Hydroxy-2-naphthalenylmethylphosphonic acid ≥98% (by TLC)
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HNMPA is a membrane impermeable inhibitor of insulin receptor tyrosine kinase (IC50 = 100µM); in rat adipocytes (IC50 = 10µM). Inhibits serine and tyrosine autophosphorylation by the human insulin receptor.
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Bisindolylmaleimide IX methanesulphonate ≥98%
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Cell-permeable PKC inhibitor. Selective for PKC (IC50=10nM) over CaM kinase II (IC50=17µM) and PKA (IC50=0.9µM). Induces apoptosis in various cell lines.
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2,3-Diphenylquinoxaline-6-carboxylic acid ≥98% (by TLC)
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Inhibits the translocation of Akt.
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3'-Carbamoyl-[1,1'-biphenyl]-3-ylcyclohexylcarbamate ≥98% (by TLC)
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URB-597 is a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), which is involved in the hydrolysis of endogenous cannabinoids such as anandamide. Inhibition of FAAH may serve to enhance the analgesic effects of endogenous cannabinoids. URB-597 has been shown to inhibit FAAH in rat cortical neuron membranes and in intact neurons with IC50 values of 4.6nM and 0.5nM, respectively. The compound has also been shown to have anxiolytic effects in rats (ID50=0.15mg/kg). Because URB-597 acts on FAAH and does not interfere with the binding of anandamide to the CB1 and CB2 receptors, it is a novel tool for drug development.
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AG-1288 ≥98% (by TLC)
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Tyrosine kinase inhibitor. It has been shown to block TNFα induced cytotoxicity and to block glucocorticoid-induced COX-2 activity in human amnion cells (IC50=21μM). It is also reported to inhibit guanylyl cyclase.
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Ilimaquinone ≥98% (by TLC)
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ADP-ribosylation factor inhibitor
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L-744,832 ≥98% (by TLC)
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Ras farnesyltransferase inhibitor. Induces tumor regression in transgenic mice with multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis. Induces p21 expression and arrests cells at G1. Causes enhanced mitotic sensitivity to taxol.
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Mevastatin sodium ≥98% (by HPLC)
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This is the active carboxylate form of mevastatin. It is active in whole cells as well as in cell free assays.
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N-Arachidonoyl-L-phenylalanine ≥98% (by TLC)
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Putative endogenous member of a growing family of lipo-amino acids (N-acyl amino acids).
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2-Arachidonoylglycerol ≥98% (by HPLC)
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Cannabinoid receptor ligand.
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3-Methyl-1-phenyl-2-pyrazolin-5-one ≥98% (by HPLC)
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A free radical scavenger and antioxidant. Displays beneficial effects in a rat model of ischemic brain damage.
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N-Arachidonyl-2-chloroethylamide ≥98% (by TLC)
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Cannabinoid receptor ligand.
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Anandamide ≥98% (by TLC)
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Endogenous [1] ligand for the CB1 receptor (CB1: Ki=52nm; CB2: Ki=1930nm [2]) and TRPV1 (Ki=5.78µM [3,4]). Inhibits NF-κB activation through direct binding to IKKβ [5] and induces apoptosis independently of cannabinoid or vanilloid receptors [6]. Activates the MAP kinase (MAPK/ERK) signalling pathway [7].
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Palmitoylethanolamide ≥98% (by TLC)
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Endogenous cannabinoid. Weak ligand of CB1 (Ki=23.8µM) and CB2 (Ki=13.9µM) receptor. Inhibits fatty acid amide hydrolase (FAAH) (IC50=5.1µM). Immunosuppressant, anti-inflammatory, anti-nociceptive and anti-convulsant in vivo. The exact mode of action has not yet been revealed. It has been suggested that PEA: i) binds to a yet to be discovered cannabinoid receptor similar to CB2; ii) administered in vivo elicits the synthesis of endogenous agonists of CB2; iii) acts as an "entourage" compound by enhancing the activity and/or by influencing the turnover of endogenous agonists of CB2, possibly but not uniquely, by inhibiting their degradation.
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Eicosa-5Z,8Z-dienoic acid ≥98% (by TLC)
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Arachidonic acid analog.
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WEB-2086 ≥98% (by HPLC)
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PAF receptor antagonist. Inhibits PAF-induced human platelet and neutrophil aggregation in vitro (IC50=0.17 and 0.36µM respectively). In vivo it dose dependently blocks eosinophil activation and displays antiallergic and anti-inflammatory activity in various models. Induces differentiation and triggers apoptosis and in a variety of cell lines.
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Histone Deacetylase Inhibitor VIII ≥98% (by TLC)
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HDAC6 inhibitor
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5(S)-Hydroxyeicosa-6E,8Z,11Z,14Z-tetraenoic acid (HETE) ≥98%
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Biosynthesis via 5-lipoxygenase. Chemotactic and chemokinetic for PMNL. Induces degranulation and calcium flux.
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DIF-1 ≥98% (by HPLC), Ultrapure
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Induces cell differentiation.
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Cp 31398 Dihydrochloride (synthetic) ≥98% (by TLC)
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CP-31398 restores mutant p53 tumor suppressor function in vitro without affecting p53 homologs p63 and p73, and in vivo inhibiting UVB-induced skin carcinogenesis in mice. Stabilization of p53 inhibits ubiquitination without altering phosphorylation at Ser12 or Ser20 or MDM2 binding. Administration of this or similar compounds has the potential to enhance cytotoxic chemotherapy.
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Actinomycin D (from Streptomyces parvulus) ≥98% (by TLC)
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An intercalating transcription inhibitor and antineoplastic antibiotic. Inhibits transcription by binding to DNA at dG residues. Induces apoptosis in many cell lines, but suppresses in PC12 cells induced by topoisomrease II inhibitor etopside. Used at 5-10 µg/mL in cell culture for halting transcription. The product is not sterile.
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Z-Guggulsterone ≥98%
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A guggul tree steroid well known for its lipid lowering properties. Acts as a selective antagonist at farnesoid X receptors (FXRs). Inhibits FXR transactivation (IC50=10µM).
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N-(1-Adamantyl)-N'-cyclohexylmorpholine-4-carboxamidine hydrochloride ≥98%
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K+ channel blocker
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Paroxetine hydrochloride ≥98%
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Highly potent and selective serotonin uptake inhibitor