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Signal Transduction
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ALX-260-037 Revised 30-May-07
Calpain Inhibitor I
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SYNONYMS Ac-LL-Norleucinal
Ac-Leu-Leu-Nle-CHO
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-037-M010   10 mg 80.00 USD Add To Cart
ALX-260-037-M050   50 mg 310.00 USD Add To Cart
Product Specification
FORMULA: C20H37N3O4
MW: 383.5
CAS NUMBER: 110044-82-1
SOURCE/HOST: Synthetic.
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture.
Product Description
Inhibits calpain I (Ki=190nM), calpain II (Ki=220nM), cathepsin B (Ki=150nM) and cathepsin L (Ki=0.5nM). Inhibits neutral cysteine proteases and the proteasome. Protects against neuronal damage caused by hypoxia and ischemia. Inhibits apoptosis in thymocytes and metamyelocytes. Inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. Also prevents nitric oxide production by activated macrophages by interfering with the transcription of inducible nitric oxide synthase (iNOS; NOS II). Inhibits the proteolysis of IκB-α and IκB-β by the ubiquitin-proteasome complex.
Product Specific Literature References
Serine and cysteine proteinase inhibitors prevent nitric oxide production by activated macrophages by interfering with transcription of the inducible NO synthase gene: J.M. Griscavage, et al.; BBRC 215, 721 (1995) Abstract
Further Categories Containing This Product:
Proteasome / Related Products • Cathepsin Inhibitors • Proteases Other Products
 
 
ALX-260-038 Revised 15-Nov-05
Calpain Inhibitor II
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SYNONYMS Ac-LLM-CHO
Ac-Leu-Leu-Met-CHO
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-038-M010   10 mg 75.00 USD Add To Cart
ALX-260-038-M050   50 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C19H35N3O4S
MW: 401.6
CAS NUMBER: 110115-07-6
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light and moisture.
Product Description
Inhibitor of calpain I, calpain II, cathepsin B and cathepsin L.
Further Categories Containing This Product:
Cathepsin Inhibitors
 
 
ALX-260-014 Revised 19-Aug-08
Calpeptin
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SYNONYMS Z-Leu-norleucinal
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-014-M005   5 mg 85.00 USD Add To Cart
ALX-260-014-M010   10 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H30N2O4
MW: 362.5
CAS NUMBER: 117591-20-5
PURITY: ≥94% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 5mg/ml soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 2 months when stored at -20°C.
HANDLING: Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light and moisture.

Product Description
Membrane permeable inhibitor of calpain I and II and cathepsin L. Promotes neurite elongation in differentiating PC12 cells. Prevents Ca2+-ionophore induced degradation of actin binding protein and P235 in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin (Prod. No. ALX-450-006) or thrombin.
Product Specific Literature References
Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins: T. Sasaki, et al.; J. Enz. Inhib. 3, 195 (1990) Abstract
Cell-penetrating inhibitors of calpain: S. Mehdi; TIBS 16, 150 (1991) Abstract
Specificity of calcium-activated neutral proteinase (CANP) inhibitors for human mu CANP and mCANP: K. Saito and R.A. Nixon; Neurochem. Res. 18, 231 (1993) Abstract
Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells: M. Pinter, et al.; Neurosci. Lett. 170, 91 (1994) Abstract
Further Categories Containing This Product:
Cathepsin 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
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • PKA Inhibitors • PKC Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase Inhibitors • Ca2+ Channels (L-type) • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Antitumor Reagents • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-201-269 Revised 18-Mar-08
Calreticulin (rabbit) (recombinant)
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calreticulin / Related Products
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ALX-201-269-C025   25 µg 170.00 USD Add To Cart
Product Specification
SOURCE/HOST: Produced in E. coli.
CONCENTRATION: 1.2mg/ml
PURITY: ≥99%
FORMULATION: Liquid. In 100mM HEPES, pH 7.5, containing 150mM NaCl and 5mM CaCl2.
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -80°C
HANDLING: Avoid freeze/thaw cycles.
Product Specific Literature References
Delineation of the lectin site of the molecular chaperone calreticulin: S.P. Thomson and D.B. Williams; Cell Stress Chaperones 10, 242 (2005) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link P15253: Calreticulin (rabbit)
Further Categories Containing This Product:
Endoplasmatic Reticulum Stress • ER-Golgi Intermediate Compartment [ERGIC] / Related Products • Recombinant Proteins / Fusion Proteins
 
