PGB1 is a non-enzymatic dehydration product of PGE1 resulting from treatment with strong base. Oligomers of PGB1 are known to exhibit antioxidant and ionophoric activity.

A selective inhibitor of JAK1 (IC₅₀ = 629 nM) that displays 30-fold selectivity for JAK1- over JAK2-dependent signaling in human whole blood; blocks IL-6/STAT1 and IL-2/STAT5 signaling in cell models and whole blood assays.

A selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding (IC50 = 31 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation, which reduces cell viability and induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).

CAS Number: 1000998-59-3 Molecular Formula: C₂₂H₂₁ClN₂O₆ Formula Weight: 444.9

An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC₅₀s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases, including p38γ and p38δ; blocks the phosphorylation of HSP27, a p38 MAPK substrate, in response to…

An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.

3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

A kaempferol glycoside that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC; inhibits the proliferation of MCF-7 breast cancer cells at 100 μM and attenuates angiotensin II-induced cell…

An inhibitor of PDKs, resulting in an increase in PDH activity (EC₅₀ = 5.2 nM for PDK2); less potently inhibits PDK1 and PDK3 (IC₅₀s = 87 and 600 nM, respectively).

A lipid peroxidation product derived from oxidized ω-6 PUFAs such as linoleic acid and arachidonic acid which is widely used as a marker of lipid peroxidation.

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

A potent inhibitor of HCV infection (EC₅₀ = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC₅₀ = 21.3 µM); displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without…

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

A specific and potent inhibitor of MPC carrier activity; potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC₅₀ = 50 nM).

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…

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.

CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

A selective inhibitor of PAD4 (IC₅₀ = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils.

An inactive analog of U-73122; can be used as a negative control.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

An HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in vitro (IC50 = 930 nM).

A steroidal saponin that displays cytotoxicity against a range of cancer cells in vitro, including leukemia, colon cancer, and prostate cancer cells (GI50 ≤ 2 µM).

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

A cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC₅₀ = 0.82-14 μM); inhibits glucagon-induced gluconeogenesis in primary hepatocytes.

An active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

A natural adenosine analog that prevents IRE1α-induced mRNA cleavage (IC₅₀ = 80 nM) and inhibits constitutive activation of XBP1 in multiple myeloma cell lines; used to study IRE1α action in the endoplasmic reticulum stress response.

A more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).

A small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.

A selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor); used to induce hyperemia, particularly in the context of myocardial perfusion imaging.

A small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism in bacteria; activates NF-κβ in RAW 264.7 macrophages, increasing the expression of TNF-α, IL-1β, and IL-8; alters cell cycling and…

A high-affinity fluorescent calcium indicator (Kd = 115 nM for calcium) that is ideal for monitoring low levels of calcium, as are found in resting cells; may be used to buffer intracellular calcium transients.

A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.