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Calmodulin Inhibitors
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Items 18 of 18
ALX-430-026 Revised 12-Sep-06
Calmidazolium chloride
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SYNONYMS 1-[bis(p-Chlorophenyl)methyl]-3-[2,4-dichloro-β-(2,4-dichlorobenzyloxy)phenethyl] imidazolium chloride
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-026-M010   10 mg 85.00 USD Add To Cart
ALX-430-026-M050   50 mg 340.00 USD Add To Cart
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Product Specification
FORMULA: C31H23Cl7N2O
MW: 687.7
CAS NUMBER: 57265-65-3
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in methanol, 100% ethanol, chloroform, DMSO or propylene glycol; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Calmodulin antagonist. At least 150 times more potent than trifluoperazine (Prod. No. ALX- 550-310) as an inhibitor of brain calmodulin-dependent phosphodiesterase. Inhibitor of voltage-gated Ca2+ channels. Blocks Ca2+-calmodulin binding to NOS.
Product Specific Literature References
Inhibitors of calmodulin impair the constitutive but not the inducible nitric oxide synthase activity in the rat aorta: V.B. Schini & P.M. Vanhoutte; J. Pharmacol. Exp. Ther. 261, 553 (1992) Abstract
Calmidazolium, a calmodulin inhibitor, inhibits endothelium-dependent relaxations resistant to nitro-L-arginine in the canine coronary artery: S. Illiano, et al.; Br. J. Pharmacol. 107, 387 (1992) Abstract
The calmodulin antagonist calmidazolium stimulates release of nitric oxide in neuroblastoma N1E-115 cells: J. Hu & E.E. el-Fakahany; Neuroreport 4, 198 (1993) Abstract
Vasoactive intestinal peptide/pituitary adenylate cyclase-activating peptide-dependent activation of membrane-bound NO synthase in smooth muscle mediated by pertussis toxin-sensitive Gi1-2: K.S. Murthy & G.M. Makhlouf; J. Biol. Chem. 269, 15977 (1994) Abstract
Mitochondrial nitric oxide synthase is constitutively active and is functionally upregulated in hypoxia: Z. Lacza, et al.; Free Radic. Biol. Med. 31, 1609 (2001) Abstract
Mitochondrial calcium uptake stimulates nitric oxide production in mitochondria of bovine vascular endothelial cells: E.N. Dedkova, et al.; Am. J. Physiol. Cell Physiol. 286, C406 (2004) Abstract; Full Text
Neural tube closure depends on nitric oxide synthase activity: A. Nachmany, et al.; J. Neurochem. 96, 247 (2006) Abstract
Further Categories Containing This Product:
NOS Other Products • Ca2+ Channels (L-type) • Phosphodiesterases / Related Products
 
 
ALX-270-171 Revised 30-Jun-08
Chlorpromazine . hydrochloride
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SYNONYMS 2-Chloro-10-(3-dimethylaminopropyl)phenothiazine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-270-171-G001   1 g 22.00 USD Add To Cart
ALX-270-171-G005   5 g 66.00 USD Add To Cart
Product Specification
FORMULA: C17H19ClN2S . HCl
MW: 318.9 . 36.5
CAS NUMBER: 69-09-0
MERCK INDEX: 14: 2185
RTECS: SO1750000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Not stable in aqueous solution. We strongly recommend always to use freshly prepared solutions.
HANDLING: Protect from light.
HAZARD: VERY TOXIC.