 
ALX-350-014 Revised 03-Apr-08
Calyculin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-014-C010   10 µg 65.00 USD Add To Cart
ALX-350-014-C025   25 µg 110.00 USD Add To Cart
ALX-350-014-C050   50 µg 190.00 USD Add To Cart
ALX-350-014-C100   100 µg 320.00 USD Add To Cart
Product Specification
FORMULA: C50H81N4O15P
MW: 1009.2
CAS NUMBER: 101932-71-2
SOURCE/HOST: Isolated from Discodermia calyx.
PURITY: ≥95%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetonitrile, chloroform, methylene chloride or benzene. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May by subject to isomerization when in solution. Biological activity is not affected by isomerization.
HANDLING: Protect from light and moisture.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Potent cell permeable inhibitor with high specificity for protein phosphatase 1 (PP1) and 2A (PP2A). Inhibits p130cas tyrosine phosphorylation. Enhances the phosphorylation level of NF-κB. Affects intracellular signalling processes that require 14-3-3. Potent non-phorbol type tumor promoter. Prevents γ-radiation induced apoptosis.
Product Specific Literature References
Okadaic acid: an additional non-phorbol-12-tetradecanoate-13-acetate- type tumor promoter: M. Suganuma, et al.; PNAS 85, 1768 (1988) Abstract
Protein phosphatases come of age: P.Cohen & P.T. Cohen; J. Biol. Chem. 264, 21435 (1989) Abstract; Full Text
Calyculin A and okadaic acid: inhibitors of protein phosphatase activity: H. Ishihara, et al.; BBRC 159, 871 (1989) Abstract
The structure and regulation of protein phosphatases: P. Cohen; Ann. Rev. Biochem. 58, 453 (1989) Abstract
Calyculin A, an inhibitor of protein phosphatases, a potent tumor promoter on CD-1 mouse skin: M. Suganuma, et al.; Cancer Res. 50, 3521 (1990) Abstract
Nonphorbol tumor promoters okadaic acid and calyculin-A induce membrane translocation of protein kinase C: R. Gopalakrishna; BBRC 189, 950 (1992) Abstract
Comparative effects of protein phosphatase inhibitors (okadaic acid and calyculin A) on human leukemia HL60, HL60/ADR and K562 cells: K. Sakurada, et al.; BBRC 187, 488 (1992) Abstract
Calyculin A, a potent inhibitor of phosphatases-1 and -2A, prevents apoptosis: Q. Song & M.F. Lavin; BBRC 190, 47 (1993) Abstract
Enhancement of AMPA-mediated synaptic transmission by the protein phosphatase inhibitor calyculin A in rat hippocampal slices: A. Figurov, et al.; Eur. J. Neurosci. 5, 1035 (1993) Abstract
Calyculin A, a non-phorbol ester type tumor promotor, induced oxidative DNA damage in stimulated human neutrophil-like cells: T. Takeuchi, et al.; BBRC 205, 1803 (1994) Abstract
Potassium and calcium channel involvement in induction of long-lasting synaptic enhancement by calyculin A, a protein phosphatase inhibitor, in rat hippocampal CA1 region: N. Murakami, et al.; Neurosci. Lett. 176, 181 (1994) Abstract
Differential toxicity of the protein phosphatase inhibitors microcystin and calyculin A: M.T. Runnegar, et al.; J. Pharmacol. Exp. Ther. 273, 545 (1995) Abstract
Inhibition of p130cas tyrosine phosphorylation by calyculin A: W. Qiu, et al.; J. Leukoc. Biol. 63, 631 (1998) Abstract
Unique features of the okadaic acid activity class of tumor promoters: H. Fujiki & M. Suganuma; J. Cancer Res. Clin. Oncol. 125, 150 (1999), Review Abstract
Calyculin A-induced vimentin phosphorylation sequesters 14-3-3 and displaces other 14-3-3 partners in vivo: G. Tzivion, et al.; J. Biol. Chem. 275, 29772 (2000) Abstract
Calyculin A induces apoptosis and stimulates phosphorylation of p65NF-kappaB in human osteoblastic osteosarcoma MG63 cells: H. Tanaka, et al.; Int. J. Oncol. 31, 389 (2007) Abstract
Further Categories Containing This Product:
PP2A / Related Products • PP1 / Related Products • Natural Products - Other Tumor Promoters • 14-3-3 Proteins / Related Products • Carcinogens & Tumor Promoters Other Products • NF-kB Pathway Modulators • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-201-224 Revised 22-Feb-06
cAMP-dependent Protein Kinase (Catalytic Subunit Cα) (mouse) (recombinant)
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SYNONYMS Protein Kinase A (Catalytic Subunit Cα) (mouse) (recombinant)
PKA (Catalytic Subunit Cα) (mouse) (recombinant)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-224-C025   25 µg 305.00 USD Add To Cart
ALX-201-224-C050   50 µg 474.00 USD Add To Cart
ALX-201-224-C100   100 µg 812.00 USD Add To Cart
Product Specification
MW: ~41kDa
SOURCE/HOST: Produced in E. coli.
CONCENTRATION:  
PURITY: ≥95% (SDS-PAGE)
FORMULATION: Liquid. In 25mM potassium phosphate, pH 6.5, containing 5mM β-mercaptoethanol, 5mM EDTA, 150mM NaCl and 50% glycerol.
SPECIFIC ACTIVITY: 1.5x107U/mg. One unit is defined as the amount of enzyme required to incorporate 1pmol phosphate per min into the specific substrate kemptide (Prod. No. ALX-160-006) at 30°C.
APPLICATION: - In vitro enzymological studies of neural and hormonal signal transduction
- Phosphorylation of target proteins in vivo (via microinjection) including ion channels, transcriptional activator proteins and regulatory enzymes of glycogen metabolism
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: -20°C
LONG TERM STORAGE: -80°C
USE/STABILITY: Stable for 6 months after receipt when stored at -20°C. Stable for 2 weeks when stored at +4°C.
HANDLING: Avoid freeze/thaw cycles.
Further Categories Containing This Product:
Enzymes • Recombinant Proteins / Fusion Proteins
 
