A peptide antagonist of PAR2 which blocks activation by trypsin (IC₅₀ = ~50 μM) but not by the synthetic agonist SLIGRL-NH2; does not affect thrombin-induced activation of PAR1 or trypsin-mediated proteolysis of casein; used to study PAR2 action in cells and in animals.

A polysulfated disaccharide that is used as a reference standard for sucralfate.

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

A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

A dual inhibitor of DNA-PK and PI3K.

A selective inhibitor of human collagenase-3, also known as MMP-13, producing 89% inhibition at 10 µg/ml; used to evaluate the role of MMP-13 in diverse processes.

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

A broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

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);…

Blocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC₅₀ = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.

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 potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

A potent inhibitor of several CDKs with selectivity for Cdk2 (IC₅₀s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.

An inhibitor of the yeast PITP Sec14, blocking both Sec14-mediated transfer of [3H]-PtdIns in vitro and growth (IC₅₀s = 0.21 and 2.87 µM, respectively).

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 reversible inhibitor of the auto and transphosphorylation kinase activity of the ErbB receptor tyrosine kinase superfamily: EGFR (IC₅₀ = 8 µM), ErbB-2 (IC₅₀ = 49 nM), ErbB3, and ErbB4 (IC₅₀ = 52 nM); induces G1 cell cycle arrest in MCF10A breast cancer cells.

An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells.

Formed by the oxidation of ebselen; lacks antioxidant acitivity.

An L-type calcium channel blocker that is selective over N-, R-, P/Q- and T-type calcium channels; displays antihypertensive activity, lowering arterial blood pressure without altering cardiac contractility.

A biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.

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…

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.

Molecular Formula: C₁₃H₁₅IN₂O₂

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

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…

A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC₅₀ = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.

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 potent antagonist for the human IP (prostacyclin) receptor that antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cAMP accumulation in a dose-dependent manner; inhibits the binding of tritiated iloprost to rodent neuroblastoma cells (Ki = ~ 3 nM).

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.2 and 5 nM, respectively); studied in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors.