A thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.

A dual inhibitor of DNA-PK and PI3K.

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

An active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3

An aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.

A selective inhibitor of ABHD6 (IC₅₀ = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.

A potent inhibitor of LSD1 (IC₅₀ = 0.02 µM) that less effectively inhibits MAO-A and MAO-B (IC₅₀s = 1.38 and 0.72 µM); blocks the expression of IE genes of HSV and hCMV in mammalian cells; represses HSV primary infection in mice and blocks HSV reactivation from…

An inhibitor of SRE activation in PC3 cells (IC₅₀ = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC₅₀ = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay.

A flavonoid compound that acts as a powerful antioxidant; inhibits TBARS formation with an IC50 value of 6.34 µM; blocks oxLDL uptake by U937-derived macrophages at 20 µM; demonstrates potent chemopreventative potential by binding JAK1/STAT3 to inhibit neoplastic transformation of…

A small diffusible signaling molecule produced by wild-type E. carotovora strain SCC 3193 involved in quorum sensing, controlling gene expression, and affecting cellular metabolism.

A potent inhibitor of autotaxin (IC50 = 2.8 nM in an in vitro enzyme assay); at 30 mg/kg, reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).

A synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist; inhibits androstenediol-dependent LNCaP cell tumor growth both in vitro (IC₅₀ = 6 nM) and in vivo.

n-Triacontanol is a plant growth regulator found in the plant cuticle waxes and in beeswax as the palmitate ester. n-Triacontanol has been reported to have growth enhancing properties when applied to the leaves of growing plants.

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC₅₀s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for…

A synthetic progestin that acts as a prodrug to norelgestromin and levonorgestrel; selectively binds the progesterone receptor and is androgenically neutral.

An orally bioavailable, reversible inhibitor of JAK1 and JAK2 (IC₅₀s = 5.9 and 5.7 nM, respectively) that has been shown to inhibit cytokine-induced phosphorylation of STAT3 in healthy human volunteers.

A dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC₅₀s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively); improves glucose homeostasis in diet-induced insulin resistant mice.

A thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection; can affect intracellular GSH concentration and ROS balance.

An EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 µM; an analog of EPEA, a natural N-acylethanolamide that impacts aging and inflammation.

A selective inhibitor of SCFMET30 ubiquitin ligase, an E3 ligase that regulates transcription, cell-cycle control, and immune response; at 5 μM, upregulates a set of methionine biosynthesis genes by altering the SCFMET30 complex, preventing ubiquitination of target proteins, including Met4.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

A highly selective inhibitor of PLD1 (IC50 = 3.7 nM) versus PLD2 (IC50 = 6.4 μM).

An irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases; at 20-200 µM arrests human epidermoid carcinoma A431 cells at mitotic metaphase; inhibits protease-resistant protein accumulation in scrapie-infected neuroblastoma cells (IC₅₀ = 0.5 µM).

A compound used to increase the levels of H₂S within mitochondria; stimulates mitochondrial electron transport and improves cellular bioenergetic function at lower concentrations (30-100 nM), while having an inhibitory effect at 300 nM; is effective in vivo.

An inactive analog of U-73122; can be used as a negative control.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A DR5 agonist (Kd= 1.2 µM; IC₅₀ = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

A potent, reversible, and cell permeable proteasome inhibitor; a more effective inhibitor of chymotrypsin-like, trypsin-like, and peptidylglutamyl peptide hydrolyzing proteasome activities compared to (S)-MG132 (IC₅₀s = 0.22 versus 0.89 µM (ChTL); 34.4 versus 104.43 µM (TL);…

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 selective inhibitor of the TGF-β type1 receptor ALK5 (IC₅₀s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively); used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2…