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A potent and selective EP1 receptor antagonist (IC50 = 2.5 nM), with >400-fold selectivity relative to EP2, EP3, EP4, DP1, and IP; has 30-fold selectivity over TP; shows complete anti-hyperalgesic activity in a rat model of chronic inflammatory joint pain.
The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo....
A potent, cell impermeable inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).
A dye used to stain proteins for IEF and SDS-PAGE; fluoresces near infrared (absorption maximum: 624 nm).
A small molecule pan activator of Ras-related GTPases, activating Rac1, cdc42, Ras, and Rab-2A with EC50 values of 20, 100, 141, and 355 nM, respectively.
A constituent of the Chinese herb Artemisia identified as having anticoagulant, hypolipidemic, vasorelaxant, antioxidant, and anti-inflammatory actions in experimental models.
A natural phenol which inhibits the monocarboxylate transporters MCT1 and MCT2 (IC50 = 28 and 14 µM, respectively); also blocks the sodium/D-glucose cotransporter (Ki = 86 µM) and the human concentrative nucleoside transporter 3 (Ki = 32 µM).
A mycotoxin that inhibits the mitochondrial ATP synthetase system; inhibits soluble ATPase (KD = 4.1 µM), ADP-stimulated respiration in isolated rat liver mitochondria (KD = 0.15 µM), and ATP-driven reduction of NAD+ by succinate (KD = 2 µM).
Progesterone, along with pregnenolone, is the biosynthetic precursor of all other steroid hormones. The main function of progesterone is to prepare the uterine lining for implantation of a fertilized ovum and to maintain pregnancy. Measurement of serum or plasma progesterone levels are used as an...
A fatty acid ester that potentiates the activity of other endocannabinoids, including 2-AG to bind to CB1 and CB2 and inhibit adenylyl cyclase; interacts with endocannabinoids in the modulation of pain sensitivity.
Antigen: recombinant human H-PGD synthase Host: mouse, clone 2A5 Cross-reactivity: (+) human and mouse H-PGD synthase Applications: IHC and WB Isotype: IgG2bκ
2-AG exhibits CB agonist activity at the CB1 receptor, is an important endogenous monoglyceride species, and is thus considered to be the natural ligand for the CB1 receptor. 2-AG can also be metabolized by COX-2 and PGD, E, F, and I synthases to form PG 2-glyceryl esters. PGF2α-SA is a stable...
The 6-keto PGF1α Quant-PAK has been designed for the convenient, precise quantification of 6-keto PGF1α by GC- or LC-MS. It includes a 50 µg vial of 6-keto PGF1α-d4 and a precisely weighed vial of unlabeled 6-keto PGF1α, with the precise weight (2-4 mg) indicated on the...
An antagonist of ERα that blocks 17β-estradiol-induced proliferation of drug-resistant cancer cell lines at concentrations ranging from 10 to 1,000 nM; drives tumor regression in mice bearing MCF-7 xenografts; inhibits ERα-dependent protein synthesis by activating the unfolded...
A phytoestrogen that competitively (vs. 17β-estradiol) binds the estrogen receptors ERα (IC50 = 11 nM) and ERβ (IC50 = 2 nM) and can induce ER-dependent gene expression in isolated cells; a weak antagonist of pregnane X receptor (IC50 = 12 μM).
The Epigenetics Screening Library contains more than 140 small molecules that are known to modulate the activity of a variety of epigenetic 'writers and erasers' and “reader” proteins in a 96-well Matrix tube rack format as 10 mM stocks in DMSO. It may include compounds that...
A potent, selective inhibitor of SPHK 1 with anti-proliferative activity; exhibits non-ATP-competitive inhibition of human recombinant GST-SPHK 1 with an IC50 value of 0.5 µM, with no inhibition against ERK2, PI3K or PKCα at concentrations up to 60 µM; inhibits proliferation of...
Estriol is a metabolite of estradiol and a major estrogen produced in the later stages of pregnancy. In a longitudinal study in healthy pregnant women, total plasma estriol levels increased from 10 weeks gestation to approximately 150 ng/ml at week 38. The majority of the estriol synthesized in the...
A nematicidal, insecticidal, antibacterial, and antifungal polyketide metabolite produced from A. westerdijkiae.
3-Thiopheneacrylic acid is a synthetic intermediate useful for pharmaceutical synthesis.
An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural...
A group A trichothecene mycotoxin derived by the metabolism of T-2 toxin.
The live cell multiplex (LCM) assay provides an efficient fluorescence-based method of quantifying the relative number of live cells resident in treated wells of an assay plate. While the LCM assay may be performed as a stand-alone assay, it is has been specifically optimized to be run in multiplex...
A partial agonist at 5-HT1A, 5-HT1B, and 5-HT2B receptors (Kis = 40, 52, and 81 nM, respectively); decreases aggressive behavior in resident-intruder tests with rats (ID50 = 0.24 mg/kg).