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A 7,7-difluoroprostacyclin derivative that acts as a selective and highly potent agonist for the IP receptor (Ki = 0.561 nM); shows weaker affinity for EP receptors, with Ki values of > 100 nM for EP1-3 and > 10 nM for EP4.
Inhibits several isoforms of protein kinase C (PKC; IC50 = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.
A short chain fatty acid that inhibits HDACs, induces growth arrest, differentiation and apoptosis in cancer cells, and suppresses inflammation by reducing the expression of pro-inflammatory cytokines.
An end product of phenylalanine metabolism in humans and primates.
A BTK inhibitor.
A synthetic analog of Joro spider toxin that blocks GluR2-lacking, Ca2+-permeable AMPA receptors (IC50 = 0.33 µM) at -60 mV but not at +40 mV; protects against ischemia-induced neuronal cell death by preventing influx of toxic levels of Ca2+ into injured neurons.
The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1. In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production. In several...
An ATP-competitive inhibitor of ATR (IC50 = 26 nM); augments DNA damage and cell death of cancer cells in response to radiation under normal and hypoxic conditions; sensitizes cancer cells to chemotherapy.
An inhibitor of PGE2 production through the selective modulation of mPGES-1 expression; dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells (IC50 = 1.8 µM) without affecting COX-2 expression.
A reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 14 nM; IC50 = 1.8 μM), which is the main receptor responsible for ADP-induced platelet aggregation; directly changes the conformation of the P2Y12 receptor to inhibit ADP binding.
A chromogenic PLA2 substrate that contains an ether-linked saturated C16 moiety at the sn-1 position and a thiol ester at the sn-2 position.
This nuclear receptor assay system utilizes proprietary human cells engineered to provide constitutive, high-level expression of the human thyroid hormone receptor alpha (NR1A1), a ligand-dependent transcription factor commonly referred to as TRα. INDIGO’s reporter cells include the...
A highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion; directs delayed cell death by apoptosis in HepG2 cells (IC50 = ~1 nM).
A cell-permeable inhibitor of furin (IC50 = 12 μM); inhibits furin-mediated cleavage of the pro-form of membrane type-1 matrix metalloproteinase MT1-MMP, resulting in decreased levels of active MT1-MMP; inhibits the invasion of Matrigel by the human fibrosarcoma cell lines HT1080.
A synthetic vitamin D2 analog; used in renal patients to block parathyroid hormone overproduction.
Antigen: phosphopeptide corresponding to amino acid residues surrounding phospho-Thr180 and phospho-Tyr182 of rat p38 MAPK Host: rabbit Cross Reactivity: (+) human p38 MAPK Application(s): WB p38 MAPK is activated by both inflammatory cytokines and by stress. It is thought to be particularly...
A tyrosine kinase inhibitor (IC50 = 370 nM).
An isothiocyanate that potently induces chemopreventative enzymes via Keap1-Nrf2 signaling and ARE-driven gene expression; at 15 μM, inhibits class I and II HDAC activity and suppresses tumor growth selectively in cancerous prostate epithelial cells without affecting normal cells.
A potent and selective PPARγ ligand, binding to the PPARγ ligand-binding domain with a Kd value of 43 nM.
An internal standard for the quantification of N-arachidonoyl dopamine by GC- or LC-MS.
A potent, selective inhibitor of mutant IDH2 (IC50 = 23 nM) that inhibits 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q (IC50s = 11 and 18 nM, respectively); suppresses cell growth of primary human AML cells and induces differentiation of...
An internal standard for the quantification of resolvin D1 by GC- or LC-MS.
An internal standard for the quantification of HPA by GC- or LC-MS.
An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces...