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ALX-270-069 Revised 04-Feb-05
HA-100 . dihydrochloride
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SYNONYMS 1-(5-Isoquinolinylsulfonyl)piperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-069-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C13H15N3O2S . 2HCl
MW: 277.3 . 73.0
CAS NUMBER: 84468-24-6
PURITY: ≥99%
APPEARANCE: Lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of myosin light chain kinase, cAMP-dependent protein kinase (PKA) and protein kinase C (PKC).
Product Specific Literature References
Role of protein kinases in stimulation of human polymorphonuclear leukocyte oxidative metabolism by various agonists. Differential effects of a novel protein kinase inhibitor: C. Gerard, et al.; J. Clin. Invest. 77, 61 (1986) Abstract
Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives: M. Hagiwara, et al.; Mol. Pharmacol. 32, 7 (1987) Abstract
Further Categories Containing This Product:
PKC InhibitorsMyosin Light Chain Kinase Inhibitors
 
 
ALX-270-071 Revised 06-Aug-07
HA-1077 . dihydrochloride
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SYNONYMS Fasudil
1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
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ALX-270-071-M001   1 mg 21.00 USD Add To Cart
ALX-270-071-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C14H17N3O2S . 2HCl
MW: 291.4 . 73.0
CAS NUMBER: 103745-39-7
MERCK INDEX: 14: 3942
PURITY: ≥98%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in water, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ.  Cell permeable Ca2+ antagonist with antivasospastic properties.
Product Specific Literature References
The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs: O. Shibuya, et al.; Acta Neurochir. 90, 53 (1988) Abstract
Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase: T. Asano, et al.; Br. J. Pharmacol. 98, 1091 (1989) Abstract
Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator: Y. Sasaki & Y. Sasaki; BBRC 171, 1182 (1990) Abstract
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle: M. Seto, et al.; Eur. J. Pharmacol. 195, 267 (1991) Abstract
A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture: M. Shirotani, et al.; J. Pharmacol. Exp. Ther. 259, 738 (1991) Abstract
Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle: S. Takizawa, et al.; Eur. J. Pharmacol. 250, 431 (1993) Abstract
Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells: H. Nagumo, et al.; Am. J. Physiol. Cell. Physiol. 278, C57 (2000) Abstract
Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCbetaI, PKCbetaII and PKCzeta in human neutrophils: X. Siomboing, et al.; Mediators Inflamm. 10, 315 (2001) Abstract
Effects of HA-1077 and Y-27632, Two Rho-Kinase Inhibitors, in the Human Umbilical Artery: M. Ark, et al.; Cell Biochem. Biophys. 41, 331 (2004) Abstract
Further Categories Containing This Product:
CAM Kinase InhibitorsMyosin Light Chain Kinase Inhibitors
 
 
ALX-301-009 Revised 09-Dec-04
1-O-Hexadecyl-2-acetyl-sn-glycero-3-phospho-(N,N,N-trimethyl)-hexanolamine
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Platelet Activating Factors [PAF] & Receptors / Related Products
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ALX-301-009-M005   5 mg 45.00 USD Add To Cart
ALX-301-009-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C30H62NO7P
MW: 579.8
CAS NUMBER: 99103-16-9
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in chloroform, 100% ethanol or methanol. Soluble in water after sonification for 1 minute at 40°C.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Slightly hygroscopic.

Product Description
PAF antagonist. Shows inhibitory behavior on platelet aggregation, secretion and phospholipid turnover.
Product Specific Literature References
Structural analogs of alkylacetylglycerophosphocholine inhibitory behavior on platelet activation: A. Tokumura, et al.; J. Biol. Chem. 260, 12710 (1985) Abstract; Full Text
Platelet activating factor is a potent stimulant of the production of active oxygen species by human monocyte-derived macrophages: M. Rouis, et al.; BBRC 156, 1293 (1988) Abstract
 
 
ALX-270-373 Revised 11-Aug-06
trans-HR22C16
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
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ALX-270-373-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C23H23N3O3
MW: 389.5
CAS NUMBER: 462630-41-7
PURITY: ≥95%
APPEARANCE: Yellow to ocher solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

Cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=800nM) by binding to the mitotic kinesin Eg5.

Product Specific Literature References
HR22C16: A Potent Small-Molecule Probe for the Dynamics of Cell Division: S. Hotha, et al.; Angew. Chem. Int. Ed. Engl. 42, 2379 (2003) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins / Related Products
 
 
ALX-350-357 Revised 05-Apr-08
Hurghadolide A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cytoskeletal Research
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ALX-350-357-C010   10 µg 120.00 USD Add To Cart
Product Specification
FORMULA: C76H130O20
MW: 1363.9
SOURCE/HOST: Isolated from marine sponge Theonella swinhoei.
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless oil.
SOLUBILITY: Soluble in DMSO (25mg/ml) or 100% ethanol (25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Cytotoxic. Disrupts the actin cytoskeleton. Antifungal.

