U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 461 - 470 of 1447 results

3.beta-3-[2-(Diethylamino)ethoxy]androst-5-en-17-one hydrochloride or U18666A, an amphipathic cationic amine, is a cell permeable research tool drug that inhibits cholesterol synthesis and trafficking, and also a weak inhibitor of hedgehog (Hh) signaling. U18666A had been used in several models both in vivo and in vitro to mimic Niemann-Pick type C disease (NPC) and for assessing the importance of molecular trafficking through the lysosomal pathway in other conditions such as atherosclerosis, Alzheimer's disease, and prion infections. U18666A also provided animal models for such disorders as petite mal (absence) epilepsy and cataracts. U18666A inhibits the enzyme desmosterol reductase responsible for reducing the desmosterol in cholesterol biosynthesis, and also blocks LDL-(low density lipoprotein) cholesterol transport from the lysosomes into the endoplasmic reticulum thereby increasing the level of caveolina-1 located within the plasma membrane caveolae. U18666A was shown to be a potent antagonist of alpha4beta2 neuronal nicotinic acetylcholine receptors and may be useful as a tool in the functional characterization and pharmacological profiling of nAChRs.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



Abietic acid (AA), a diterpene produced by conifer species, such as grand fir and lodgepole pine, has been reported to have anti-inflammatory and immunomodulatory effects and can be used as a wound-healing agent. Its treatment elevates cell migration and tube formation in human umbilical vein vascular endothelial cells by the activation of ERK and p38 MAPKs. In addition was shown, that abietic acid could be used as an antimetastatic agent or as an adjuvant for anticancer therapy. AA acts as a PPARα/γ dual activator to inhibit age-related inflammation by suppressing NF-κB and the MAPK/AP-1 pathway and can be a useful agent for improving skin photoaging.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Oxophenylarsine (Phenylarsine oxide, PAO, PhAsO) is an organometallic compound with the phenyl group and an oxygen atom bonded to an arsenic atom. The arsenic atom in PAO has a high affinity for the sulfur atom of thiols inorganic compounds, in particular, forming stable complexes with vicinal cysteine residues in protein structures. This effect makes it the useful tool to investigate the interaction of peptides such as insulin with their receptors and the signal transduction from the receptor to the cell interior. Oxophenylarsine is commonly used in cell biological research as an inhibitor of phosphotyrosine phosphatases (PTPases); in particular, PTPases HA1, HA2, and SH-PTP2 have been identified as substrates for Oxophenylarsine. Covalent binding of Oxophenylarsine to cysteinyl residues residing in the catalytic sites causes inactivation of PTPases. Oxophenylarsine also acts on other phosphatases that harbor vicinal thiol groups [i.e., inositol 1,2,3,5,6-pentakisphosphate 5-phosphatase or calcineurin, a Ca2+/calmodulin-dependent serine/threonine phosphatase. Also, NADPH oxidase and mitochondrial adenine nucleotide transporter were reported to be inhibited by Oxophenylarsine. Furthermore, steric inhibition of Oxophenylarsine-linked NFκB was suggested to be responsible for its decreased binding to DNA.
Myristicin, a natural product found in nutmeg oil and nutmeg extract, contains the carbon skeleton for a series of drugs of abuse related to the 3,4-methylenedioxyamphetamines (MDAs). Myristicin, 1-(3-methoxy-4,5-methylenedioxyphenyl)-2-propene, was identified as the major component of commercially available nutmeg oil and in the organic extract of nutmeg powder. Myristicin, or methoxysafrole, is a benzodioxole with slight MAO-inhibiting properties. Myristicin is active at the 5-HT receptors in the brain, and has been shown to have hypotensive, sedative, anti-depressant, anesthetic, hallucinogenic, and serotonergic properties. Large doses generally cause hyper-excitability, followed by CNS depression. Myristicin has been shown to have potent anti-cancer properties. A 65% inhibition of the tumor multiplicity in the lung of rats was observed as the result of treatment of myristicin in rats. Myristicin showed a 31% inhibition of tumor formation in the forestomach of rats. Mice given 5 to 50 mg doses of myristicin, showed 4- to 14-fold increase in liver glutathione S-transferase (GST) activity.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



