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A prodrug of gemcitabine designed for improved oral bioavailability; inhibits the growth of human non-small cell lung cancer NCI-H460 cells, colon cancer HCT116 cells, and breast cancer MCF-7 cells both in vitro (IC50s = 0.78, 0.92, and 0.64 μM, respectively) and in xenograft cancer...
A cell-permeable quinazolinyl-urea compound that has been shown to inhibit Gli transcription activity (IC50 = 70 nM).
A cell-permeable acyl urea first identified as an inhibitor of human liver glycogen phosphorylase (IC50 = 53 nM); blocks glucagon-induced hepatic glycogenolysis in vivo.
A methyl ester version of 17(R)-RvD1 which may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties.
An endogenous ceramide, generated by ceramide synthase 6, that acts a lipid second messenger to regulate apoptosis and stress signaling.
A CDK inhibitor that most potently inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdc2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively); inhibits the growth of parasites, including Plasmodium, at micromolar doses.
An abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.
A polyphenolic anthocyanin with high antioxidant activity, protecting erythrocytes from apoptosis; impairs growth and induces apoptosis in the highly tumorigenic RE-149 DHD cell line; inhibits a range of mammalian and bacterial proteases, including neutrophil elastase, MMP-1, and MMP-9.
A triazolothiadiazine that inhibits PDE4 (EC50 = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC50 = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC50 = 48.2, 37.2, 452, and 49.2 nM, respectively).
A naturally occuring deaminated sialic acid that is thought to be a precursor for the biosynthesis of other members of the sialic acid family; can be used to analyze nonulosonic acid residues in polysialoglycoproteins.
A synthetic peptide that blocks PKC activity in HepG2 cells stimulated with calcium and diacylglycerol when applied at 10 µM.
Source: Active recombinant N-terminal His-tagged enzyme amino acids 101-399 purified from E. coli Mr: 37 kDa (theoretical); 33.5 kDa (observed) SIRT3, is a mitochondrial protein that is synthesized as an enzymatically inactive protein. Human SIRT3 is activated by a matrix-processing peptidase. The...
A natural bacterial product that activates GPR132 (also known as G2A) with an EC50 value of 11.8 µM.
An indole-based, time-dependent inhibitor of Icmt (IC50 = i = 0.14 µM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells.
An isotopically enriched form of a PUFA standard with carbon-13 occurring at positions 1, 2, 3, 4, and 5; used to study metabolic processes related to arachidonic acid by means of mass spectrometry.
An inactive enantiomer of nutlin-3 that may serve as a useful control for non-MDM2 related cellular activities; also called enantiomer b based on the elution pattern during chiral separation of (±)-nutlin-3.
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.
Inhibits Gli1-mediated transcription (EC50 = 5 μM) in a variety of cell types disrupting the hh signaling pathway downstream of Smo and Sufu; displays antiproliferative and antitumor activity against Ewing sarcoma family of tumor cells.
A potent, reversible 5-LO inhibitor, blocking LTB4 synthesis with an IC50 value of 0.7 μM in intact human polymorphonuclear leukocytes; also attenuates LTB4 synthesis, prevents carrageenan-induced pleurisy, and protects against PAF-induced shock in mice when given intraperitoneally.
L-Biopterin is the oxidized form of BH4, a NOS cofactor. L-Biopterin can be reduced to BH4 via thioredoxin reductase followed by dihydropteridine reductase or reduced glutathione. It is extremely toxic to human melanocytes in culture (IC50 = 0.2 µM after 48 hrs). L-Biopterin is rarely found...
A potent, selective inhibitor of TrkA (IC50 = 2 nM); used to clarify the role of TrkA in regulating cell function.
A hydrophobic bile acid formed in the liver by conjugation of lithocholate with taurine; induces apoptosis in hepatocytes at 75 µM; used to experimentally induce cholestasis.
A degradation product of the surfactant, Triton X that produces weak estrogenic effects in animal and human research studies.
This nuclear receptor assay system utilizes proprietary non-human mammalian cells engineered to provide constitutive, high-level expression of human liver X receptor alpha (NR1H3), a ligand-dependent transcription factor commonly referred to as LXRα. INDIGO’s reporter cells include the...