALX-350-015-M250   250 mg 150.00 USD Add To Cart
ALX-350-015-G001   1 g 295.00 USD Add To Cart
Product Specification
FORMULA: C20H16N2O4
MW: 348.4
CAS NUMBER: 7689-03-4
MERCK INDEX: 14: 1735
SOURCE/HOST: Isolated from Mappia foetida Miers (Nothapodytes foetida (Wt.) Sleumer).
PURITY: ≥98% (HPLC)
APPEARANCE: Pale yellow powder.
SOLUBILITY: Soluble in DMSO (10mg/ml), methanol (40mg/ml) or 0.1N sodium hydroxide (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture. After reconstitution, prepare aliquots and store at -20°C.
HAZARD: IRRITANT. TOXIC.

Product Description
Potent antitumor agent. Inhibitor of DNA-topoisomerase I. Activates p53 resulting in upregulated expression of TRAIL-R2 (DR5) and Bak to overcome TRAIL resistance in Bax-deficient human colon carcinoma cells. Suppresses nitric oxide (NO) biosynthesis.
Product Specific Literature References
M.E. Wall, et al.; JACS 88, 3888 (1966)
The current status of camptothecin analogues as antitumor agents: W.J. Slichenmyer, et al.; J. Natl. Cancer Inst. 85, 271 (1993), (Review) Abstract
RNA synthesis inhibitors increase melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; Mol. Brain Res. 23, 47 (1994) Abstract
Camptothecins: from bench research to hospital wards: M. Potmesil; Cancer Res. 54, 1431 (1994), (Review) Abstract
Forskolin and camptothecin induce a 30 kDa protein associated with melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; J. Neurosci. 15, 298 (1995) Abstract
Differential stabilization of eukaryotic DNA topoisomerase I cleavable complexes by camptothecin derivatives: A. Tanizawa, et al.; Biochemistry 34, 7200 (1995) Abstract
The anti-cancer drug camptothecin inhibits elongation but stimulates initiation of RNA polymerase II transcription: M. Ljungman & P.C. Hanawalt; Carcinogenesis 17, 31 (1996) Abstract
The cell cycle effects of camptothecin: Z. Darzynkiewicz, et al.; Ann. N. Y. Acad. Sci. 803, 93 (1996) Abstract
Camptothecin-induced apoptosis in p53-null human leukemia HL60 cells and their isolated nuclei: effects of the protease inhibitors Z-VAD-fmk and dichloroisocoumarin suggest an involvement of both caspases and serine proteases: T. Shimizu & Y. Pommier; Leukemia 11, 1238 (1997) Abstract
Camptothecin and taxol: discovery to clinic: M.E. Wall; Med. Res. Rev. 18, 299 (1998), Review Abstract
Camptothecin suppresses nitric oxide biosynthesis in RAW 264.7 macrophages: W.F. Chiou, et al.; Life Sci. 69, 625 (2001) Abstract
Reversal of multidrug resistance-associated protein-mediated daunorubicin resistance by camptothecin: D. Chauvier, et al.; J. Pharm. Sci. 91, 1765 (2002) Abstract
Camptothecin and taxol: historic achievements in natural products research: N.H. Oberlies & D.J. Kroll; J. Nat. Prod. 67, 129 (2004), Review Abstract
Camptothecin and its analogues: a review on their chemotherapeutic potential: D. Sriram, et al.; Nat. Prod. Res. 19, 393 (2005), Review Abstract
The effects of camptothecin on RNA polymerase II transcription: roles of DNA topoisomerase I:: G. Capranico, et al.; Biochimie 89, 482 (2007) Abstract
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Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Natural Products - Nitric Oxide Pathway Modulators • Natural Products - Antitumor Reagents • MDR Inhibitors • p53 Other Products • Alkaloids
 
 
ALX-430-128 Revised 21-Feb-08
Nutlin-3
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SYNONYMS (±)-4-[4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-piperazin-2-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-128-M001   1 mg 35.00 USD Add To Cart
ALX-430-128-M005   5 mg 160.00 USD Add To Cart
ALX-430-128-M025   25 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C30H30Cl2N4O4
MW: 581.5
CAS NUMBER: 548472-68-0
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO, dimethyl formamide or acetonitrile; sparingly soluble in a 1:10 solution of ethanol:PBS, pH 7.2.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at -20°C.

We do not recommend storing the aqueous solution for more than one day.
HAZARD: IRRITANT.

