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A synthetic analog of PGD1 with a hydroxyl-group in place of the C-1 carboxylic acid.
An HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in vitro (IC50 = 930 nM).
PPA is the product of peroxidase-catalyzed reduction of PPHP. It can be used as a reference standard for HPLC analysis of peroxidase assays.
Antigen: human EP2 receptor amino acids 335-358 Host: rabbit Cross-Reactivity: (+) human, mouse, and rat EP2 receptors; (−) EP1, EP3, and EP4 receptors Application(s): FC and ICC
Reversibly and selectively blocks Tie2 kinase activity (IC50 = 250 nM); reduces angiogenesis in a Matrigel neovascularization assay and delays tumor growth in MOPC-315 plasmacytoma and SVR angiosarcoma xenograft models.
A natural 1,4-naphthoquinone that has diverse effects in cells and animals; causes the generation of ROS and induces apoptosis in cancer cells; activates signaling through Nrf2 and ARE, inducing the expression of Nrf2 target genes, including NQO1 and HO-1 in cultured neuronal cells.
A potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay); blocks B-RafV600E–dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50s = 78 and 60 nM, respectively); displays good oral bioavailability.
A pan-CDK inhibitor (IC50s = 3, 1, 1, and 4 nM for CDK1, CDK2, CDK5, and CDK9, respectively) that inhibits DNA synthesis in A2780 ovarian cancer cells (IC50 = 4 nM); 5 mg/kg prevents tumor growth by 50% in an A2780 ovarian carcinoma mouse xenograft model; active against a broad...
A broad-spectrum inhibitor of 2OG oxygenases that inhibits JMJD2 demethylase activity (IC50 = 87 μM); inhibits JMJD2A, JMJD2E and the 2OG oxygenases PHF8, PHD2, and FIH (IC50s = 1.7, 2.4, 13.3, 14.3, and 20.5 μM, respectively).
An analytical reference standard that is structurally similar to known phytocannabinoids; intended for research and forensic applications
A potent, reversible inhibitor of γ-secretase, reducing the cleavage of APP to Aβ40 in SH-SY5Y cells with an IC50 value of 5 nM; orally bioavailable and crosses the blood-brain barrier, as orally administered MK-0752 dose-dependently reduces the generation of new amyloid β...
Travoprost is the Alcon trade name for fluprostenol isopropyl ester, an F-series PG analog which has been approved for use as an ocular hypotensive drug. Fluprostenol isopropyl ester is a prodrug which is converted by esterase enzymatic activity in the cornea to yield the corresponding free acid,...
The initial compound identified in a screen for PAD4 inhibitors (IC50 = 3.2 µM in functional assay) that was optimized to produce the more potent PAD4 inhibitors, GSK484 and GSK199.
Ins(1,5)P2 is a member of the inositol phosphate (InsP) molecular family that play critical roles as small, soluble second messengers in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3 is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of...
Antigen: synthetic peptide from human PCSK9 amino acids 490-502 Host: rabbit Cross Reactivity: (+) human, murine, and rat PCSK9 Application(s): ICC and WB PCSK9 is a member of the subtilisin serine protease family with an important role in lipoprotein metabolism. Several gain of function mutations...
A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.
(R)-benzyl Mandelate is a synthetic intermediate useful for pharmaceutical synthesis.
A leptin standard set.
One of the stereoisomers of FTY720-phosphate that is apparently not formed in vivo; binds to S1P receptors with 5-130-fold lower affinity compared to FTY720 (S)-phosphate
AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194.
A natural chalcone with antibacterial, antifungal, anticancer, anti-reverse transcriptase, antitubercular, and antioxidant activities.
A fluorometric substrate for and competitive inhibitor of cytochrome P450 1A1; used to study the metabolism of arachidonic acid and the mechanisms of vasodilation; inhibits nitric oxide synthesis by uncoupling nNOS (Ki = 0.76 µM).
A competitive, selective antagonist of NMB receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines); blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.
The isoprostanes are a family of eicosanoids of non-enzymatic origin produced by the random oxidation of tissue phospholipids by oxygen radicals. Isoprostanes appear as artifacts in tissue and plasma samples which have undergone oxidative degradation during prolonged or improper storage. They also...