Product Description
Inhibits calmodulin stimulation of cyclic nucleotide phosphodiesterase. Dopamine antagonist. D2 antagonist. H1 antagonist. Inhibits TNF-α production. Potent PLA2 inhibitor. Inhibits nitric oxide synthase (NOS) in mouse brain and prevents lipopolysaccharide induction of NOS in mouse lung. Antipsychotic.
Product Specific Literature References
Chlorpromazine as a substitute for ortho-dianisidine and ortho-tolidine in the determination of chlorine, hemoglobin, and peroxidase activity: H.B. Collier; Clin. Biochem. 7, 331 (1974) Abstract
Drug-protein interactions: binding of chlorpromazine to calmodulin, calmodulin fragments, and related calcium binding proteins: D.R. Marshak, et al.; Biochemistry 24, 144 (1985) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Chlorpromazine inhibits both the constitutive nitric oxide synthase and the induction of nitric oxide synthase after LPS challenge: M. Palacios, et al.; BBRC 196, 280 (1993) Abstract
Protective effect of calmodulin inhibitors against acute cyanide- induced lethality and convulsions in mice: H. Yamamoto; Toxicol. Lett. 66, 73 (1993) Abstract
Pharmacologic inhibitors of tumor necrosis factor production exert differential effects in lethal endotoxemia and in infection with live microorganisms in mice: M.G. Netea, et al.; J. Infect. Dis. 171, 393 (1995) Abstract
Pharmacological regulation of mitochondrial nitric oxide synthase: A. Boveris, et al.; Methods Enzymol. 359, 328 (2002) Abstract
Brain mitochondrial nitric oxide synthase: in vitro and in vivo inhibition by chlorpromazine: S. Lores-Arnaiz, et al.; Arch. Biochem. Biophys. 430, 170 (2004) Abstract
Further Categories Containing This Product:
Phosphodiesterases / Related Products • TNF-alpha & TNF Receptors Other Products • Chemopreventive Agents Other Products • NOS Inhibitors (NOS Induction & Enzyme Activity) • PLA2 Inhibitors • Dopaminergics & Dopamine Receptors / Related Products
 
 
ALX-420-008 Revised 04-Dec-07
Compound 48/80 . trihydrochloride
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-420-008-M100   100 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C32H46N3O3 . 3HCl
MW: 520.7 . 109.4
CAS NUMBER: 94724-12-6
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (100mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HAZARD: TOXIC.

Product Description
Oligomeric mixture of condensation products of N-methyl-p-methoxyphenethylamine and formaldehyde. The trimer is the most abundant oligomere in the mixture. Blocks calmodulin and human platelet phospholipase C and ADP ribosylation. Activates G-proteins in a manner similar to G-protein-coupled receptors.
Product Specific Literature References
Activation of bovine rod outer segment phosphatidylinositol-4,5- bisphosphate phospholipase C by calmodulin antagonists does not depend on calmodulin: B.D. Gehm, et al.; Biochemistry 30, 11302 (1991) Abstract
Biscoclaurine alkaloids inhibit receptor-mediated phospholipase A2 activation probably through uncoupling of a GTP-binding protein from the enzyme in rat peritoneal mast cells: S. Akiba, et al.; Biochem. Pharmacol. 44, 45 (1992) Abstract
Phosphorylation of smg p21B in rat peritoneal mast cells in association with histamine release inhibition by dibutyryl-cAMP: K. Izushi, et al.; FEBS Lett. 314, 241 (1992) Abstract
ADP-ribosylation of rho proteins is inhibited by melittin, mast cell degranulating peptide and compound 48/80: G. Koch, et al.; Eur. J. Pharmacol. 226, 87 (1992) Abstract
Activation of the Na+/K(+)-pump in rat peritoneal mast cells following histamine release: a possible role in cell recovery: T. Knudsen, et al.; Br. J. Pharmacol. 108, 120 (1993) Abstract
Eclosion hormone activates phosphatidylinositol hydrolysis in silkworm abdominal ganglia during adult metamorphosis: Y. Shibanaka, et al.; Eur. J. Biochem. 211, 427 (1993) Abstract
Further Categories Containing This Product:
Phospholipase C / Related Products • G-proteins & GTPases Other Products
 
 
ALX-270-208 Revised 04-Feb-05
J-8 . hydrochloride
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SYNONYMS (N-8-Aminooctyl)-5-iodo-1-naphthalenesulfonamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-270-208-M005   5 mg 35.00 USD Add To Cart
ALX-270-208-M025   25 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C18H25IN2O2S . HCl
MW: 460.4 . 36.5
APPEARANCE: Off-white powder.
SOLUBILITY: Soluble in DMSO; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic .

