ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC₅₀s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…

A small molecule inhibitor of the TGF-β receptor type 1 kinase (IC₅₀ = 56 nM) that has been used to study the role of TGF-β signaling in triple negative breast cancer cells and hepatocellular carcinoma cells.

A potent and selective EP4 receptor antagonist (Ki = 24 nM); reverses the anti-inflammatory action of PGE2 in LPS - activated human macrophages at 100 nM.

A melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values = 10-27 and 158-513 nM, respectively); used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways.

A natural chalcone that has anti-inflammatory actions, supporting its use as a skin lightening agent, particularly for rosacea and atopic dermatitis; induces apoptosis and suppresses migration and invasion of cancer cells in vitro; has antibacterial and anti-parasitic actions.

PGE2 p-acetamidophenyl ester is a crystalline derivative of PGE2. PGE2 is one of the primary COX products of arachidonic acid and one of the most widely investigated PGs. Its activity influences inflammation, fertility and parturition, gastric mucosal integrity, and immune modulation. The effects…

A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks…

A cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

Inhibits several isoforms of protein kinase C (PKC; IC₅₀ = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…

A benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC₅₀ = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment…

CAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme. The in vivo pharmacological efficacy of CAY10499 has not been reported.

Eltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase…

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

A potent, non-ATP-competitive inhibitor of Plk1 (IC₅₀ = 9 nM); induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM); active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents.

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

A selective inhibitor of cFMS kinase (IC₅₀ = 0.03 μM) that prevents CSF-1-induced monocyte growth with an IC₅₀ value of 0.14 μM; at 75-100 mg/kg, inhibits joint connective tissue and bone degradation in mouse models of arthritis.

A hybrid molecule patterned after N-arachidonoyl serotonin; inhibits capsaicin-induced TRPV1 channel activation (IC₅₀ = 2.57 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC₅₀ > 50 μM).

A competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM); derepresses transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells at 250 µM.

O-ASHA is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible manner with a…

An LPA analog containing palmitic acid at the sn-1 position.

An LDH inhibitor (Kis = 5.46 and 15.06 µM, for the A and B isoforms, respectively) that prevents proliferation of many different cancer cells by blocking glycolysis and ATP production.

Formal Name: N-?[[(4-?aminophenyl)?amino]?thioxomethyl]?-?4-?(1,?1-?dimethylethyl)?-benzamide CAS Number: 1011301-27-1 Molecular Formula: C₁₈H₂₁N₃OS

A selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.

Hexanolamino PAF C-16 is a PAF analog with mixed PAF receptor agonist/antagonist properties. In human monocyte-derived macrophages, it is an antagonist which inhibits the production of reactive oxygen species in response to PAF C-16. On the other hand, in rabbit platelets and guinea pig…

A stable inhibitor of FAS that leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.

A natural macrocyclic antibiotic that inhibits RNA polymerase with selectivity for Gram-positive bacteria over Gram-negative bacteria (IC₅₀s = 0.4 and 6 μM, respectively); has potent antibacterial activity against most Gram-positive bacteria and effectively targets the Gram-positive…

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

An antibiotic that can inhibit cell wall synthesis in plant-pathogenic oomycetes (MIC = 25 µg/ml for P. medicaginis M2913) and certain fungi as well as some bacterial species (MIC = 400 µg/ml for S. aureus).

Selectively inhibits human NHE-1 with an IC₅₀ value of 14 nM; reduces infarct size in a rabbit myocardial ischemia-reperfusion model without adversely affecting hemodynamics or cardiac function.