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ALX-270-403 Revised 12-Jun-08
2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-403-M001   1 mg 115.00 USD Add To Cart
Product Specification
FORMULA: C20H10BrN3O2
MW: 404.2
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 2 months if stored at -20°C.
HANDLING: Packaged under inert gas. Protect from light. After reconstitution, prepare aliquots and store at -20°C.
HAZARD: TOXIC.
IDENTITY: Identity determined by NMR.

Product Description
Cell permeable, unsymmetrical compound that displays antiproliferative properties. Potent, selective and ATP-competitive inhibitor of CDK4/cyclin D1 (IC50=76nM), CDK2/cyclin E (IC50=520nM) and CDK1/cyclin B (IC50=2.1µM). Shows little activity towards CaMKII, PKA and GSK-3β (IC50>20µM).
Product Specific Literature References
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors: G. Zhu, et al.; J. Med. Chem. 46, 2027 (2003) Abstract
 
 
ALX-480-006 Revised 22-Oct-08
8-Bromoguanosine-3',5'-cyclic Monophosphate . sodium salt
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SYNONYMS 8-Br-cGMP . Na
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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ALX-480-006-M010   10 mg 48.00 USD Add To Cart
ALX-480-006-M050   50 mg 145.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O7P . Na
MW: 423.1 . 23.0
CAS NUMBER: 51116-01-9
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white powder.
PURITY DETAIL: Low in fluorescent and colored impurities.
SOLUBILITY: Soluble in water or aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by 1H-NMR, MS and UV.

Product Description
Activator of cGMP-dependent protein kinases (PKGs) 1α, 1β and type II and cGMP-gated ion channels (cGMP agonist). Has increased metabolic stability and membrane permeability compared to cGMP (Prod. No. ALX-480-059).
Product Specific Literature References
Sodium nitroprusside-induced protein phosphorylation in intact rat aorta is mimicked by 8-bromo cyclic GMP: R.M. Rapoport, et al.; PNAS 79, 6470 (1982) Abstract
The nitric oxide--cyclic GMP pathway and synaptic depression in rat hippocampal slices: C.L. Boulton, et al.; Eur. J. Neurosci. 6, 1528 (1994) Abstract
Nitric oxide in skeletal muscle: L. Kobzik, et al.; Nature 372, 546 (1994) Abstract
Nitric oxide. More jobs for that molecule: S. Snyder; Nature 372, 504 (1994) Abstract
Further Categories Containing This Product:
PKG Activators
 
 
ALX-480-026 Revised 03-Aug-06
8-Bromoguanosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . sodium salt (high purity)
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SYNONYMS Rp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Rp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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ALX-480-026-MC05   0.5 mg 90.00 USD Add To Cart
ALX-480-026-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O6PS . Na
MW: 439.2 . 23.0
CAS NUMBER: 150418-07-8
PURITY: ≥99% (HPLC)
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cGMP-dependent protein kinase (PKG) 1α and 1β. Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases; no metabolic side effects. Significantly more lipophilic and membrane permeant as compared to cyclic GMP (Prod. No. ALX-480-059) or Rp-cGMPS (Prod. No. ALX-480-072).
Product Specific Literature References
Nitric oxide regulates luteinizing hormone-releasing hormone secretion: M. Moretto, et al.; Endocrinology 133, 2399 (1993) Abstract
Role of guanylyl cyclase and cGMP-dependent protein kinase in long-term potentiation: M. Zhuo, et al.; Nature 368, 635 (1994) Abstract
Further Categories Containing This Product:
PKG Inhibitors
 
 
ALX-480-027 Revised 25-Jun-08
8-Bromoguanosine 3',5'-cyclic Monophosphothioate, Sp-Isomer . sodium salt (high purity)
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SYNONYMS Sp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Sp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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ALX-480-027-M001   1 mg 80.00 USD Add To Cart
ALX-480-027-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O6PS . Na
MW: 439.2 . 23.0
CAS NUMBER: 153660-03-8
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by MS, 1H-NMR and UV.

Product Description
Unspecific activator of both cGMP-dependent protein kinase (PKG) 1α and cAMP-dependent protein kinase (PKA). Resistant to cyclic nucleotide phosphodiesterases. Much more lipophilic and membrane permeant as compared to cyclic GMP (Prod. No. ALX-480-059) or Sp-cGMPS (Prod. No. ALX-480-073).
Product Specific Literature References
Evidence for two intracellular calcium pools in Dictyostelium: the cAMP- induced calcium influx is directed into a NBD-Cl- and 2,5-di-(tert- butyl)1,4-hydroquinone-sensitive pool: H. Flaadt, et al.; J. Cell Sci. 105, 1131 (1993) Abstract
Further Categories Containing This Product:
PKG Activators • PKA Activators
 
 
ALX-350-005 Revised 02-Oct-07
Bryostatin 1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-005-C010   10 µg 85.00 USD Add To Cart
Product Specification
FORMULA: C47H68O17
MW: 905.0
CAS NUMBER: 83314-01-6
MERCK INDEX: 14: 1457
PURITY: ≥97%
APPEARANCE: Colorless oil.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Store tightly sealed. Binds to glass and plastic surfaces in aqueous solutions.

Product Description
Binds to and activates protein kinase C (PKC). Antineoplastic.
Product Specific Literature References
Isolation and structure of Bryostatin 1: G.R. Pettit, et al.; J. Am. Chem. Soc. 104, 6846 (1982)
Bryostatin 1: differentiating agent from the depths: R.M. Stone; Leuk. Res. 21, 399 (1997) Abstract
Chemistry and clinical biology of the bryostatins: R. Mutter & M. Wills; Bioorg. Med. Chem. 8, 1841 (2000), (Review) Abstract
The clinical development of the bryostatins: A. Clamp and G.C. Jayson; Anticancer Drugs 13, 673 (2002) Abstract
The chemistry and biology of the bryostatin antitumour macrolides: K.J. Hale, et al.; Nat. Prod. Rep. 19, 413 (2002), Review Abstract
Bryostatin-1: pharmacology and therapeutic potential as a CNS drug: M.K. Sun & D.L. Alkon; CNS Drug Rev. 12, 1 (2006), Review Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Activators & Inducers) • PKC Activators • Natural Products - Immunomodulators • Natural Products - Antitumor Reagents • Marine Natural Products
 
 
ALX-350-246 Revised 07-Oct-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol. Specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Natural Products - Anti-inflammatory Agents • EGFR Kinase Inhibitors • Glutathione / Related Products • Chalcones • Phosphodiesterases / Related Products • Natural Products - Chemopreventive Agents • Glutathione S-Transferase • Sirtuins / Related Products • Natural Products - Antioxidants • IkB Kinases [IKKs] / Related Products
 
 
ALX-270-061 Revised 30-Oct-08
t-Butylhydroquinone
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SYNONYMS tBHQ
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+-ATPase / Related Products
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ALX-270-061-G010   10 g 30.00 USD Add To Cart
Product Specification
FORMULA: C10H14O2
MW: 166.2
CAS NUMBER: 1948-33-0
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
IDENTITY: Identity determined by IR.

Product Description
Inhibitor of the endoplasmic reticulum Ca2+-ATPase. Activates extracellular signal-regulated protein kinase 2 (ERK2).
Product Specific Literature References
Butylated hydroxyanisole and its metabolite tert-butylhydroquinone differentially regulate mitogen-activated protein kinases. The role of oxidative stress in the activation of mitogen-activated protein kinases by phenolic antioxidants: R. Yu, et al.; J. Biol. Chem. 272, 28962 (1997) Abstract; Full Text
Further Categories Containing This Product:
MAPK Pathway Activators
 
 
ALX-270-359 Revised 08-Dec-04
3-(3-tert-Butyl-4-methoxybenzylidenyl)indolin-2-one
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-270-359-M001   1 mg 50.00 USD Add To Cart
ALX-270-359-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C20H21NO2
MW: 307.4
CAS NUMBER: 293302-19-9
SOURCE/HOST: Synthetic.
PURITY: ≥98% (1H-NMR, HPLC)
APPEARANCE: Yellow crystals.
SOLUBILITY: Soluble in DMSO (>70mg/ml) or methanol (1.5mg/ml). Sparingly soluble in aqueous buffers (12.5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable as a powder for at least two years when stored at +4°C in the dark. Stock solutions made in DMSO should be stored in the dark and used within one month.
HANDLING: Protect from light. Keep cool and dry.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR, IR, ESI-MS and UV.

