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An orally available, semi-synthetic penicillin antibiotic.
A purine analog with immunosuppressive effects; serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with lymphocyte proliferation; used to benefit IBD, as well as additional diseases with immunological or autoimmunological components.
PGF2α methyl ester is an analog of PGF2α in which the C-1 carboxyl group has been esterified as the methyl ester. PGF2α methyl ester was one of the first PG esters shown to have ocular hypotensive activity. This compound continues to be a standard by which other ocular hypotensive...
A potent, selective, and orally bioavailable antagonist of MCP-1 binding to CCR2 (IC50 = 3.7 nM); inhibits chemotaxis in vitro (IC50 = 4.7 nM) and displays acceptable oral bioavailability in mice, rats, dogs, monkeys, and chimpanzees.
An intermediate in the synthesis of tetrahydrofolic acid in many non-mammalian organisms, including bacteria and fungi; metabolized by a variety of enzymes in mammals, including N-acetyltransferases; may also be utilized by bacteria or fungi that are living in mammalian organisms.
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 natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.
A secondary metabolite produced by some species of lichen that binds FAS-II enzymes to produce antibacterial and antiplasmodial effects; inhibits PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei (IC50...
A diglycan that binds galectins-1, -3, -8, and -9 with Kd values between 24 and 78 µM; used to investigate the roles of these galectins in cell signaling and carcinogenesis.
An endogenous ligand of the NOP1 (ORL1) receptor (Ki = 88 μM) involved in pain, memory, stress responses, anxiety, locomotion, and feeding behavior.
A potent and selective inhibitor of autotaxin, inhibiting recombinant autotaxin β with an IC50 value of 8.8 nM; inhibits LPA release from adipocytes (IC50 = 90 nM) and reduces plasma autotaxin activity by 57% when used at 5 μM.
A potent, selective, orally active inhibitor of COX-2 with an IC50 value of 10 nM and approximately 18,000-fold selectivity for COX-2 over COX-1
An inhibitor of FASN that strongly suppresses the growth of human breast cancer cell lines (IC50 = 21 µM for SK-BR-3 cells); also blocks the GTP-binding site of the cell division protein FtsZ from Bacillus, preventing bacterial division.
A β1-adrenergic receptor antagonist (Kis = 1.14 and 48.7 µM for β1 and β2, respectively); has applications in cardiology and vascular disease.
A thienyl cycloalkanone that is part of the NCI small molecule repository.
A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC50s = 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively); demonstrates antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM) and in an FGFR-driven...
A dual inhibitor of COX and 5-LO enzymes (IC50 = 0.73, 0.31, and 0.99 μM for COX-1, COX-2, and 5-LO, respectively, in whole blood).
The racemic version of a CYP450 metabolite of arachidonic acid that potently inhibits proximal tubule ATPase activity.
The COX Activity Assay utilizes the peroxidase component of cyclooxygenases. The peroxidase activity is assayed colorimetrically by monitoring the appearance of oxidized TMPD at 590 nm.The assay can be used to measure COX activity (COX-1 and COX-2) in cell lysates, tissue homogenates, and purified...
A nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (IC50 = 2.7 nM); does not alter PPARγ activity.
The PLAs are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The iPLA2 are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-BEL is an irreversible,...
A lipopeptide antibiotic effective against resistant Gram-positive bacteria (MIC90s range from 0.25-16 mg/L); alters bacterial plasma membrane potential and redirects the binding of proteins essential for cell division and cell wall synthesis.
A lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.
A synthetic CMR1/TRPM8 super agonist that is 2.5-fold more efficacious and nearly 200-fold more potent than the reference cold thermosensory agonist, l-menthol.