A potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC₅₀s = 0.7 and 0.9 nM, respectively); blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.

An antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC₅₀ = 100 nM); inhibits ADP-induced platelet aggregation ex vivo; shown to be beneficial in the prevention of vascular ischemic events for patients without…

A potent antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC₅₀ = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC₅₀ = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…

A heptose that inhibits glucokinases and hexokinases from diverse organisms through competition with D-glucose (Ki = 0.25 mM); blocks glucose oxidation and glucose-mediated insulin release from pancreatic islet cells.

Potassium chloride stock solution (1 M) contains filtered potassium chloride (1 M). It is ready to use as supplied.

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

A specific inhibitor of class I α-1,2-mannosidase (IC₅₀ = 20 mM), a key enzyme for N-glycan processing in the endoplasmic reticulum and Golgi; inhibiting α-1,2-mannosidase with 1-Deoxymannojirimycin generates N-linked oligosaccharides with high mannose content, preventing…

Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

A selective inhibitor of TAF1 bromodomain 2 (Kd = 1.8 µM; IC₅₀ = 0.9 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…

A mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 and B2 being the two major components; demonstrates rapid in vitro bactericidal activity against major multidrug-resistant Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumonia.

A natural intermediate in the pteridine pathway that can be produced naturally from 7-oxobiopterin or in vitro by the oxidation of pterin by xanthine oxidase.

An activator of PLC that stimulates superoxide generation, increase in cytoplasmic calcium, and inositol phosphate formation in human neutrophils when used at a concentration of 15-50 µM; promotes the hydrolysis of phosphatidylinositol bisphosphate by all PLC isoforms.

A synthetic antibiotic that inhibits dihydrofolate reductase (DHFR), with prominent selectivity for bacterial DHFR over mammalian DHFR (IC₅₀s = 5 and 30,000 nM, respectively); commonly used in combination with sulfamethoxazole to minimize acquired resistance.

A stable inhibitor of FAS that leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.

Piriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC₅₀ value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…

A selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 µM.

A selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer; increases ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues; metabolized by CYP450 enzymes to active metabolites; alters cholesterol…

A major component of the root of P. suffruiticosa that at 30 µM inhibits the growth of human hepatocellular carcinoma SK-HEP-1 cells by causing cell cycle arrest and suppressing the activation of NF-κB.

Bicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…

Inhibits microtubule polymerization (IC₅₀ =3.2 μM) by binding to tubulin, which disrupts spindle formation during mitosis; blocks the growth of MCF-7 human breast carcinoma cells (IC₅₀ = 13 nM); inhibits neutrophil motility and activity (5 μmol/kg in a mouse model of…

A selective IDO1 inhibitor (IC₅₀ = 7.1 nM in HeLa cells); promotes T and natural killer-cell growth, increases IFN-γ production, and reduces conversion to Treg-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells; inhibits…

A natural, potent and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively; also inhibits papain, calpain, and cathepsins B and H.

A triazolothiadiazine that inhibits PDE4 (EC₅₀ = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC₅₀ = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC₅₀ = 48.2, 37.2, 452, and 49.2 nM, respectively).

A platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC₅₀ = 2 µM), blocking protein splicing and cell growth.

An EpEDE acid formed from DGLA, either by a strong oxidizing agent or by cytochrome P450 epoxygenases; biological properties are poorly understood.

Contains selected eicosanoids produced by the metabolism of prostaglandins; designed for direct use in LC-MS applications.

An FGFR inhibitor.

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

A potent, selective, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively); shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist MK-801.

A dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A₁, A_2A, and A₃ receptors with K_i values of 8.96, 23.0, and 8.3 µM, respectively.