Product Description
Selective receptor tyrosine kinase (RTK) inhibitor. Inhibits HER-2 RTK (IC50 ~13µM) [1]. Consists predominantly of the E-isomer, contains ~10% of the Z-isomer [1].
Product Specific Literature References
[1] Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases: L. Sun, et al.; J. Med. Chem. 41, 2588 (1998) Abstract
 
 
ALX-350-250 Revised 22-Jul-08 New product
Butyrolactone I
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-250-C200   200 µg 135.00 USD Add To Cart
Product Specification
FORMULA: C24H24O7
MW: 424.5
CAS NUMBER: 87414-49-1
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable and selective inhibitor of the cyclin-dependent kinases CDK1/cyclin B, CDK2 and CDK5. Inhibits cell cycle progression at the G1/S and G2/M transitions. Blocks Fas-induced apoptosis. Displays antitumor activity.
Product Specific Literature References
Butyrolactone I, a selective inhibitor of cdk2 and cdc2 kinase: M. Kitagawa, et al.; Oncogene 8, 2425 (1993) Abstract
Inhibition of cell cycle oscillation of DNA replication by a selective inhibitor of the cdc2 kinase family, butyrolactone I, in Xenopus egg extracts: A. Someya, et al.; BBRC 198, 536 (1994) Abstract
A cyclin-dependent kinase inhibitor, butyrolactone I, inhibits phosphorylation of RB protein and cell cycle progression: M. Kitagawa, et al.; Oncogene 9, 2549 (1994) Abstract
Evidence for cdk5 as a major activity phosphorylating tau protein in porcine brain extract: T. Hosoi, et al.; J. Biochem. 117, 741 (1995) Abstract
Transcriptional activation of the cdc2 gene is associated with Fas- induced apoptosis of human hematopoietic cells: Y. Furukawa, et al.; J. Biol. Chem. 271, 28469 (1996) Abstract; Full Text
Antitumor effects of butyrolactone I, a selective cdc2 kinase inhibitor, on human lung cancer cell lines: K. Nishio, et al.; Anticancer Res. 16, 3387 (1996) Abstract
An exogenous cdk inhibitor, butyrolactone-I, induces apoptosis with increased Bax/Bcl-2 ratio in p53-mutated pancreatic cancer cells: M. Wada, et al.; Anticancer Res. 18, 2559 (1998) Abstract
Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi and A. Eskin; J. Neurochem. 72, 605 (1999) Abstract
Butyrolactone I induces cyclin B1 and causes G2/M arrest and skipping of mitosis in human prostate cell lines: M. Suzuki, et al.; Cancer Lett. 138, 121 (1999) Abstract
Butyrolactone I reversibly inhibits meiotic maturation of bovine oocytes, without influencing chromosome condensation activity: M. Kubelka, et al.; Biol. Reprod. 62, 292 (2000) Abstract; Full Text
Involvement of Cdk5/p25 in digoxin-triggered prostate cancer cell apoptosis: H. Lin, et al.; J. Biol. Chem. 279, 29302 (2004) Abstract; Full Text
Regulation of mitotic function of Chk1 through phosphorylation at novel sites by cyclin-dependent kinase 1 (Cdk1): T. Shiromizu, et al.; Genes Cells 11, 477 (2006) Abstract
 
 
ALX-202-026 Revised 30-Aug-07
Ca2+/Calmodulin-dependent Protein Kinase II (rat brain)
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SYNONYMS CaM Kinase II (rat brain)
CAMK2 (rat brain)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY CAM Kinases
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ALX-202-026-C001   1 µg 295.00 USD Add To Cart
Product Specification
MW: ~65kDa. Composed of 60kDa and 50kDa subunits in ratios of 1:3 to 1:4.
EC: 2.7.1.123
SOURCE/HOS