3-Tyrosine, in contrast to the para isomer, is readily racemized. The majority of the load was metabolized to m-hydroxyphenylacetic acid but m-hydroxymandelic acid and 3,4-dihydroxyphenylacetic acid were also detected. Low circulating levels of m-tyrosine in the plasma suggest that most of the load is held due to a first pass effect somewhere in the enterohepatic system and that this portion of the load is not in equilibrium with the plasma m-tyrosine. The metabolism of a m-tyrosine may give further insight into the deficiencies of the phenylalanine hydroxylating system found in the various phenotypes of phenylketonuria. 3-Tyrosine has been used experimentally as a substitute for L-DOPA in the treatment of Parkinsonism. 3-tyrosine mimics the action of Dopa in two experimental animal models. It was also obvious from the experiments with d,l- and l-m-tyrosine that only the l-isomer (3-Tyrosine) is active.
Epipregnanolone is an epimer of endogenous neurosteroid pregnanolone, it has been shown to antagonize GABAA and NMDA receptors. In addition epipregnanolone inhibits calcium T-currents and stimulates TRPM3 channel. Epipregnanolone displays anesthetic properties. Epipregnanolone has been shown to reduce alcohol self-administration in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gibberellic acid was first discovered in Japan in 1935 as a result of the study of a condition common in rice plants called "foolish seedling" disease, which caused the plants to grow much taller than normal. The effects of gibberellins weren't widely understood until years later. Gibberellic acid, GA3 is a naturally occurring plant hormone that regulates the growth of plants, including triggering seed germination. Gibberellic Acid is not manufactured; it's a natural product extracted from the Gibberella fujikuroi fungus. There are over 100 known forms of gibberellic acid; GA3 is the most effective. Gibberellic acid (GA3) is used extensively in Egypt and other countries, to increase the growth of many fruits (such as strawberries and grapes) and vegetables (such as tomatoes, cabbages and cauliflower). Carcinogenic effect of Gibberellic acid has being demonstrated in several studies. Gibberellic acid increased the activity of testicular 3β-HSD and 17β-HSD and elevated testosterone content in rats, acting as an agonist of steroidogenesis in male rats. Gibberellic acid has being suggested to promote ulcer-healing, healing of surgical wounds or open fractures and treatment of bronchitis or thrombophlebitis in animals including humans.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Anisomycin (2-p-methoxyphenylmethyl-3-acetoxy-4-hydroxypyrrolidine) is an antibiotic isolated from cultures of various Streptomyces. Anisomycin is a potent, structurally specific, and reversible inhibitor of protein biosynthesis in certain yeast and mammalian cells. The inhibition occurs subsequent to the formation of aminoacyl transfer ribonucleic acid but prior to the release of polypeptides from the polyribosome. Anisomycin has unspecified effects that can produce temporary amnesia for a reactivated memory and they also could be responsible for any permanent effects that anisomycin produces. Anisomycin is known to cause apoptosis by activation of MAPK cascade.
Status:
US Approved Allergenic Extract (1994)

Class (Stereo):
CHEMICAL (ACHIRAL)



Cinnamyl alcohol (CAL, 3-phenyl-2-propen-1-ol) is found mostly in esterized form as a natural component in cinnamon oil obtained from the bark of the Cylonese cinnamon tree. Furthermore, (esterized) CAL is a component of the balsam of Peru from Myroxylon pereirae, of Styrax (balsam) from the wood of Liquidambar orientalis Miller or Liquidambar styraciflua L. and further plant extracts. The regulatory status of CAL includes approval (21 CFR 172.515) by the FDA and Generally Recognized as Safe (GRAS) as flavor ingredient [Number 2294] by the Flavor and Extract Manufacturers Association. CAL included in the Council of Europes list of substances which may be used in foodstuffs. CAL have been reported as common component of food occurring mainly in a wide variety of fruits, vegetables, and spices in varying concentrations. The plant phenolic CAL is used as a fragrance ingredient and has antipyretic and antiproliferative effects. A recent report also demonstrated its vasodilatory activity.