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Signal Transduction
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ALX-270-015 Revised 11-Jan-07
Leuhistin
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SYNONYMS (2R,3S)-3-Amino-2-hydroxy-2-(1H-imidazol-4-ylmethyl)-5-methylhexanoic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Aminopeptidases / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-015-M001   1 mg 50.00 USD Add To Cart
ALX-270-015-M005   5 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C11H19N3O3
MW: 241.3
CAS NUMBER: 129085-76-3
RTECS: NI8258000
SOURCE/HOST: Microbial product.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water, methanol, 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Inhibitor of aminopeptidase M.
Product Specific Literature References
Probestin, a new inhibitor of aminopeptidase M, produced by Streptomyces azureus MH663-2F6. I. Taxonomy, production, isolation, physico-chemical properties and biological activities: T. Aoyagi, et al.; J. Antibiot. (Tokyo) 43, 143 (1990) Abstract
Leuhistin, a new inhibitor of aminopeptidase M, produced by Bacillus laterosporus BMI156-14F1. I. Taxonomy, production, isolation, physico- chemical properties and biological activities: T. Aoyagi, et al.; J. Antibiot. (Tokyo) 44, 573 (1991) Abstract
Leuhistin, a new inhibitor of aminopeptidase M, produced by Bacillus laterosporus BMI156-14F1. II. Structure determination of leuhistin: S. Yoshida, et al.; J. Antibiot. (Tokyo) 44, 579 (1991) Abstract
Biosynthetic study of leuhistin, a new inhibitor of aminopeptidase M: S. Yoshida, et al.; J. Antibiot. (Tokyo) 44, 683 (1991) Abstract
Related Products
 
 
ALX-270-016 Revised 05-May-08
H-7 . dihydrochloride
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SYNONYMS (±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-016-M010   10 mg 60.00 USD Add To Cart
ALX-270-016-M025   25 mg 120.00 USD Add To Cart
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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
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SYNONYMS N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-017-M001   1 mg 22.00 USD Add To Cart
ALX-270-017-M005   5 mg 55.00 USD Add To Cart
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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-270-018 Revised 07-Dec-04
Tyrphostin AG 1288
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SYNONYMS α-Cyano-(3,4-dihydroxy-5-nitro)cinnamonitrile
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-018-M001   1 mg 40.00 USD Add To Cart
ALX-270-018-M005   5 mg 120.00 USD Add To Cart
ALX-270-018-M025   25 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C10H5N3O4
MW: 231.2
CAS NUMBER: 116313-73-6
PURITY: ≥98%
APPEARANCE: Orange solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Store tightly sealed in the dark. Protect from light.

 
 
ALX-270-019 Revised 27-Apr-06
Bisindolylmaleimide I . hydrochloride
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SYNONYMS GF-109203X . HCl
Gö 6850 . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-019-M001   1 mg 45.00 USD Add To Cart
ALX-270-019-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C25H24N4O2 . HCl
MW: 412.5 . 36.5
PURITY: ≥98%
APPEARANCE: Orange to red powder.
SOLUBILITY: Soluble in DMSO or methanol. Slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Water soluble form of bisindolylmaleimide I (Prod. No. ALX-270-049), a protein kinase C (PKC) inhibitor.
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991) Abstract; Full Text
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model: S. Kuchera, et al.; Agents Actions 39, C169 (1993) Abstract
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
 
 
ALX-270-020 Revised 07-Dec-04
Bisindolylmaleimide IX . methanesulfonate
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SYNONYMS Ro 31-8220 . methanesulfonate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-020-M001   1 mg 45.00 USD Add To Cart
ALX-270-020-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C25H23N5O2S . CH4O3S
MW: 457.6 . 96.1
CAS NUMBER: 138489-18-6
PURITY: ≥98%
APPEARANCE: Red solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective inhibitor of protein kinase C (PKC).
Product Specific Literature References
Atypical isoforms of pKc and insulin secretion from pancreatic beta- cells: evidence using Go 6976 and Ro 31-8220 as Pkc inhibitors: T.E. Harris, et al.; BBRC 227, 672 (1996) Abstract
 
 
ALX-270-022 Revised 09-Jan-08
AEBSF . hydrochloride
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SYNONYMS 4-(2-Aminoethyl)benzenesulfonylfluoride . HCl
Pefabloc®SC
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Proteases Other Products
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ALX-270-022-M050   50 mg 40.00 USD Add To Cart
ALX-270-022-M250   250 mg 145.00 USD Add To Cart
ALX-270-022-G001   1 g 360.00 USD Add To Cart
Product Specification
FORMULA: C8H10FNO2S . HCl
MW: 203.2 . 36.5
CAS NUMBER: 30827-99-7
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from moisture.

