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.

An immunosuppressant used to prevent transplant rejection; potent inhibitor of IL-2 activation of lymphocytes (IC50 = 5 pM); specifically interacts with FKBP12 to form a complex which inhibits mTORC1.

A non-steroidal androgen receptor antagonist (IC50 = 36 nM); reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

A selective inhibitor of the Src family of non-receptor tyrosine kinases (IC₅₀s = 2 and 6 nM for Lck and Src, respectively); used in combination with PD 0325901, CHIR99021, and SB-590885 to support self-renewal of naïve human embryonic stem cells.

A stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.

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…

An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…

A potent blocker of HCN channels that inhibits HCN4 more potently than HCN1 (IC₅₀s = 32 and 158 nM, respectively); modulates the sinoatrial node and slows heart rate; reduces neuropathic pain in several animal models.

A potent and selective inhibitor of Wip1 (IC₅₀ = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.

An agonist for mCAR (EC₅₀ = 20 nM) that is effective for the mouse receptor but not for human or rat CAR receptors; potently induces cytochrome P450 monooxygenases and multidrug resistance and xenobiotic efflux proteins.

An indole-based SERM that binds to both ERα (IC₅₀ = 26 nM) and ERβ (IC₅₀ = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and…

A potent lipid signaling molecule that exhibits a wide range of biological activities; it enhances cell growth and inhibits the normal apoptotic response to a variety of stimuli.

A thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides.

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 selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay (pA2 = 8.1); demonstrates analgesic activity in a mouse writhing assay (ED50 = 0.9 mg/kg); potentiates the vasorelaxation of human pulmonary vein induced by PGE2 (EC50 = 7.75 µM).

An allosteric, reversible inhibitor of PAR1 on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC₅₀ value of 0.26 µM; also blocks platelet activation induced by thrombin but not by PMA, U-46619, or collagen.

A skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions.

A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC₅₀ = 5 nM); inhibition of GSK activates the Wnt-signaling pathway and sustains pluripotency in human and mouse ESCs; maintains…

Mn(III)TMPyP is a cell-permeable SOD mimic and peroxynitrite decomposition catalyst. The rate constants for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M−1s−1 and ~2 x 106 M−1s−1, respectively.

A cell-permeable inhibitor of Arp2/3 complex action that inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC₅₀s = 4, 32, and 24 µM, respectively); prevents the formation of actin filament comet tails by Listeria in infected SKOV3 cells…

A selective antagonist of the dopamine D3 receptor (pKi = 8.0); has high oral bioavailability and enters the central nervous system of the rat.

An inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ; blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ; selectively toxic to some carcinoma cell lines expressing the…

A stable, monomethoxylated resveratrol derivative that at 0.1-10 μM reduces neurotoxicity in SH-SY5Y cells induced by the parkinsonian mimetic 6-OHDA and scavenges DPPH radicals (IC₅₀ = 47.1 μM).

A selective inhibitor of ASK1 (IC₅₀ = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…

A lipophilic activator of PKA and PKG (Ka = 0.05 and 0.11 μM, respectively); inhibits PDE VA, PDE III, and PDE IV with IC50 values of 0.9, 24, and 25 μM, respectively.

A potent, non-ATP-competitive inhibitor of Plk1 (IC₅₀ = 9 nM); induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM); active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents.

A sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles; selectively inhibits the growth of influenza A and B viruses in plaque reduction assays (IC₅₀s = 5-14 nM) and to directly inhibit influenza A and B virus neuraminidases…

A potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

An endocannabinoid analog that does not bind to CB1, CB2, or TRPV1; at 5 mg/kg antagonizes the hypotensive effects of a 10 mg/kg IV bolus of abnormal cannabidiol (Abn-CBD) in an anesthetized rat blood pressure model; relaxes isolated rat mesenteric arteries and abdominal aorta, and increases the…

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);…