A cell-permeable selective PDE4 inhibitor.

A potent inhibitor of all three human Pim kinases (IC₅₀s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer…

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.

A natural isothiocyanate which induces the expression of phase II detoxification enzymes and activates Nrf2, promoting the expression of antioxidant and phase II genes; acts as a quorum sensing inhibitor, blocking acyl-homoserine lactone signaling in P. aeruginosa without affecting growth…

CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

C-6 ceramide is a cell-permeable analog of naturally occurring ceramides. With a longer carbon chain than C-2 ceramide, it is somewhat more hydrophobic, and may more closely mimic the effects of natural ceramides. C-6 ceramide mediates many diverse biological activities including apoptosis,…

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

A product of CYP2A6 metabolism of the primary nicotine metabolite, cotinine; as a biomarker of nicotine metabolism.

A potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively; less effectively inhibits NHE4 (IC₅₀ ≥10 μM).

A potent agonist of β-adrenergic receptors (pEC₅₀ = 8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively).

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC₅₀ = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC₅₀ = 0.6 µM); shows good in vivo potency and duration of action.

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

A small molecule inhibitor of human cytomegalovirus viral replication (EC₅₀ = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.

A selective GPR55 inverse agonist that antagonizes GPR55 constitutive activity (IC₅₀ = 15 μM); blocks GPR55-mediated endothelial wound healing and reverses LPI-inhibited platelet aggregation.

Mn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.

A small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

A cell-permeable inhibitor of JMJD2E (KDM4DL; IC₅₀ = 920 nM); reduces the expression of immediate early genes of HSV (IC₅₀ = ~10 µM) and hCMV, blocks viral infection, and suppresses the level of viral reactivation in a ganglia explant model of latently infected mice.

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

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

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 serotonin 5-HT1B and 5-HT1D receptor agonist (IC₅₀s = 9.3 and 7.3 nM, respectively) that also has affinity for the 5-HT1F receptor (IC₅₀ = 17.8 nM); constricts human middle meningeal arteries (EC₅₀ = 89.9 nM) and reduces vascular inflammation associated with migraines.

Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM. Iloprost…

2-Hydroxymyristic acid is an inhibitor of protein myristoylation requiring about 0.5 mM concentration for full inhibition of acylation.

A potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.

A selective, orally bioavailable inhibitor of Akt1, 2, and 3 (Kis = 0.08, 2, and 2.6 nM, respectively); inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies.

A cell permeable, competitive inhibitor of HIF-1α prolyl hydroxylase; stabilizes HIF-1α expression at normal oxygen tensions in cultured cells at concentrations between 0.1 and 1 mM.

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.

Formal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C₂₀H₁₉N₃O₂

A selective DNA-PK inhibitor (IC₅₀ = 14 nM) that increases the cytotoxicity of ionizing radiation and etoposide in human colon cancer cell lines in vitro and potentiates the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.

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 orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM) that inhibits thrombin formation without prolonging bleeding time; approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.

A chromogenic cephalosporin substrate commonly used to detect β-lactamases in bacteria and other microbes.