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An analog of valeric acid, long used as an anticonvulsant; inhibits Class I HDACs with an IC50 of ~2 mM; also inhibits GSK3 and depletes cellular IP3.
Antigen: phosphopeptide corresponding to amino acid residues surrounding phospho-Ser774 of rat dynamin Host: sheep Cross-reactivity: (+) rat dynamin Application: WB
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).