Product Description
Inhibitor of p53/MDM2 interaction (IC50=0.09µM).
Product Specific Literature References
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2: L.T. Vassilev, et al.; Science 303, 844 (2004) Abstract
Reactivation of the p53 pathway as a treatment modality for KSHV-induced lymphomas: G. Sarek, et al.; J. Clin. Invest. 117, 1019 (2007) Abstract; Full Text
General Literature References
Drug discovery and p53: D.P. Lane, et al.; Drug Discov. Today 8, 347 (2003) Abstract
Further Categories Containing This Product:
Ubiquitin Ligases [E3]
 
 
ALX-430-151 Revised 22-Jul-08
RITA
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SYNONYMS Reactivation of p53 and Induction of Tumor Cell Apoptosis
2,5-bis(5-Hydroxymethyl-2-thienyl)furan
NSC652287
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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ALX-430-151-M001   1 mg 75.00 USD Add To Cart
ALX-430-151-M005   5 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C14H12O3S2
MW: 292.4
CAS NUMBER: 213261-59-7
PURITY: ≥98%
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Soluble in 100% ethanol (1mg/ml), DMSO (20mg/ml), dimethyl formamide (30mg/ml); 0.5mg/ml soluble in a 1:1 solution of dimethyl formamide: PBS (pH 7.2) (dilute the dimethyl formamide solution with PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least two years after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Inhibitor of p53/HDM2 interaction. Activator of p53 function in tumors. Potently inhibits the growth of a variety of  cancer cell lines in the submicromolar range. It has been suggested that RITA selectively targets cells expressing p53 by other mechanisms than direct binding to the N-terminal domain of p53 [4].
Product Specific Literature References
[1] DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells: W. Nieves-Neira, et al.; Mol. Pharmacol. 56, 478 (1999) Abstract; Full Text
[2] Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism: M.I. Rivera, et al.; Biochem. Pharmacol. 57, 1283 (1999) Abstract
[3] Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors: N. Issaeva, et al.; Nat. Med. 10, 1321 (2004) Abstract
[4] NMR indicates that the small molecule RITA does not block p53-MDM2 binding in vitro: M. Krajewski, et al.; Nat. Med. 11, 1135 (2005) Abstract
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers)
 
 
ALX-201-221 Revised 02-Oct-06
Pin1 (human) (recombinant)
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SYNONYMS Peptidyl-prolyl cis-trans Isomerase Pin1 (human) (recombinant)
PPIase Pin1 (human) (recombinant)
Peptidyl-prolyl cis-trans Isomerase NIMA-interacting 1 (human) (recombinant)
PPIase NIMA-interacting 1 (human) (recombinant)
Rotamase Pin1 (human) (recombinant)
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Alzheimer Research Other Products
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ALX-201-221-C100   100 µg 325.00 USD Add To Cart
Product Specification
MW: ~18.2kDa
SOURCE/HOST: Recombinant human peptidyl-prolyl cis-trans isomerase (PPIase) Pin1 produced in E. coli.
CONCENTRATION: 1mg/ml
PURITY: ≥95% (SDS-PAGE)
FORMULATION: Liquid. In 20mM TRIS-HCl, pH 7.5, containing 100mM sodium chloride, 5mM DTT and 20% glycerol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
Further Categories Containing This Product:
Stress & Heat Shock Proteins Other Products • Recombinant Proteins/Fusion Proteins • Antiviral Signalling/Related Products • p53 Other Products
 
 
ALX-201-426 Revised 24-Jul-08 New product
Sirtuin 1 (human) (recombinant) (His)
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SYNONYMS Sirt1 (human) (recombinant) (His)
SIR2-like Protein 1 (human) (recombinant) (His)
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins/Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-426-C010   10 µg 300.00 USD Add To Cart
ALX-201-426-C050   50 µg 470.00 USD Add To Cart
Product Specification
SOURCE/HOST: Produced in E. coli. The mature peptide of human sirtuin 1 (aa 2-555) is fused at the N-terminus to a His-tag.
PURITY: ≥90% (SDS-PAGE)
FORMULATION: Liquid. 0.2μm-filtered solution in 55mM TRIS-Cl, pH 8.2, containing 150mM sodium chloride.
ENDOTOXIN CONTENT: <1EU/µg protein (LAL-test).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Working aliquots are stable for up to 3 months when stored at -20°C.
HANDLING: Avoid freeze/thaw cycles. After opening, prepare aliquots and store at -20°C.
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General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link Q96EB6: SIRT1 (human)
MANUFACTURER Manufactured by AdipoGen, Inc.
Related Products
Further Categories Containing This Product:
Recombinant Proteins/Fusion Proteins • NAD+ Metabolism/Related Products • p53 Other Products
 
 
ALX-201-430 Revised 12-Aug-08 New product
Sirtuin 2 (human) (recombinant) (His)