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An esterified form of the free acid which may be more amenable for certain applications.
A steroidal lactone present in W. somnifera that induces aggregation of vimentin, peripherin, neurofilament-triplet protein, and keratin intermediate filaments as well as disrupt the organization of microtubules and actin/microfilaments, causing apoptosis; potential anti-tumor agent to target...
8(S),15(S)-DiHETE is formed when 15(S)-HETE is subjected to further oxidation by 15-LO. It causes eosinophil chemotaxis with an ED50 value of 1.5 µM but is not chemotactic for neutrophils. 8(S),15(S)-DiHETE antagonizes the hyperalgesic activity of 8(R),15(S)-DiHETE and LTB4 in the...
A histamine H2 receptor antagonist that decreases gastric acid secretion (ED50 = 0.9 µM in isolated gastric mucosa of bullfrog and ED50s = 1.383 and 0.08 μmol/kg in rats and dogs, respectively).
A natural isoflavone which is biotransformed by intestinal bacteria to give the phytoestrogens daidzein and equol, resulting in antithrombotic, antiallergic, and other salutary effects; modulates serotonin receptors when given intraperitoneally; suppresses LPS-mediated activation of NF-κB in...
An intertnal standard for the quantification of 2,3-dinor TXB2 by GC- or LC-MS.
An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines...
A PI3Kα inhibitor (IC50 = 0.8 nM) that demonstrates antiproliferative activity in T47D, SK-BR-3, and MCF-7 cells with IC50 values of 0.6, 1.5, and 7.8 μM, respectively; induces apoptosis and blocks angiogenesis both in vitro and in vivo.
An inhibitor of UCH-L1 activity (IC50 = 0.88 Ki = 0.4 μM) that demonstrates selectivity for UCH-L1 compared to UCH-L3 (IC50 = 25 μM); leads to cell death through the apoptosis pathway due to an impaired ubiquitin-proteasome pathway.
Phytanic acid is a saturated 20-carbon branched-chain fatty acid which can only be derived from dietary sources. In cases of peroxisomal disorders, elevated levels of phytanic acid have been observed, and this is linked to diseases such as infantile phytanic acid storage disease and Refsum’s...
A naturally occurring carnitine derivative formed by carnitine acetyltransferase during β-oxidation of uneven chain fatty acids; plays a role in mitochondrial metabolism and demonstrates beneficial cardiovascular effects as well as free radical scavenging activity.
A synthetic intermediate useful for pharmaceutical synthesis.
A synthetic estrogen that is effective in hormone replacement therapy; stored in adipose tissue, where it is slowly released and metabolized in the liver to its active form, ethynyl estradiol.
A nonsteroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzein by human intestinal microflora; exhibits EC50 values of 200 and 74 nM for human ERα and ERβ, respectively and induces breast cancer cell proliferation in vitro at concentrations as low as 100...
An inhibitor of TORC1/2, acting as a sub-nanomolar ATP-dependent inhibitor of mTOR kinase; interferes with the growth of cell lines which are resistant to rapamycin and pan-PI3K inhibitors; inhibits angiogenesis and tumor growth in several xenograft models; reduces invasion and metastasis.
O-ASHA is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible manner with a...
A potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM); less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets; prevents LPS-induced synthesis of TNF-α in...
A potent inhibitor of PLD, inhibiting human PLD1 and PLD2 in vitro (IC50 = 220 and 310 nM, respectively) and PLD activity in cells; inhibits the dopamine receptor.
A triazole derivative that serves as the active ingredient in a formulation that is used in adjunctive treatment of LGS to limit seizure frequency.
A reversible inhibitor of serine proteases such as trypsin (Ki = 0.06 pM), chymotrypsin (Ki = 9.5 nM), and kallikrein (Ki = 0.8 nM); widely used as a protein purification tool to prevent proteases present in tissue samples from degrading the protein of interest.
A topically-active imidazole antifungal compound that has broad spectrum activity in vitro against dermatophytes, molds, yeasts, dimorphic fungi, and some Gram-positive bacteria; a potent inhibitor of cytochrome P450 aromatase (Ki = 68 nM, IC50 = 270 nM).
15(S)-HETE-d8 contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14, and 15 positions. It is intended for use as an internal standard for the quantification of 15(S)-HETE by GC- or LC-MS.
An immunosuppressive mycotoxin which inhibits 20S proteasomal chymotrypsin activity (IC50 = 10 μM), preventing activation of NF-κB; induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils; inhibits geranylgeranyltransferase I and farnesyltransferase (IC50...
A metabolite of cefpodoxime proxetil, the oral third generation cephalosporin antibiotic that demonstrates potent activity against most Gram-positive and Gram-negative bacteria (MIC90 ranges from 0.015-8 µg/ml).