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An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells.
A natural flavonoid with antioxidant, anti-inflammatory, and anticancer properties; inhibits HIF-1α expression in cancer cells; decreases pro-inflammatory gene expression and oxidative stress in ischemia/reperfusion injury.
A potent, competitive inhibitor of HMG-CoA reductase (Ki = 2.3 nM).
Ins(3)P1 is a member of the inositol phosphate (InsP) molecular family of second messengers that play a critical role in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3, is a second messenger produced in cells by PLC-mediated hydrolysis of...
A fluorescent probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
6α-PGI1 is a stable PGI2 analog resistant to hydrolysis in aqueous solutions. 6α-PGI1 promotes cAMP accumulation in human thyroid slices and cells in a concentration dependent manner. However, it is about 10-fold less potent than the β-isomer and 100-fold less potent than PGI2 in...
A cell-permeable antagonist of calmodulin (Ki = 11 μM); also associates, at lower affinities, with calcium-binding domains of other proteins, including troponin C and myosin light chain kinase (Ki = 70 and 300 μM, respectively).
An inhibitor of RSKs.
A lipophilic analog of 17-trifluoromethylphenyl trinor PGF2α.
Blocks lysosomal acidification through selective inhibition of the V-type ATPase (EC50 = 2.1-2.3 μM); blocks cell surface expression of viral glycoproteins without affecting their synthesis and, at 0.8 μM, prevents entry of influenza virus into cells.
A non-metabolizable glucose analog widely used as a glycolytic inhibitor to study metabolic activity with related to cancer, neurodegeneration, calorie restriction, and aging.
Molecular Formula: C19H24N10O • 2CH3SO3H
An agonist of human CAR (EC50 = 49 nM); induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes.
An inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM); alters the expression of genes in the MAPK, NF-κB, and...
An agonist of RORγt, inducing reporter gene expression with an EC50 value of ~800 nM; increases expression of IL-17, while decreasing expression of PD-1, in a variety of T cells.
A high-affinity TP receptor antagonist; produces platelet shape change, but not aggregation, with an EC50 value of 9.7 nM.
A secondary bile acid with hepatoprotective properties; inhibits apoptosis, in part by interfering with the mitochondrial pathway of cell death, inhibiting ROS, reducing ER stress, and stabilizing the unfolded protein response.
A selective inhibitor of PAF-AH1b2- and 1b3-mediated hydrolysis of PAF to lyso-PAF (IC50s = 37 and 880 nM, respectively); impairs Neuro2a and PC3 tumor cell survival at 10 µM.
A metabolite of lipoxygenase-mediated oxidation of DHA; activates Nrf2-dependent antioxidant gene expression, acts as a PPARγ agonist (EC50 = ~200 nM), and inhibits pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 µM).
13,14-dihydro-15-keto PGF2α-d4 contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of 13,14-dihydro-15-keto PGF2α by GC- or LC-MS.
Cayman’s TMRE Mitochondrial Membrane Potential Assay Kit utilizes tetramethylrhodamine ethyl ester (TMRE), a cell permeable, cationic dye which accumulates in the mitochondrial matrix based on mitochondrial membrane potential (ΔψM). This assay, which is suitable for high-throughput...
A non-selective inhibitor of NOS isoforms in vitro (IC50s = 0.71, 0.78, and 5.8 µM for rat nNOS, bovine eNOS, and rat iNOS, respectively); shows good anti-nociceptive effects without affecting blood pressure via inhibition of eNOS in vivo.
A trisubstituted purine which binds microtubules, reversibly altering cellular function; it directly binds tubulin, disrupts the structure of the microtubule cytoskeleton, and arrests cell cycle in the G2/M phase.
The more predominant-occurring (~80%) stereoisomer of the endogenous oxysterol 27-hydroxy cholesterol.