Product Description
Highly selective calmodulin (CaM) antagonist. Inhibitor of Ca2+/calmodulin-dependent phosphodiesterase. Has a selectivity of ~300-fold over Ca2+/CaM-dependent enzymes compared with Ca2+-dependent but CaM-independent enzymes, e.g. protein kinase C (PKC) and transglutaminase.
Product Specific Literature References
Calmodulin antagonists of improved potency and specificity for use in the study of calmodulin biochemistry: S. MacNeil, et al.; Biochem. Pharmacol. 37, 1717 (1988) Abstract
Complexes formed between calmodulin and the antagonists J-8 and TFP in solution: C.J. Craven, et al.; Biochemistry 35, 10287 (1996) Abstract
Further Categories Containing This Product:
Phosphodiesterases / Related Products
 
 
ALX-270-109 Revised 14-Apr-08
Ophiobolin A
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SYNONYMS Cochliobolin A
Ophiobalin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-270-109-MC01   0.1 mg 50.00 USD Add To Cart
ALX-270-109-M001   1 mg 220.00 USD Add To Cart
Product Specification
FORMULA: C25H36O4
MW: 400.6
CAS NUMBER: 4611-05-6
RTECS: RL1576000
SOURCE/HOST: Isolated from Bipolaris leersia MST-FP107.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dimethyl formamide, DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Cell permeable antagonist of calmodulin. Inhibits Ca2+/calmodulin-dependent phosphodiesterase. Inhibits P-glycoprotein-mediated transport. Exhibits antibacterial, antitumor and nematocidal activities. Phytotoxic.
Product Specific Literature References
The structure of ophiobolin, a C25 terpenoid having a novel skeleton: S. Nozoe, et al.; JACS 87, 4968 (1965) Abstract
The constitution of cochliobolin: L. Canonica, et al.; THL 7, 1211 (1966)
Ophiobolin A. A natural product inhibitor of calmodulin: P.C. Leung, et al.; J. Biol. Chem. 259, 2742 (1984) Abstract; Full Text
Role of Calmodulin Inhibition in the Mode of Action of Ophiobolin A: P.C. Leung, et al.; Plant Physiol. 77, 303 (1985) Abstract; Full Text
Characterization of the interaction of ophiobolin A and calmodulin: P.C. Leung, et al.; Int. J. Biochem. 20, 1351 (1988) Abstract
Microbial metabolites of ophiobolin A and antimicrobial evaluation of ophiobolins: E. Li, et al.; J. Nat. Prod. 58, 74 (1995) Abstract
The biology of ophiobolins: T.K. Au, et al.; Life Sci. 67, 733 (2000), Review Abstract
Calmodulin and lipid binding to synaptobrevin regulates calcium-dependent exocytosis: S. Quetglas, et al.; EMBO J. 21, 3970 (2002) Abstract; Full Text
Herbicidal potential of ophiobolins produced by Drechslera gigantea: A. Evidente, et al.; J. Agric. Food Chem. 54, 1779 (2006) Abstract
Inhibition of P-glycoprotein-mediated transport by terpenoids contained in herbal medicines and natural products: N. Yoshida, et al.; Food Chem. Toxicol. 44, 2033 (2006) Abstract
Further Categories Containing This Product:
Calmodulin Inhibitors • Phosphodiesterases / Related Products • Natural Products with Antibiotic Activity • MDR Inhibitors • P-glycoprotein [Pgp] / Related Products • Other Toxins • Natural Products - Antitumor Reagents
 
 
ALX-350-338 Revised 16-Jun-08
Ophiobolin B
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SYNONYMS Cochliobolin B
Zizanin B
Ophiobolsin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-338-M001   1 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C25H38O4
MW: 402.6
CAS NUMBER: 5601-74-1
SOURCE/HOST: Isolated from Bipolaris leersia MST-FP107.
APPEARANCE: White to off-white solid.
FORMULATION: ≥95% (HPLC)
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Originally isolated from Helminthosporium sp. Inhibitor of calmodulin action in calcium regulation. Exhibits antibacterial, antitumor and nematocidal activities.
Product Specific Literature References
The structure of ophiobolin, a C25 terpenoid having a novel skeleton: S. Nozoe, et al.; JACS 87, 4968 (1965) Abstract
Microbial metabolites of ophiobolin A and antimicrobial evaluation of ophiobolins: E. Li, et al.; J. Nat. Prod. 58, 74 (1995) Abstract
The biology of ophiobolins: T.K. Au, et al.; Life Sci. 67, 733 (2000), (Review) Abstract
Further Categories Containing This Product:
Calmodulin Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Antitumor Reagents • Natural Products with Antibiotic Activity
 