Product Specific Literature References
Hurghadolide A and swinholide I, potent actin-microfilament disrupters from the Red Sea sponge Theonella swinhoei: D.T. Youssef & S.L. Mooberry; J. Nat. Prod. 69, 154 (2006) Abstract
General Literature References
Marine natural products. XXIII. Three new cytotoxic dimeric macrolides, swinholides B and C and isoswinholide A, congeners of swinholide A, from the Okinawan marine sponge Theonella swinhoei: M. Kobayashi, et al. ; Chem. Pharm. Bull. (Tokyo) 38, 2960 (1990) Abstract
Marine natural products. XXXI. Structure-activity correlation of a potent cytotoxic dimeric macrolide swinholide A, from the Okinawan marine sponge Theonella swinhoei, and its isomers: M. Kobayashi, et al.; Chem. Pharm. Bull. (Tokyo) 42, 19 (1994) Abstract
Swinholide A is a microfilament disrupting marine toxin that stabilizes actin dimers and severs actin filaments: M.R. Bubb, et al.; J. Biol. Chem. 270, 3463 (1995) Abstract; Full Text
Two classes of metabolites from Theonella swinhoei are localized in distinct populations of bacterial symbionts: C.A. Bewley, et al.; Experientia 52, 716 (1996) Abstract
Autoregulation of actin synthesis responds to monomeric actin levels: A. Lyubimova, et al.; J. Cell. Biochem. 65, 469 (1997) Abstract
Misakinolide A is a marine macrolide that caps but does not sever filamentous actin: D.R. Terry, et al.; J. Biol. Chem. 272, 7841 (1997) Abstract; Full Text
Actin-depolymerizing effect of dimeric macrolides, bistheonellide A and swinholide A: S.Y. Saito, et al.; J. Biochem. 123, 571 (1998) Abstract
Structural basis of swinholide A binding to actin: V.A. Klenchin, et al.; Chem. Biol. 12, 187 (2005) Abstract; Full Text
Further Categories Containing This Product:
Natural Products - Antifungal AgentsActin / Related ProductsMarine Natural Products
 
 
ALX-420-039 Revised 14-Aug-08
Imiquimod
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SYNONYMS 1-(2-Methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine
R-837
PRODUCT LINE Inflammation
PRODUCT CATEGORY TLR Agonists Other Products
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ALX-420-039-M100   100 mg 55.00 USD Add To Cart
ALX-420-039-M250   250 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H16N4
MW: 240.3
CAS NUMBER: 99011-02-6
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (3mg/ml) or dimethyl formamide; slightly soluble in water (warm to 37°C, vortex); insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for up to 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C.

Product Description
Topical immune response modifier that inhibits angiogenesis. Up-regulates IL-18 and down-regulates MMP-9 through recognition of Toll-like receptor 7 (TLR7) and subsequent activation of MyD88-dependent pathway.
Product Specific Literature References
Imiquimod applied topically: a novel immune response modifier and new class of drug: R.L. Miller, et al.; Int. J. Immunopharmacol. 21, 1 (1999) Abstract
Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway: H. Hemmi, et al.; Nat. Immunol. 3, 196 (2002) Abstract
In vivo and in situ modulation of the expression of genes involved in metastasis and angiogenesis in a patient treated with topical imiquimod for melanoma skin metastases: C. Hesling, et al.; Br. J. Dermatol. 150, 761 (2004) Abstract
Imiquimod as an antiangiogenic agent: V.W. Li, et al.; J. Drugs Dermatol. 4, 708 (2005) Abstract
Imiquimod is a strong inhibitor of tumor cell-induced angiogenesis: S. Majewski, et al.; Int. J. Dermatol. 44, 14 (2005) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Stimulation of TLR7 can be achieved with 1-10µg/ml of the compound for 6 to 24 hours.

Related Products:
- ddWater (endotoxin-free) (Prod. No. ALX-505-008)
- PBS (endotoxin-free) (Prod. No. ALX-505-007)
 
 
ALX-350-145 Revised 28-Mar-07
Isobavachalcone
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SYNONYMS 2’,4’,4-Trihydroxy-3’-[3’’-methylbut-3’’-enyl]chalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-145-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C20H20O4
MW: 324.4
CAS NUMBER: 20784-50-3
SOURCE/HOST: Isolated from plant Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Inhibits platelet aggregation. Inhibitor of Epstein-Barr virus early antigen (EBV-EA) induction. Exhibits potent inhibitory effect on skin tumor promotion. Potent inhibitor of MMP-2. Displays DNA strand-scission (cleaving) activity. Shows antifungal activity.
Product Specific Literature References
Antiplatelet flavonoids from seeds of Psoralea corylifolia: W.J. Tsai, et al.; J. Nat. Prod. 59, 671 (1996) Abstract
Antioxidative components of Psoralea corylifolia (Leguminosae): H. Haraguchi, et al.; Phytother. Res. 16, 539 (2002) Abstract
Chalcones, coumarins, and flavanones from the exudate of Angelica keiskei and their chemopreventive effects: T. Akihisa, et al.; Cancer Lett. 201, 133 (2003) Abstract
Antitrichomonal and antioxidant activities of Dorstenia barteri and Dorstenia convexa: N.O. Omisore, et al.; Braz. J. Med. Biol. Res. 38, 1087 (2005) Abstract
Chalcones and other compounds from the exudates of Angelica keiskei and their cancer chemopreventive effects: T. Akihisa, et al.; J. Nat. Prod. 69, 38 (2006) Abstract
Inhibition of matrix metalloproteinase-2 secretion by chalcones from the twigs of Dorstenia barteri Bureau.: B. Ngameni, et al.; Arkivoc ix, 91 (2007) Full Text
 
