A potent, cell-permeable inhibitor of all JAK isoforms (IC50 = 6.1, 12, and 8.0 nM for JAK1, JAK2, and JAK3, respectively); useful in ameliorating inflammatory or autoimmune components of a host of diseases.

An N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.

A non-nucleoside DNA methyltransferase inhibitor (IC₅₀ = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.

A metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).

A natural anthocyanidin.

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5

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…

An analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to…

ApNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate AEA (Item No. 90050). It also will hydrolyze…

A natural isoflavone which acts as a phytoestrogen; stimulates the growth of estrogen-dependent breast cancer cells in vivo; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover; increases bone formation in collagen matrix in vivo.

A potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC₅₀ = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

A positive allosteric modulator of the M1 mAChR; dose-dependently reduces the concentration of acetylcholine required to activate M1; the effective range for potentiation is 0.1 to 100 μM with 3 nM acetylcholine; restores impairment in reversal learning in a mouse model of Alzheimer’s disease.

A cell-permeable ACL inhibitor (IC₅₀ = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.

A nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

A natural benzoquinone which directly binds and inhibits XIAP (IC50 = 4.1 μM); blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP; prevents NF-κB activation by inhibiting IKK; protects against XIAP- and caspase-dependent inflammation.

An activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.

A selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.

A cell-permeable, potent inhibitor of both SHP-1 and SHP-2 (IC₅₀ = 355 and 318 nM, respectively); much less effective against other protein tyrosine phosphatases and DUSP26.

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.

An orally active, potent, and selective EP2 receptor antagonist (IC₅₀ = 16 nM); over 1,000-fold less active at other prostanoid receptors, including other EP receptors.

Blocks mitochondrial complex III; inhibits the activity of the NADH oxidase in certain bacteria.

An atypical antidepressant with diverse actions, most notably on the glutamatergic system; attenuates glutamate release and modulates the function of AMPAR; acts as an agonist of the µ-opioid receptor (EC₅₀s = 194 and 641 nM for human and mouse receptors, respectively).

The oxidized form of NADPH; serves as a cofactor in various biological reactions.

A synthetic analog of 2'-deoxy-guanosine which is used to treat or prevent cytomegalovirus (CMV) infections; inhibits the replication of human CMV with an IC₅₀ value of 0.01 μM and is effective against strains of CMV from human, monkey, mouse, and guinea pig.

An agonist of the Gαi-linked dopamine receptors D2, D3, and D4 (Ki = 3.9, 2.2, 0.5, and 5.1 nM for D2S, D2L, D3, and D4, respectively); relatively inactive at the Gαs-linked dopamine receptors D1 and D5, as well as at serotonin and adrenergic receptors.

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway. It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a…

A hydrolyzable tannin with phytotoxic activity.

A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.

A selective cholesterol transport inhibitor that targets the NPC1L1 (KDs = 12,000, 540, 40, and 220 nM for its glucuronide in mouse, rat, rhesus monkey, and human, respectively); blocks intestinal cholesterol absorption in various animal models (IC₅₀s = 0.0005-0.05 mg/kg).