A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.2 and 5 nM, respectively); studied in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

A cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator.

Formal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C₁₂H₁₅Cl₂NO

A phorbol ester that is commonly used to activate certain types of protein PKC and, indirectly, certain MAP kinase pathways; prolonged treatment with PMA produces various effects, ranging from tumorigenesis to hematopoietic differentiation.

A lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.

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

An antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC₅₀ values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways.

A cyanoquinoline that irreversibly inhibits the receptor tyrosine kinases EGFR (IC₅₀ = 39 nM) and HER2 (IC₅₀ = 1.2 μM); disrupts Akt and MAPK pathways, inducing apoptosis and suppressing the growth of tumor cell lines.

A potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively); effective in treating allergic rhinitis and conjunctivitis; does not cause cognitive or psychomotor impairment at…

An inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs; reduces ethylene-mediated plant changes in growth and development; inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.

A cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.

A selective GPR55 inverse agonist that antagonizes GPR55 constitutive activity (IC₅₀ = 15 μM); blocks GPR55-mediated endothelial wound healing and reverses LPI-inhibited platelet aggregation.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

A potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC₅₀ = 3.2 and 26 µM, respectively).

A selective inhibitor of ASK1 (IC₅₀ = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

An abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.

A potent inhibitor of calcium release-activated calcium channels in lymphocytes (IC₅₀ = 100 nM); also inhibits lung IL-4 and CysLT generation in animal models of asthma.

A natural monoacylglycerol that is metabolized by monoacylglycerol lipase; an agonist of GPR119 (EC₅₀ = 2.5 µM), stimulating the release of glucagon-like peptide-1 from intestinal L-cells.

A broad spectrum tyrosine kinase inhibitor that blocks angiogenesis through its actions on VEGFR isoforms; has low nanomolar efficacy against VEGFR1 (FLT1), VEGFR2, VEGFR3 (FLT4), and KIT, as well as CSF1R, PDGFRA, and PDGFRB; effective in vivo and useful in the management of certain types of cancer.

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

Chrysophanol is an anthraquinone originally found in species of Rheum. Chrysophanol exhibits anti-inflammatory, antiviral, antibiotic, and anticancer activities. In animal models of cerebral ischemia/reperfusion, chrysophanol inhibits activation of the NALP3 inflammasome, ameliorating…

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

Selective, nonpeptide antagonist of the CRH-R1 (Ki = 1 nM) that, consequently, reduces the release of corticotropin in response to chronic stress.

A potent and selective inhibitor of Vps34 (IC₅₀ = 25 nM in vitro); induces a rapid and pronounced loss of phosphorylation of SGK3.

CAS Number: 883986-34-3 Molecular Formula: C₂₄H₂₅N₅O₄ Formula Weight: 447.5

A small molecule inhibitor of nucleophosmin dimers that can prevent cell proliferation and induce apoptosis in various cancer cell lines (IC₅₀s = 1.4-4 µM).

A potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

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,…