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PLC catalyzes the hydrolysis of phosphatidyl inositol (4,5) bisphosphate (PIP2) on the cytoplasmic side of the cell membrane to yield diacylglycerol and inositol-1,4,5-triphosphate (IP3). This reaction initiates a well-known signal transduction pathway common to most cells. PLC thio-PIP2 is an...
A potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM); can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.
A cell-permeable green fluorescent dye (excitation and emission maxima are 494 and 520 nm, respectively); used to analyze cell proliferation and track cell migration in vivo.
A potent and selective inhibitor of class I α-mannosidases and serves as a key inhibitor of glycoprotein biosynthesis; inhibits both human ER α-1,2-mannosidase I and Golgi class I mannosidases (Golgi α-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM, respectively;...
A minor component of the oligomycin complex that acts as an inhibitor of the mitochondrial F1FO-ATP synthase, which leads to cell death.
One of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid.
LTD4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. It is the first CysLT metabolite of LTC4. Like LTC4, LTD4-induced bronchoconstriction and enhanced vascular permeability contribute to the...
A naturally occurring PUFA formed through a 2-carbon chain elongation of arachidonic acid; present in the adrenal glands, brain, testis, and kidney.
A natural alkaloid in the betel nut; an agonist of the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5; causes smooth muscle contraction; has been shown to improve learning and memory and may prove to be useful in treating dementia.
An intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.
A synthetic compound made up of the arginine-glycine-aspartate motif used to inhibit integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation; also can directly induce apoptosis by activating pro-caspase-3.
JTE-013 is a potent, selective S1P2 receptor antagonist that binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, (IC50 values >10 µM for human S1P1 and S1P3). It reverses the inhibitory effects of S1P on cell migration of vascular endothelial cells and...
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.
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.
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.
Melatonin is a hormone of the pineal gland. Hormone; mediates photoperiodicity in mammals; inhibits cerebellar nitric oxide synthetase; peroxynitrite scavenger. Melatonin has complex effects on apoptotic pathways, inhibiting apoptosis in immune cells and neurons but enhancing apoptotic cell death of...
A potent inhibitor of PKC (IC50 = 2.7 nM for the rat brain enzyme).
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).
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.
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...
An inhibitor of the ERAD pathway, blocking the degradation of misfolded proteins at a dose of 8 µM; associates with the p97-associated deubiquitinating complex in cells, preventing deubiquitination of substrates by ataxin-3; interferes with both retrograde and anterograde trafficking of...
A hydrophobic peptide chemosensitizer that reverses P-glycoprotein-mediated multidrug resistance; binds to the P-glycoprotein multidrug transporter (MDR1; Kd = 77 nM).