 
ALX-430-039 Revised 06-May-08
Phenoxybenzamine . hydrochloride
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-430-039-M100   100 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C18H22ClNO . HCl
MW: 303.8 . 36.5
CAS NUMBER: 63-92-3
MERCK INDEX: 14: 7256
RTECS: DP3750000
PURITY: ≥95% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Irreversible calmodulin inhibitor. Also known for its selective α-adrenergic blocking activity.
Product Specific Literature References
Interaction of alpha adrenergic antagonists with calmodulin: C.Q. Earl, et al.; Life Sci. 35, 524 (1984) Abstract
In vivo recovery of alpha 1-adrenoceptors in rat myocardial tissue after alkylation with phenoxybenzamine: J. Salles, et al.; Eur. J. Pharmacol. 266, 35 (1994) Abstract
Evidence for a functional interaction between calmodulin and the glucocorticoid receptor: Y.M. Ning & E.R. Sanchez; BBRC 208, 48 (1995) Abstract
 
 
ALX-350-311 Revised 07-Feb-05
Stellettamide A . trifluoroacetate
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-311-C100   100 µg 460.00 USD Add To Cart
Product Specification
FORMULA: C26H45N2O . CF3CO2
MW: 401.7 . 113.0
CAS NUMBER: 129744-24-7
SOURCE/HOST: Isolated from the marine sponge Stellata sp.
PURITY: ≥95%
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Inhibits intrinsic tyrosine fluorescence in a concentration-dependent manner. Binds to calmodulin and inhibits Ca2+/calmodulin-dependent enzyme activities.
Product Specific Literature References
Stellettamide-A, a novel inhibitor of calmodulin, isolated from a marine sponge: Y. Abe, et al.; Br. J. Pharmacol. 121, 1309 (1997) Abstract
Further Categories Containing This Product:
Calmodulin Inhibitors • Alkaloids • Marine Natural Products
 
 
ALX-550-310 Revised 03-Jun-08
Trifluoperazine . dihydrochloride
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-550-310-G001   1 g 20.00 USD Add To Cart
ALX-550-310-G005   5 g 75.00 USD Add To Cart
Product Specification
FORMULA: C21H24F3N3S . 2HCl
MW: 407.5 . 73.0
CAS NUMBER: 440-17-5
MERCK INDEX: 14: 9680
RTECS: SP1750000
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and moisture.
HAZARD: HARMFUL.

Product Description
Calmodulin inhibitor. Antipsychotic and sedative dopamine antagonist. Potent and irreversible inhibitor of cAMP-gated cationic channels. Inhibits DNA repair. Potent neurotoxin.
Product Specific Literature References
New drug evaluations amiloride (Midamor, Merck, Sharp and Dohme): H.L. Macfie, et al.; Drug Intel. Clin. Pharm. 15, 94 (1981) Abstract
Trifluoperazine binding to porcine brain calmodulin and skeletal muscle troponin C: J. Massom, et al.; Biochemistry 29, 671 (1990) Abstract
Inhibition of olfactory cyclic nucleotide-activated current by calmodulin antagonists: S.J. Kleene; Br. J. Pharmacol. 111, 469 (1994) Abstract
Trifluoperazine-induced conformational change in Ca(2+)-calmodulin: M. Vandonselaar, et al.; Nat. Struct. Biol. 1, 795 (1994) Abstract
Inhibition of Nav1.7 and Nav1.4 sodium channels by trifluoperazine involves the local anesthetic receptor: P.L. Sheets, et al.; J. Neurophysiol. 96, 1848 (2006) Abstract
Trifluoperazine protects brain plasma membrane Ca(2+)-ATPase from oxidative damaging: P. Souza dos Santos, et al.; Exp. Brain Res. 177, 347 (2007) Abstract
The antipsychotic drug trifluoperazine inhibits DNA repair and sensitizes non small cell lung carcinoma cells to DNA double-strand break induced cell death: A.G. Polischouk, et al.; Mol. Cancer Ther. 6, 2303 (2007) Abstract
Trifluoperazine stimulates ionizing radiation induced cell killing through inhibition of DNA repair: S. Gangopadhyay, et al.; Mutat. Res. 633, 117 (2007) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products • Neurotoxins • Dopaminergics & Dopamine Receptors / Related Products • DNA Replication Inhibitors • MAPK Pathway Activators
 
 
ALX-270-151 Revised 10-May-05
W-5 . hydrochloride