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15(S)-HETE is a major arachidonic acid metabolite produced by the 15-LO pathway. It has been characterized as a potent inhibitor of 5-LO. The mechanism by which 15(S)-HETE acts as a leukotriene inhibitor is not clear. In studies with P-18 mast/basophil cells, it was shown that specific 15-HETE...
A fluorescent molecular rotor characterized by low background fluorescence, low fluorescence anisotropy, and good water solubility; its large hydrophobic structures allow it to associate in a non-covalent manner with hydrophobic pockets in proteins in solution.
A natural isoflavone which promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.
This formulation of 15-deoxy-.DELTA.12,14-PGJ2 contains 90-95% of the trans,trans-.DELTA.12,14 isomer, and 5-10% of other double bond isomers which have similar PPARγ ligand activity (see Catalog No. 18570).
A monohydroxy fatty acid derived from arachidonic acid; synthesis of 11-HETE by rat PMNL has been reported, but the stereochemistry of the 11-HETE produced is not defined.
An inhibitor of PARPs which can be used in cells or in animals; binds and inhibits the PARP TNKS1 (IC50 = 1 μM); inhibits MMP-2 when used at higher concentrations (IC50 = 56 μM).
A S-nitrosothiol that acts as an NO donor under acidic conditions; decomposes with a half-life of one minute in 0.1 M phosphate buffer, pH 5.0, at 37°C; relaxes phenylephrine-constricted rat aortic strips 59% and 16% at pH 6.0 and 7.4, respectively.
A pyrrotopyrimidine-based, multi-targeted antifolate with broad in vivo antitumor activity; potently inhibits multiple folate-dependent enzymes involved in both purine and pyrimidine synthesis (Kis range from 7 nM - 9.3 μM).
Antigen: human recombinant Nod2 amino acids 28-301 Host: mouse, clone 2D9 Cross Reactivity: (+) human Nod2 Application(s): IHC and WB Nod2 is a member of the apoptosis regulating protein family that has caspase recruitment-domains (CARDs) and also includes Apaf-1 and Nod1. Nod1 and Nod2 act as...
A competitive antagonist of capsaicin activation of the TRPV1 (IC50s = 24.5 and 85.6 nM for human and rat, respectively); reverses thermal and mechanical hyperalgesia in a rat model of inflammatory pain.
A polyunsaturated triacylglycerol with α-linolenoyl (18:3) side-chains attached at the C-1, C-2, and C-3 positions that is useful in lipid research.
The kinesin-like spindle protein Eg5 (also known as kinesin-5, kinesin family protein 11, or Kif11) is a motor protein that is essential for establishing a bipolar spindle during mitosis both in normal and tumor cells. Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM) with...
A naturally derived macrolide that inhibits actin polymerization in vitro at 5-10 µg/ml; demonstrates cytotoxic activity in mouse KA31T and NIH3T3 tumor cells (GI50s = 1 and 4 µg/ml, respectively) and antiviral activity against HSV-1 (ED50 = 1 µg/ml).
A partial CB receptor agonist isolated from the bark of M. officinalis that has been used in Asian traditional medicine for the treatment of anxiety, sleep disorders, and allergic diseases; demonstrates selectivity for the peripheral CB2 receptor subtype (EC50 = 3.28 μM; Ki = 1.44...
The 1'S stereoisomer of the naturally occurring nicotine metabolite, nicotine-1'-N-oxide.
A reversible ERK1/2 inhibitor (IC50 value of 180 nM).
A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.
15-deoxy-.DELTA.12,14-PGJ2-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 15-deoxy-.DELTA.12,14-PGJ2 by GC- or LC-mass spectrometry.
A quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versus IC50s > 10 μM for JAK1 and JAK2); also inhibits EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and...
A PPARα agonist and hypolipidemic drug used clinically to treat dyslipidemia and cardiovascular disease; exhibits EC50 values of 18 and 30 µM for mouse and human PPARα, respectively.
An internal standard for the quantification of PGF2α-1-glyceryl ester by GC- or LC-MS.
A muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum; inhibits a component of store-operated calcium entry (SOCE) that is coupled to the skeletal muscle ryanodine receptor, with 20 µM azumolene causing a 70% reduction in SOCE in myotubes.
An inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and Smac from mitochondria; prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation; inhibits the nuclear translocation of AIF, preventing the death of OVCAR-3 cells induced by...
A cell-permeable inhibitor of Epac1 and Epac2 (IC50 = 5.9 µM for Epac2); inhibits Epac1-mediated Rap1-GDP exchange activity at 25 µM, but has no effect on PKA activity; blocks Epac-mediated phosphorylation of Akt in HEK293 cells expressing either Epac1 or Epac2.