A mycotoxin which induces apoptosis

Beauvericin is a mycotoxin originally derived from Beauveria bassiana, a common fungal parasite of arthropods. It is also produced by the fungus Fusarium, a pathogen of insects and plants. Beauvericin is cytotoxic against insect cells, killing the insect cell line SF-9 with a 50% cytotoxic concentration of 2.5 μM. In mammalian cells, beauvericin induces apoptosis with an IC₅₀ of 4.5 μM.

A designer drug

Phenylpiperazine is the base compound from which a broad series of bioactive products are derived. Many are entactogenic drugs which induce central serotonin release. Substituted phenylpiperazines, such as 1-(3-chlorophenyl)piperazine, have been identified as designer drugs or drugs of abuse. This product is intended for forensic applications.

A designer drug

1-(m-Trifluoromethylphenyl) piperazine (TFMPP) is an entactogenic drug which selectively promotes the release of serotonin. When used in combination with 1-benzylpiperazine, TFMPP increases both serotonin and dopamine, mirroring the effects of 3,4-methylenedioxymethamphetamine. Drug-drug synergism may induce seizures. TFMPP has been identified in party pills and powders. Its metabolism in rats has been described. This product is intended for forensic applications.

A mycotoxin that disrupts microtubule organization

Citrinin is a mycotoxin originally isolated from Penicillium citrinum that is also produced by a variety of other fungi that are found as contaminants in human foodstuffs and animal feeds. Citrinin exerts cytotoxic and genotoxic effects in various mammalian cells, causing mycotoxic nephropathy in livestock and Balkan nephropathy and yellow rice fever in humans. Because citrinin induces apoptosis and blocks tubulin polymerization as well as mitotic spindle assembly, it is useful as a biological research reagent.

An internal standard for the quantification of docosahexaenoyl ethanolamide

Docosahexaenoyl ethanolamide-d₄ contains four deuterium atoms at the 1, 1', 2, and 2' positions. It is intended for use as an internal standard for the quantification of docosahexaenoyl ethanolamide by GC- or LC-mass spectrometry (MS).

A dihydroxy- derivative of vitamin D₂

Ercalcitriol is the active circulating metabolite of vitamin D₂ formed by 25-hydroxylase in the liver and 25-hydroxyvitamin D -hydroxylase in the kidney. By binding to the vitamin D receptor (VDR), ercalcitriol activates VDR to interact with the retinoid X receptor (RXR), forming the VDR/RXR/cofactor complex, which regulates gene transcription. Because ercalcitriol circulates at picomolar concentrations and is highly lipophilic, it is difficult to quantify.

Potential drug of abuse

1-(4-Fluorobenzyl) piperazine is a substituted BZP with a potential for abuse. The physiological and toxicological properties of this compound have not been evaluated. This product is intended for forensic and research applications. 1-(4-Fluorobenzyl) piperazine is also used as a precursor in the synthesis of certain bioactive compounds.

Potential drug of abuse

1-(p-Fluorophenyl) piperazine (hydrochloride) is a substituted phenylpiperazine with a potential for abuse. The physiological and toxicological properties of this compound have not been evaluated. This product is intended for forensic and research applications.

An analog of MDMA

3,4-Dimethoxymethamphetamine (hydrochloride) (DMMA) is an analog of 3,4-methylenedioxymethamphetamine (MDMA), a psychoactive drug and research chemical of the phenethylamine and amphetamine chemical classes. DMMA appears to interfere with monoamine transport, inhibiting uptake of noradrenalin and serotonin transporters (Kis = 22.8 and 7.7 μM and IC₅₀s = 253.4 and 108 μM, respectively). DMMA is significantly less potent than MDMA (Kis = 0.6 and 2.5 μM and IC₅₀s = 6.6 and 34.8 μM for MDMA inhibition of noradrenalin and serotonin transporters, respectively).

An inhibitor of hedgehog signaling

Cyclopamine is a natural steroidal alkaloid that inhibits signaling through the hedgehog pathway at the level of the pathway activator Smoothened. By altering gene expression in this signaling sequence, cyclopamine induces defects in morphogenesis, first observed in chicks and sheep as cyclopia. As a readout of action, cyclopamine inhibits hedgehog-dependent expression of Pax7 with an IC₅₀ value of 24 nM. Although teratogenic during development, cyclopamine has potential applications in the treatment of cancer.

A stimulant drug and appetite suppressant

Diethylcathinone is a stimulant drug of the phenethylamine, amphetamine, and cathinone chemical classes that is used as an appetite suppressant. It functions as an inactive prodrug that only becomes active when further metabolized to ethcathinone, a selective norepinephrine releasing agent. In the US, diethylcathinone is classified as a Schedule IV controlled substance, with low potential for abuse.

A designer drug

4-Methyl-α-pyrrolidinobutiophenone (MPBP) is a synthetic cathinone with psychoactive properties which has recently been identified in party pills and powders. The metabolism of MPBP has been characterized. The biological and toxicological properties of this compound are unknown. This product is intended for forensic and research applications.

A synthetic cannabinoid

JWH 031 is a synthetic cannabinoid (CB) with a relatively low binding affinity for the central CB₁ receptor (K_i = 399 nM). Despite its low affinity for CB₁, this pyrrole-based cannabinoid is efficacious in reducing spontaneous activity and increasing antinociception in mice. This product is intended for forensic and research applications.

A prodrug of a potent FP receptor agonist

Ethyl amides of PGs serve as prodrugs, as they are hydrolyzed in certain tissues to generate the bioactive free acid.

A DNA methyltransferase inhibitor

5-Azacytidine, a chemical analogue of the DNA and RNA nucleoside cytidine, is an inhibitor of DNA methyltransferases, potentially serving to reverse epigenetic changes. It reduces hypermethylation associated with certain diseases, including myelodysplastic syndromes (IC₅₀s = 2.4 and 2.6 μM for in vitro anti-myeloma activity) and cancer (IC₅₀s ~ 0.4 μM for inhibiting proliferation of various cancer cell lines). 5-Azacytidine has a reported half-life of 17 hours and is considerably cytotoxic; it must be incorporated into DNA to covalently trap DNA methyltransferases.

Water-soluble analog of forskolin

NKH477 is a water-soluble analog of forskolin which has both inotropic and vasodilator effects when administered intravenously. Like forskolin, NKH477 activates adenylyl cyclases without altering the activity of phosphodiesterases or sodium/potassium ATPases. This compound stimulates cardiac (type V) adenylyl cyclase more potently than other isoforms. NKH477 relaxes guinea pig tracheal smooth muscle precontracted with histamine with an EC₅₀ of 32.6 nM.

An HSP90 inhibitor with anti-cancer effects

PU-H71 (hydrate) is a purine scaffold HSP90 inhibitor that has potent in vitro anti-myeloma activity in both drug-sensitive (MM-1S, RPMI-8226/S, INA-6, NCI-H929, U266) and drug-resistant (MM-1R, RPMI-8226/Dox40, OMP-1) human myeloma cell lines (IC₅₀s = 100-300 nM). It also demonstrates considerable efficacy inhibiting growth of triple-negative breast cancer tumor cell lines MDA-MB-468, MDA-MB-231, and HCC-1806 (IC₅₀s = 65, 140, and 87 nM, respectively), diffuse large B-cell lymphomas (GI₅₀ = 1.39 μM), and various hepatocellular carcinoma cell lines (GI₅₀s < 3 μM).

An internal standard for the quantification of DMABA NHS ester

DMABA-d₁₀ NHS ester is intended for use in combination with DMABA NHS ester (Item No. 11216) as a derivatizing reagent for PE lipids in order to facilitate MS characterization and to quantify relative changes in their abundance.