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Serine / Threonine Kinases / Related Products
You are here: Product Lines > Signal Transduction > Kinases / Related Products > Serine / Threonine Kinases / Related Products
 
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ALX-270-039 Revised 15-Nov-06
A-3 . hydrochloride
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SYNONYMS N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-039-M010   10 mg 65.00 USD Add To Cart
ALX-270-039-M050   50 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C12H13ClN2O2S . HCl
MW: 284.8 . 36.5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.
Product Specific Literature References
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Casein Kinase Inhibitors
 
 
ALX-480-011 Revised 17-Jan-05
Adenosine 3',5'-cyclic Monophosphate . sodium salt
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SYNONYMS Cyclic AMP . Na
cAMP . Na
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-011-M100   100 mg 38.00 USD Add To Cart
ALX-480-011-M250   250 mg 70.00 USD Add To Cart
ALX-480-011-G001   1 g 195.00 USD Add To Cart
Product Specification
FORMULA: C10H11N5O6P . Na
MW: 328.2 . 23.0
CAS NUMBER: 37839-81-9
MERCK INDEX: 14: 2708
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Key regulator of many cellular reactions. Naturally occurring activator of cAMP-dependent protein kinase (PKA).
Product Specific Literature References
TGF-beta 1 and cyclic AMP promote apoptosis in resting human B lymphocytes: J. Lomo, et al.; J. Immunol. 154, 1634 (1995) Abstract
Further Categories Containing This Product:
PKA Activators
 
 
ALX-480-085 Revised 05-Sep-07
Adenosine-3’,5’-cyclic Monophosphothioate, Rp-Isomer . sodium salt
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SYNONYMS Rp-cAMPS . Na
cAMPS . Na, Rp-Isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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ALX-480-085-M001   1 mg 120.00 USD Add To Cart
ALX-480-085-M005   5 mg 490.00 USD Add To Cart
Product Specification
FORMULA: C10H11N5NaO5PS
MW: 367.3
CAS NUMBER: 73208-40-9
PURITY: ≥99% (low adenosine, cAMP and Sp-cAMPS content)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water or aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
For application and literature references see the triethylammonium salt (Prod. No. ALX-480-012).
Further Categories Containing This Product:
PKA Inhibitors
 
 
ALX-480-012 Revised 27-Apr-06
Adenosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . triethylammonium salt
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SYNONYMS Rp-cAMPS . TEA
cAMPS . TEA, Rp-Isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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ALX-480-012-M001   1 mg 110.00 USD Add To Cart
ALX-480-012-M005   5 mg 460.00 USD Add To Cart
Product Specification
FORMULA: C10H12N5O5PS . C6H16N
MW: 345.5 . 101.0
CAS NUMBER: 151837-09-1
PURITY: ≥99%
APPEARANCE: White lyophilized solid.
SOLUBILITY: Soluble in water
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Competitive inhibitor of protein cAMP-dependent protein kinase type I and II (cAMP antagonist). Resistant against mammalian cyclic nucleotide-dependent phosphodiesterases. Significantly more lipophilic as compared to cAMP and thus membrane permeable in many biological systems.
Product Specific Literature References
A mechanistic and kinetic analysis of the interactions of the diastereoisomers of adenosine 3',5'-(cyclic)phosphorothioate with purified cyclic AMP-dependent protein kinase: J.D. Rothermel; Biochem. J. 251, 757 (1988) Abstract
Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3',5'-cyclic phosphorothioates: W.R.G. Dostmann, et al.; J. Biol. Chem. 265, 10484 (1990) Abstract; Full Text
Inhibition of cGMP-dependent protein kinase by (Rp)-guanosine 3',5'- monophosphorothioates: E. Butt, et al.; FEBS Lett. 263, 47 (1990) Abstract
Regulation of kainate receptors by cAMP-dependent protein kinase and phosphatases: L.Y. Wang, et al.; Science 253, 1132 (1991) 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
Further Categories Containing This Product:
PKA Inhibitors
 
 
ALX-480-086 Revised 30-Aug-06
Adenosine 3',5'-cyclic Monophosphothioate, Sp-Isomer . sodium salt
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SYNONYMS Sp-cAMPS . Na
cAMPS . Na, Sp-Isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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ALX-480-086-M001   1 mg 75.00 USD Add To Cart
ALX-480-086-M005   5 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C10H11N5NaO5PS
MW: 367.3
CAS NUMBER: 717794-13-5
PURITY: ≥99% (low adenosine, cAMP and Rp-cAMPS content)
APPEARANCE: White to off-white lyophilized powder.
SOLUBILITY: Soluble in water or aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
For application and literature references see the triethylammonium salt (Prod. No. ALX-480-013).
Further Categories Containing This Product:
PKA Activators
 
 
ALX-480-013 Revised 10-Feb-05
Adenosine 3',5'-cyclic Monophosphothioate, Sp-Isomer . triethylammonium salt
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SYNONYMS Sp-cAMPS . TEA
cAMPS . TEA, Sp-Isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-013-M001   1 mg 75.00 USD Add To Cart
ALX-480-013-M005   5 mg 298.00 USD Add To Cart
ALX-480-013-M010   10 mg 580.00 USD Add To Cart
Product Specification
FORMULA: C16H27N6O5PS
MW: 446.5
CAS NUMBER: 93602-66-5
PURITY: ≥99%
APPEARANCE: White lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Activator of cAMP-dependent protein kinase (PKA) (cAMP agonist). Considerably higher resistance against cyclic nucleotide-dependent phosphodiesterases as compared to N6,O2'-dibutyryladenosine 3',5'-cyclic monophosphate (dibutyryl-cAMP) (Prod. No. ALX-480-045) or 8-bromoadenosine-3',5'-cyclic monophosphate (8-Br-cAMP) (Prod. No. ALX-480-007). No metabolic side effects. Membrane permeable in many biological systems.
Product Specific Literature References
Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3',5'-cyclic phosphorothioates: W.R.G. Dostmann, et al.; J. Biol. Chem. 265, 10484 (1990) Abstract; Full Text
Cyclic AMP antagonist Rp-cAMPS inhibits amylase exocytosis from saponin- permeabilized parotid acini: T. Takuma & T. Ichida; J. Biochem. 110, 292 (1991) Abstract
Second messenger signaling in the regulation of cytosolic pH and DNA synthesis by parathyroid hormone (PTH) and PTH-related peptide in osteoblastic osteosarcoma cells: role of Na+/H+ exchange: T. Sugimoto, et al.; J. Cell Physiol. 152, 28 (1992) Abstract
The activation of cAMP-dependent protein kinase is directly linked to the stimulation of bone resorption by parathyroid hormone: H. Kaji, et al.; BBRC 182, 1356 (1992) Abstract
Intracellular cyclic AMP not calcium, determines the direction of vesicle movement in melanophores: direct measurement by fluorescence ratio imaging: P.J. Sammak, et al.; J. Cell. Biol. 117, 57 (1992) Abstract
Effects of activators and inhibitors of protein kinase A on increases in quantal size at the frog neuromuscular junction: W. Van Der Kloot & D.D. Branisteanu; Pfluegers Arch. 420, 336 (1992) Abstract
Further Categories Containing This Product:
PKA Activators
 
 
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
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-270-448 Revised 24-Jul-06
ALK5 Inhibitor I
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SYNONYMS TGF-β RI Kinase Inhibitor I
3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
PRODUCT LINE Chemokines & Cytokines
PRODUCT CATEGORY Transforming Growth Factor beta [TGFbeta] & Receptors / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-448-M001   1 mg 30.00 USD Add To Cart
ALX-270-448-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H12N4
MW: 272.3
PURITY: ≥97% (1H-NMR)
APPEARANCE: Yellow to brown solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description

Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=51nM). Displays ~15-fold greater selectivity over p38α MAPK (IC50=740nM). Inhibits TGF-β-dependent cellular growth (IC50=89nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC50=47nM in mink lung cells).
Product Specific Literature References
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain: J.S. Sawyer, et al.; J. Med. Chem. 46, 3953 (2003) Abstract
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI): J. Singh, et al.; Bioorg. Med. Chem. Lett. 13, 4355 (2003) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors
 
 
ALX-270-445 Revised 20-Jul-06
ALK5 Inhibitor II
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SYNONYMS TGF-β RI Kinase Inhibitor II
2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
PRODUCT LINE Chemokines & Cytokines
PRODUCT CATEGORY Transforming Growth Factor beta [TGFbeta] & Receptors / Related Products
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ALX-270-445-M001   1 mg 60.00 USD Add To Cart
ALX-270-445-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C17H13N5
MW: 287.3
PURITY: ≥97% (1H-NMR)
APPEARANCE: Yellow solid.
SOLUBILITY: 5mg/ml soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=23nM, 4nM and 18nM for binding, auto-phosphorylation and cellular assay in HepG2 cells of TGF-β RI kinase, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK (IC50>16µM).
Product Specific Literature References
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors: F. Gellibert, et al.; J. Med. Chem. 47, 4494 (2004) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors
 
 
ALX-270-386 Revised 24-Feb-05
Aloisine
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SYNONYMS RP106
7-n-Butyl-6-(4-methoxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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Product Numbers:</