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 selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

The ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…

A hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM; orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.

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.

A more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).

An intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.

A cyanoquinoline that irreversibly inhibits the receptor tyrosine kinases EGFR (IC₅₀ = 39 nM) and HER2 (IC₅₀ = 1.2 μM); disrupts Akt and MAPK pathways, inducing apoptosis and suppressing the growth of tumor cell lines.

A cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.

A potent, bioavailable JAK inhibitor with preference for JAK2 (IC₅₀ = 2 nM) over JAK1 and JAK3 (IC₅₀s = 130 and 250 nM, respectively); effective against JAK2V617F as well as JAK2 and inhibits phosphorylation of STAT5 in vivo.

A selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC₅₀ = 0.04-0.28 µM) over BD1 (IC₅₀ = 1.8-3.1 µM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces…

A selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC₅₀ = 26.4 nM; Ki = 5 nM).

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 thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC₅₀ = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).

A cell-permeable selective PDE4 inhibitor.

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.

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 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).

An intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.

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 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 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.

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.

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.