 
ALX-350-275 Revised 04-Aug-08 New product
Jasplakinolide
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SYNONYMS Jaspamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cytoskeletal Research
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ALX-350-275-C050   50 µg 150.00 USD Add To Cart
ALX-350-275-C100   100 µg 250.00 USD Add To Cart
Product Specification
FORMULA: C36H45BrN4O6
MW: 709.7
CAS NUMBER: 102396-24-7
SOURCE/HOST: Isolated from Jaspis splendens.
PURITY: ≥97% (HPLC)
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in 100% ethanol, 83% methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by MS.

Product Description
Cell permeable F-actin probe. Induces actin polymerization. Completely inhibits the binding of phalloidin to F-actin. Antifungal and anti-proliferative agent.
Product Specific Literature References
New class of antifungal agents: jasplakinolide, a cyclodepsipeptide from the marine sponge, Jaspis species: V.R. Scott, et al.; Antimicrob. Agents Chemother. 32, 1154 (1988) Abstract
In vitro screening of crude extracts and pure metabolites obtained from marine invertebrates for the treatment of breast cancer: J. Stingl, et al.; Cancer Chemother. Pharmacol. 30, 401 (1992) Abstract
Jasplakinolide, a cytotoxic natural product, induces actin polymerization and competitively inhibits the binding of phalloidin to F-actin: M.R. Bubb, et al.; J. Biol. Chem. 269, 14869 (1994) Abstract; Full Text
Growth modulation and differentiation of acute myeloid leukemia cells by jaspamide: I. Fabian, et al.; Exp. Hematol. 23, 583 (1995) Abstract
Jasplakinolide's inhibition of the growth of prostate carcinoma cells in vitro with disruption of the actin cytoskeleton: A.M. Senderowicz, et al.; J. Natl. Cancer Inst. 87, 46 (1995) Abstract
Jasplakinolide: interaction with radiation and hyperthermia in human prostate carcinoma and Lewis lung carcinoma: H. Takeuchi, et al.; Cancer Chemother. Pharmacol. 42, 491 (1998) Abstract
Role of actin-filament disassembly in lamellipodium protrusion in motile cells revealed using the drug jasplakinolide: L.P. Cramer; Curr. Biol. 9, 1095 (1999) Abstract
Actin stabilization by jasplakinolide enhances apoptosis induced by cytokine deprivation: S.C. Posey & B.E. Bierer; J. Biol. Chem. 274, 4259 (1999) Abstract; Full Text
The anti-proliferative agent jasplakinolide rearranges the actin cytoskeleton of plant cells: H. Sawitzky, et al.; Eur. J. Cell Biol. 78, 424 (1999) Abstract
Effects of jasplakinolide on the kinetics of actin polymerization. An explanation for certain in vivo observations: M.R. Bubb, et al.;; J. Biol. Chem. 275, 5163 (2000) Abstract; Full Text
A role for the actin cytoskeleton in the initiation and maintenance of store-mediated calcium entry in human platelets. Evidence for conformational coupling: J.A. Rosado, et al.; J. Biol. Chem. 275, 7527 (2000) Abstract; Full Text
A simple model for the cooperative stabilisation of actin filaments by phalloidin and jasplakinolide: B. Visegrády, et al.; FEBS Lett. 579, 6 (2005) Abstract
Dynamics of an F-actin aggresome generated by the actin-stabilizing toxin jasplakinolide: F. Lázaro-Diéguez, et al.; J. Cell Sci. 121, 1415 (2008) Abstract
Further Categories Containing This Product:
Actin / Related ProductsMarine Natural Products
 
 
ALX-380-027 Revised 09-May-08
K-252a
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-380-027-C100   100 µg 98.00 USD Add To Cart
ALX-380-027-C500   500 µg 290.00 USD Add To Cart
ALX-380-027-M001   1 mg 395.00 USD Add To Cart
Product Specification
FORMULA: C27H21N3O5
MW: 467.5
CAS NUMBER: 97161-97-2
SOURCE/HOST: Isolated from Nocardiopsis sp.
PURITY: