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A potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM).
Inhibits PKCδ (IC50 = 3 μM), CAM kinase III, and a wide range of protein kinases, including PRAK and MAPKAP-K2 (IC50s = 1.9 and 5 μM, respectively); stimulates autophagy by targeting a signaling cascade upstream of mTORC1.
A fluorescent molecule that can be used to detect cholesterol by fluorescence and freeze-fracture electron microscopy.
An intermediate form of vitamin D which is obtained from dietary sources, such as fish, or through the conversion of 7-dehydrocholesterol by ultraviolet light; metabolized to the active form 1,25-dihydroxyvitamin D3 by CYP450 isoforms in the liver.
DL-α-lipoic acid is a cyclic disulfide antioxidant that interconverts with its reduced dithiol form. It is an essential cofactor for decarboxylation reactions of the citric acid cycle, and acts as a general antioxidant.{12280,12281,12322} DL-α-lipoic acid can act as a direct radical...
Traumatic acid is a product of the hydroperoxide lyase pathway in plants. It is a wound healing agent that stimulates cell division near a wound site to form a protective callus.
AMC-AA is one of several fatty acid amides which can be used to measure FAAH activity. Exposure of AMC-AA to FAAH results in the release of the fluorescent aminomethyl coumarin that absorbs at 360 nm and emits at 465 nm, allowing for fast and convenient measurement of FAAH activity using a simple...
CAS Number: 1185039-20-6 Synonyms: GOE-3450-d4; Neurontin-d4 Molecular Formula: C9H13D4NO2 Formula Weight: 175.3
An inhibitor of Nrf2 (IC50 = 1.9 µM) that blocks downstream target gene expression; substantially enhances cytotoxicity in non-small cell lung cancer (NSCLC) cells treated with platinum-based drugs.
F16 is a small, cationic, lipophilic molecule which binds preferentially to mitochondrial membranes and disrupts their function. F16 was discovered in high throughput screens for tumor inhibitors, where it was found to induce apoptosis in HER-1/EGFR-expressing breast carcinoma cell lines. In...
A process impurity formed during the preparation of naratriptan.
An orally-active agonist of LXRα and LXRβ, activating the human isoforms with EC50 values of 190 and 30 nM, respectively; alters LXR-regulated gene expression in mice and rats, affecting pathways related to glucose and lipid metabolism.
A macrolactam that binds to macrophilin-12 and inhibits calcineurin as well as prolyl isomerase; the activation of T cells by allogeneic dendritic cells (IC50 = 0.55 nM) and suppresses the generation of pro-inflammatory cytokines; used in countering inflammatory skin diseases, such as...
Source: one ampoule contains salt-free GRX from E. coli Mr: 10 kDa
A compound used to increase the levels of H2S within mitochondria; stimulates mitochondrial electron transport and improves cellular bioenergetic function at lower concentrations (30-100 nM), while having an inhibitory effect at 300 nM; is effective in vivo.
A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM); inhibits the H3K79 methylation in various human leukemia cell lines (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression and inhibiting proliferation; intravenous infusion of...
A synthetic intermediate useful for pharmaceutical synthesis.
An 8-aza-9-oxo-15-hydroxy saturated analog of PGE2; selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3,000, 2,000, and >3,000 nM, respectively); stimulates cAMP formation in excised mouse ovaries.
BHT is a phenolic antioxidant and free radical scavenger. It has been shown to inhibit lipid peroxidation.
A potent, cell-permeable inhibitor of the tyrosine kinase activity of the epidermal growth factor (EGF) receptor (IC50 = 0.45 nM); effective in cells, blocking tyrosine phosphorylation induced by either EGF or heregulin (IC50s = 39 and 220 nM, respectively).
A cell-permeable inhibitor of PTPs (IC50s = 0.09-1.7 µM) through oxidation of the catalytic cysteine residue; inhibits redox-sensitive CYP isoforms with IC50 values less than 10 µM; inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3...
The aminonucleoside portion of PANS that is used to induce nephropathy in laboratory animal models to study focal and segmental glomerulosclerosis, the induction of nephrosis, and the events leading to proteinuria in rats.
Used as a substrate of guanylate kinases to generate dGDP, which in turn is phosphorylated to dGTP, a nucleotide precursor used in DNA synthesis; can be efficiently phosphorylated by the type I thymidylate kinase of the malarial agent P. falciparum.
10ml of 250 mM Tris-HCl, pH 7.6, containing 750 mM sodium chloride, 5% NP-40, 2.5% sodium deoxycholate, and 0.5% SDS