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A natural product which acts as a small molecule inhibitor of HIF signaling, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations; effectively attenuates the HIF pathway both in cells and in vivo, in mice.
A protopanaxatriol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-diabetic actions; protects against DNA damage and apoptosis induced by ultraviolet light.
A natural phthalide that induces the expression of GST and reduces chemical-induced carcinogenesis in mice; inhibits COX-1 and -2 at 250 pg/ml and blocks topoisomerase-I and-II activity at 100 µg/ml.
An inhibitor of GSK3α (IC50 = 34 nM, GSK3β similar) that stimulates glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM); induces expression of β-catenin-LEF/Tcf regulated reporter genes HEK293 cells.
A phospholipid containing the long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions.
An antitumor antibiotic that crosslinks double stranded DNA and is widely used as a tool to selectively inhibit DNA synthesis and mutagenensis, to stimulate genetic recombination, chromosome breakage and sister chromatid exchange, and to induce DNA repair.
1-Hexadecyl lysophosphatidic acid is an ether analog of LPA containing a hexadecyl group at the sn-1 position. LPA binds to five different GPCRs to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell...
A mycotoxin found as food contaminants that causes mycotoxic nephropathy in livestock and Balkan nephropathy and yellow rice fever in humans; induces apoptosis, blocks tubulin polymerization, and disrupts mitotic spindle assembly.
2-Aminomethylpyrimidine (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.
An adrenergic α1A receptor agonist (Ki = 1.4 µM) that demonstrates selectivity against the α1B and α1C receptor subtypes (Kis = 23.9 and 47.8 µM, respectively); frequently used to precontract smooth muscle in preparations designed to study the properties of various...
The precursor of OEA, an endogenous, potent agonist for PPARα (EC50 = 120 nM); OEA suppresses food intake and reduces weight gain in rats and PPARα wild-type mice, but not in PPARα knockout mice.
Docosatrienoic acid is a rare ω-3 fatty acid not readily detected in normal phospholipid PUFA pools. It inhibits [3H]-LTB4 binding to pig neutrophils at a concentration of 5 µM.
Antigen: phosphopeptide corresponding to amino acid residues surrounding phospho-Tyr1472 of NMDA Receptor NR2B Subunit Host: rabbit Cross Reactivity: (+) human and rat NMDA receptor; expected to react with bovine, canine, chicken, mouse, non-human primates, and zebrafish NMDA receptor...
Antigen: recombinant full-length protein (Item No. 15139) Host: rabbit Species Reactivity: (+) human Application(s): ELISA, IP, and WB
A selective PPARd agonist that acts as a partial agonist (EC50 = 53 nM) in transactivation assays and as a full agonist (EC50 = 30 nM) in the oxidation of free fatty acid; increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity in high fat fed ApoB100/CETP-transgenic mice...
A synthetic analog of PGF2α; an FP receptor agonist and a potent luteolytic agent in rats and hamsters; the optically active, 15(R) enantiomer of cloprostenol responsible for the majority of its biological activity.
An analog of 2-OG that has been developed as an inhibitor of HIF-PHs.
An inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (KD = 25 μM); prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis; blocks translation in some viruses that do not require eIF4E or a cap structure for...
A tacrine dimer, linked via a 7-carbon alkyl spacer; inhibits AChE (IC50 = 0.40 nM), making it more than 1,000 times more potent than tacrine ;protects against hydrogen peroxide induced apoptosis in rat pheochromocytoma cells.
A natural, potent and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively; also inhibits papain, calpain, and cathepsins B and H.
An inhibitor of JAK3 (IC50 = 79 nM); also inhibits the transglutaminases TGM2 and Factor XIIIa (IC50s= 10 and 25 nM, respectively) in the absence of dithiothreitol; breaks down in neutral buffer to form ZM 449829.
CZC-54252 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50s = 1.28 and 1.85 nM for wild-type and G2019S mutant forms of LRRK2, respectively). It has been shown to protect against neuronal injury induced by Parkinson’s disease-related LRRK2-G2019S mutant activity in...
A selective CRF1 antagonist (Ki = 4 nM); inhibits cAMP accumulation and ACTH production in vitro (pIC50s = 7.1 and 6.9, respectively) and reduces CRF- and stress-induced ACTH production in vivo.
A modified pyrimidine that is capable of producing interstrand cross-links in double-stranded DNA; used to quantify DNA hydroxymethylation levels in biological samples.