 
ALX-201-229 Revised 15-May-07
cAMP-dependent Protein Kinase (Holoenzyme Type IIα, Cα2 (mouse)/RIIα2 (human)) (recombinant)
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SYNONYMS Protein Kinase A (Holoenzyme Type IIα, Cα2 (mouse)/RIIα2 (human)) (recombinant)
PKA (Holoenzyme Type IIα, Cα2 (mouse)/RIIα2 (human)) (recombinant)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-229-C020   20 µg 474.00 USD Add To Cart
ALX-201-229-C050   50 µg 812.00 USD Add To Cart
ALX-201-229-C100   100 µg 1'489.00 USD Add To Cart
Product Specification
MW: ~172kDa
SOURCE/HOST: Produced in E. coli.
CONCENTRATION: ~1mg/ml
FORMULATION: Liquid. In 20mM MOPS, pH 7.0, containing 150mM sodium chloride and 50% glycerol.
SPECIFIC ACTIVITY: 1.5x107U/mg (for the Cα catalytic subunit of the activated holoenzyme). One unit is defined as the amount of enzyme required to incorporate 1pmol phosphate per min into the specific substrate kemptide (Prod. No. ALX-160-006) at 30°C.
APPLICATION: Suitable for analyzing PKA type II agonists (cAMP analogs) or antagonists.
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: -20°C
LONG TERM STORAGE: -80°C
USE/STABILITY: Stable for at least 6 months after receipt when stored at -20°C.
HANDLING: Avoid freeze/thaw cycles.
Product Description
Inactive holoenzyme consisting of one dimeric human regulatory subunit type IIα and two monomeric mouse catalytic subunits. Activate by addition of the second messenger cAMP (Ka~100nM) (Prod. No. ALX-480-011) releasing two monomeric catalytic subunits.
Product Specific Literature References
[1] Assays of protein kinase: R. Roskoski, Jr.; Meth. Enzymol. 99, 3 (1983) Abstract
[2] PrKX is a novel catalytic subunit of the cAMP-dependent protein kinase regulated by the regulatory subunit type I: B. Zimmermann, et al.; J. Biol. Chem. 274, 5370 (1999) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION

Roskoski-Assay

Protein kinase activity may be measured by using a modified radioactive assay [1].
The assay is performed in a mixture containing 50mM MOPS, pH 7.0, 10mM MgCI2, 0.25mg/ml BSA, 100µM kemptide (peptide substrate), 100µM unlabeled ATP mixed with [γ-32p] ATP (500-1000cpm/pmol) in a final volume of 50µI. Reaction is started by addition of the Cα subunit from activated PKA holoenzyme, type IIα and can be stopped after a 5 min. incubation at 30°C by spotting the reaction mix onto Whatman® P-81 filters and soaking the filters four times in 75mM phosphoric acid (10ml per sample) for at least 5 min. After four washing steps rinse filters with ethanol, dry and count.
For the detection of phosphorylation in substrate proteins the phosphotransferase reaction can alternatively be stopped by taking aliquots of the mixture and adding SDS sample buffer. The phosphorylation status of the substrate proteins can subsequently be analysed using SDS PAGE and autoradiography [2].
Further Categories Containing This Product:
Enzymes • Recombinant Proteins / Fusion Proteins
 
 
ALX-201-225 Revised 26-Jul-05
cAMP-dependent Protein Kinase (Regulatory Subunit RIα) (bovine) (recombinant)
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SYNONYMS Protein Kinase A (Regulatory Subunit RIα) (bovine) (recombinant)
PKA (Regulatory Subunit RIα) (bovine) (recombinant)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-225-C025   25 µg 474.00 USD Add To Cart
ALX-201-225-C050   50 µg 812.00 USD Add To Cart
ALX-201-225-C100   100 µg 1'489.00 USD Add To Cart
Product Specification
MW: ~43kDa/subunit; homodimer
SOURCE