Product Description
Specific irreversible inhibitor of serine proteases including trypsin, chymotrypsin, plasmin, plasma kallikrein, and thrombin. Stable, non-toxic alternative to PMSF (Prod. No. ALX-270-184). Inhibitor of NAD(P)H oxidase. Activator of MAP kinases JNK and p38.
Product Specific Literature References
Irreversible enzyme inhibitors. 180. Irreversible inhibitors of the C'la component of complement derived from m-(phenoxypropoxy)benzamidine and phenoxyacetamide: B.R. Baker & H.J. Cory; J. Med. Chem. 14, 119 (1971) Abstract
Serine protease inhibitors block priming of monocytes for enhanced release of superoxide: P. Megyeri, et al.; Immunology 86, 629 (1995) Abstract; Full Text
Inhibition of amyloid beta-protein production in neural cells by the serine protease inhibitor AEBSF: M. Citron, et al.; Neuron 17, 171 (1996) Abstract
Lysis of leukemic cells by human macrophages: inhibition by 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), a serine protease inhibitor: Y. Nakabo & M.J. Pabst; J. Leukoc. Biol. 60, 328 (1996) Abstract; Full Text
Inhibition of NADPH oxidase activation by 4-(2-aminoethyl)-benzenesulfonyl fluoride and related compounds: V. Diatchuk, et al.; J. Biol. Chem. 272, 13292 (1997) Abstract; Full Text
4-(2-Aminoethyl)benzenesulfonyl fluoride attenuates tumor-necrosis-factor-alpha-induced blood-brain barrier opening: P. Megyeri, et al.; Eur. J. Pharmacol. 374, 207 (1999) Abstract
Evaluation of two inhibitors of invasion: LY311727 [3-(3-acetamide-1-benzyl-2-ethyl-indolyl-5-oxy)propane phosphonic acid] and AEBSF [4-(2-aminoethyl)-benzenesulphonyl fluoride] in acute murine toxoplasmosis: R. Buitrago-Rey, et al.; J. Antimicrob. Chemother. 49, 871 (2002) Abstract; Full Text
Heme oxygenase-1 gene activation by the NAD(P)H oxidase inhibitor 4-(2-aminoethyl) benzenesulfonyl fluoride via a protein kinase B, p38-dependent signaling pathway in monocytes: N. Wijayanti, et al.; J. Biol. Chem. 280, 21820 (2005) Abstract; Full Text
Inhibitory effect of 4-(2-aminoethyl)-benzenesulfonyl fluoride, a serine protease inhibitor, on PI3K inhibitor-induced CHOP expression: T. Hosoi, et al.; Eur. J. Pharmacol. 554, 8 (2007) Abstract
Further Categories Containing This Product:
Heme Oxygenase / Related Products • MAPK Pathway Activators • Cell Stress, Oxidative Stress & Redox Signalling Other Products • Fatty Acid Amide Hydrolase [FAAH] / Related Products
 
 
ALX-270-034 Revised 10-Jun-08
ODQ
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SYNONYMS 1H-[1,2,4]Oxadiazole[4,3-a]quinoxalin-1-one
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-034-M010   10 mg 46.00 USD Add To Cart
ALX-270-034-M050   50 mg 185.00 USD Add To Cart
Product Specification
FORMULA: C9H5N3O2
MW: 187.2
CAS NUMBER: 41443-28-1
PURITY: ≥98%
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in DMSO (5mg/ml), ethyl acetate or 100% ethanol (1.2mg/ml); insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Solutions may decompose slowly.
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Potent and selective inhibitor of nitric oxide (NO)-sensitive guanylyl cyclase.
Product Specific Literature References
Nitric oxide-dependent long-term potentiation is blocked by a specific inhibitor of soluble guanylyl cyclase: C.L. Boulton, et al.; Neuroscience 69, 699 (1995) Abstract
Novel guanylyl cyclase inhibitor, ODQ reveals role of nitric oxide, but not of cyclic GMP in endothelin-1 secretion: F. Brunner, et al.; FEBS Lett. 376, 262 (1995) Abstract
Potent and selective inhibition of nitric oxide-sensitive guanylyl cyclase by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one: J. Garthwaite, et al.; Mol. Pharmacol. 48, 184 (1995) Abstract
cGMP mediates the vascular and platelet actions of nitric oxide: confirmation using an inhibitor of the soluble guanylyl cyclase: M.A. Moro, et al.; PNAS 93, 1480 (1996) Abstract
Characterization of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one as a heme-site inhibitor of nitric oxide-sensitive guanylyl cyclase: A. Schrammel, et al.; Mol. Pharmacol. 50, 1 (1996) Abstract
The nitric oxide-cyclic GMP pathway and synaptic plasticity in the rat superior cervical ganglion: E. Southam, et al.; Br. J. Pharmacol. 119, 527 (1996) Abstract
A comparative study of the effects of three guanylyl cyclase inhibitors on the L-type Ca2+ and muscarinic K+ currents in frog cardiac myocytes: N. Abi-Gerges, et al.; Br. J. Pharmacol. 121, 1369 (1997) Abstract
Selective guanylyl cyclase inhibitor reverses nitric oxide-induced vasorelaxation: L.J. Olson, et al.; Hypertension 29, 254 (1997) Abstract
Effects of a novel inhibitor of guanylyl cyclase on dilator responses of mouse cerebral arterioles: C.G. Sobey & F.M. Faraci; Stroke 28, 837 (1997) Abstract
Comparison of two soluble guanylyl cyclase inhibitors, methylene blue and ODQ, on sodium nitroprusside-induced relaxation in guinea-pig trachea: T.L. Hwang, et al.; Br. J. Pharmacol 125, 1158 (1998) Abstract
Endothelial heme oxygenase-1 induction by hypoxia. Modulation by inducible nitric-oxide synthase and S-nitrosothiols: R. Motterlini, et al.; J. Biol. Chem. 275, 13613 (2000) Abstract; Full Text
 
 
ALX-270-035 Revised 07-Dec-04
Tyrphostin AG 1295
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SYNONYMS 6,7-Dimethyl-2-phenylquinoxaline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY