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PKA Inhibitors
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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
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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 InhibitorsPKC InhibitorsCasein Kinase InhibitorsPKG Inhibitors
 
 
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-151-016 Revised 17-Jan-05
cAMP-dependent Protein Kinase Inhibitor (5-22) amide
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SYNONYMS PKA Inhibitor (5-22) amide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-151-016-MC05   0.5 mg 110.00 USD Add To Cart
ALX-151-016-M001   1 mg 180.00 USD Add To Cart
Product Specification
SEQUENCE: H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-NH2
FORMULA: C84H137N29O26
MW: 1969.2
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Potent inhibitor of cAMP-dependent protein kinase (PKA).
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase: H.-C. Cheng, et al.; J. Biol. Chem. 261, 989 (1986) Abstract; Full Text
Primary structural determinants essential for potent inhibition of cAMP- dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitor protein: D.B. Glass, et al.; J. Biol. Chem. 264, 8802 (1989) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-151-014 Revised 15-Dec-04
cAMP-dependent Protein Kinase Inhibitor (5-24)
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SYNONYMS PKA Inhibitor (5-24)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-151-014-MC05   0.5 mg 90.00 USD Add To Cart
ALX-151-014-M001   1 mg 160.00 USD Add To Cart
Product Specification
SEQUENCE: H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-OH
FORMULA: C94H148N32O31
MW: 2222.4
PURITY: ≥97%
APPEARANCE: White to off-white powder.
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in water or 5 % acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.
Product Description
Potent inhibitor of cAMP-dependent protein kinase (PKA). The peptide corresponds to the active site of the skeletal muscle inhibitor protein.
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase: H.-C. Cheng, et al.; J. Biol. Chem. 261, 989 (1986) Abstract; Full Text
Phosphorylation of Avena phytochrome in vitro as a probe of light- induced conformational changes: Y.S. Wong, et al.; J. Biol. Chem. 261, 12089 (1986) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-151-018 Revised 13-Feb-06
cAMP-dependent Protein Kinase Inhibitor (5-24) amide
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SYNONYMS PKA Inhibitor (5-24) amide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-151-018-MC05   0.5 mg 90.00 USD Add To Cart
ALX-151-018-M001   1 mg 160.00 USD Add To Cart
Product Specification
SEQUENCE: H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-NH2
FORMULA: C94H149N33O30
MW: 2221.4
PURITY: ≥97%
APPEARANCE: White to off-white lyophilized powder.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase: H.-C. Cheng, et al.; J. Biol. Chem. 261, 989 (1986) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-151-017 Revised 15-Dec-04
cAMP-dependent Protein Kinase Inhibitor (14-24) amide
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SYNONYMS PKA Inhibitor (14-24) amide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-151-017-M001   1 mg 90.00 USD Add To Cart
ALX-151-017-M005   5 mg 360.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-NH2
FORMULA: C49H86N24O15
MW: 1251.4
PURITY: ≥97%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Further Categories Containing This Product:
Peptides
 
 
ALX-151-021 Revised 14-Aug-02
H-Arg-Gly-Tyr-Ser-Leu-Gly-OH
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-151-021-M001   1 mg 40.00 USD Add To Cart
ALX-151-021-M005   5 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C28H45N9O9
MW: 651.7
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Synthetic hexapeptide substrates and inhibitors of 3':5'-cyclic AMP- dependent protein kinase: B.E. Kemp, et al.; PNAS 73, 1038 (1976) Abstract
Synthetic peptide substrates of the cAMP-dependent protein kinase: B.E. Kemp, et al.; Fed. Proc. 35, 1384 (1976)
Further Categories Containing This Product:
Peptides
 
 
ALX-480-024 Revised 18-Jun-08
8-Bromoadenosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . sodium salt
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SYNONYMS Rp-8-Br-cAMPS . Na
8-Br-cAMPS . Na, Rp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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ALX-480-024-MC05   0.5 mg 95.00 USD Add To Cart
ALX-480-024-M001   1 mg 175.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O5PS . Na
MW: 423.2 . 23.0
CAS NUMBER: 129735-00-8
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 250 mM soluble in water, aqueous solutions, DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions should be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.
IDENTITY: Identity determined by 1H-NMR, MS and UV.

Product Description
Inhibitor of cAMP-dependent protein kinase (PKA), preferentially binding to type I PKA. Lipophilic analog of Rp-cAMPS (Prod. No. ALX-480-012, and Prod. No. ALX-480-085). Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases. Significantly more lipophilic and membrane permeant as compared to Rp-cAMPS or 8-Br-cAMP (Prod. No. ALX-480-007).
Product Specific Literature References
Activation of intestinal CFTR Cl- channel by heat-stable enterotoxin and guanylin via cAMP-dependent protein kinase: A.C. Chao, et al.; EMBO J. 13, 1065 (1994) Abstract
Novel (Rp)-cAMPS analogs as tool for inhibition of cAMP-kinase in cell culture: B.T. Gjertsen, et al.; J. Biol. Chem. 270, 20599 (1995) Abstract; Full Text
Further Categories Containing This Product:
PKA Inhibitors
 
 
ALX-350-027 Revised 19-Aug-08
Calphostin C
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SYNONYMS UCN-1028C
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-027-C100   100 µg 85.00 USD Add To Cart
ALX-350-027-M001   1 mg 595.00 USD Add To Cart
Product Specification
FORMULA: C44H38O14
MW: 790.8
CAS NUMBER: 121263-19-2
SOURCE/HOST: Isolated from Cladosporium cladosporioides MST-FP1798.
PURITY: ≥95% (HPLC)
APPEARANCE: Dark red solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for 3 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
Potent and selective inhibitor of the protein kinase C (PKC) regulatory site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G and pp60v-src protein tyrosine kinase. Induces apoptotic DNA fragmentation and cell death. Kills breast cancer cells. Has antiviral potential. Inhibits cardiac L-type Ca2+ channels.
Product Specific Literature References
Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C: E. Kobayashi, et al.; BBRC 159, 548 (1989) Abstract
Potent and specific inhibitors of protein kinase C of microbial origin: T. Tamaoki and H. Nakano; Biotechnology 8, 732 (1990) Abstract
Inhibition of protein kinase C by calphostin C is light-dependent: R.F. Bruns, et al.; BBRC 176, 288 (1991) Abstract
Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C: R. Gopalakrishna, et al.; FEBS Lett. 314, 149 (1992) Abstract
Calphostin C, a specific protein kinase C inhibitor, activates human neutrophils: effect on phospholipase A2 and aggregation: S. Svetlov and S. Nigam; Biochim. Biophys. Acta 1177, 75 (1993) 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
Growth inhibition of herpes simplex virus-type 1 in calphostin C-treated astrocytes: C.G. Castagnino, et al.; Intervirology 38, 332 (1995) Abstract
Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels: H.C. Hartzell & A. Rinderknecht; Am. J. Physiol. 270, C1293 (1996) Abstract
Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity: C.L. Chen, et al.; Pharm. Res. 16, 1003 (1999) Abstract
Potent killing of paclitaxel- and doxorubicin-resistant breast cancer cells by calphostin C accompanied by cytoplasmic vacuolization: B. Guo, et al.; Breast Cancer Res. Treat. 82, 125 (2003) Abstract
 
 
ALX-270-281 Revised 28-Sep-06
Daphnetin
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SYNONYMS 7,8-Dihydroxycoumarin
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-281-M005   5 mg 25.00 USD