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.

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

A selective, reversible inhibitor of FAS (pIC₅₀ = 7.8).

A cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.

An isomer of Vitamin E that has less potent antioxidant properties than α-tocotrienol.

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 flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, antioxidant, antitumor, and neuroprotective activities at concentrations from 5-75 μM.

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…

An inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

A carboxylic acid-based inhibitor of aldose reductase (IC₅₀ = 0.01-15 μM) that suppresses high glucose-induced proliferation of vascular smooth muscle cells as well as prevents high glucose-induced intracellular NADH/NAD+ increase and membrane-bound protein kinase C activation.

A selective dual inhibitor of mTORC1 and mTORC2.

A selective cell-permeable inhibitor of non-muscle myosin II ATPases, inhibiting Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC₅₀ = 0.5-5.0 μM), while poorly inhibiting smooth muscle myosin (IC₅₀ = 80 μM).

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

A small molecule pan activator of Ras-related GTPases, activating cdc42, Ras, and Rac1 with EC₅₀ values of 102, 109, and 151 nM, respectively.

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

A small molecule inhibitor of KCNJ1 (IC₅₀ = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 µM; has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 µM.

A dibenzoxazepine which acts as a selective antagonist of PGE2 at the human EP1 receptor (IC₅₀ = 6.7 µM); at doses between 0.3-300 µM, is a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach and trachea.

A water-soluble, slow-releasing H2S donor which demonstrates vasodilator and anti-hypertensive activity in hypertensive rats when given intravenously; also protects against endotoxic shock in rats, inhibiting pro-inflammatory signaling.

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 broad spectrum, orally available kinase inhibitor that targets primarily tyrosine kinases, including VEGFR and EGFR, with IC₅₀ values in the nanomolar range; also potently blocks non-receptor tyrosine kinases, including ABL, RET, and SRC, as well as several serine/threonine kinases.

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 selective agonist of S1P3 (EC₅₀ = 72-132 nM); less effectively activates S1P1 (EC₅₀ = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.

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 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).

An N-cyanosulphonamide that selectively blocks the sodium/bicarbonate cotransporter (NBC, also known as SLC4A7) with a Ki value of 1.7 µM, with full inhibition occurring at ~30 µM in myocytes; prevents changes in pH associated with depolarization and hyperpolarization of ventricular myocytes.

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

A selective inhibitor of STAT3 activation, dimerization and nuclear translocation (IC₅₀ = 5.1 μM at 37°C); 10 μM induces apoptosis in STAT3-dependent breast cancer cells.

An amino acid derivative and an intermediate, by-product, or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis; also a product of SAM-dependent methylation of biological molecules, including DNA, RNA, and histones, and other proteins.

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

A potent inhibitor of calcium release-activated calcium channels in lymphocytes (IC₅₀ = 100 nM); also inhibits lung IL-4 and CysLT generation in animal models of asthma.

A cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC₅₀ = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC₅₀s = 820, 565, and 89 nM for p110α, β, and γ, respectively); blocks constitutive PI3K…