screening

Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active, competitive inhibitor of heme oxygenase-1 (HO-1) that markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 and exhibits anti-cancer activity.

The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list of targets. Stability data is not available for the compounds as supplied in the screening library.

PD 198306 is a selective inhibitor of MAPK ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.

Compound V007-6018 is a pharmaceutical compound used for drug screening.

(Z)-2-fluoro-1,3-bis(4-methoxyphenyl)prop-2-en-1-one is a screening compound and can be used in new drug development related research.

Thiamine monophosphate chloride dihydrate (Aneurine monophosphate chloride) is a compound used in the screening of ligands that promote protein stability

AKOS002039287 is an aromatic derivative containing a sulfonamide group, which can be used as a potential drug screening compound and biochemical reagent.

Scopolin (Scopoloside) formation is increased by the enhanced activity of PAL. Scopolin can reduce the clinical symptoms of rat AIA by inhibiting inflammation and angiogenesis, and this compound may be a potent agent for angiogenesis related diseases and can serve as a structural base for screening more potent synthetic analogs.

G150 inhibited interferon expression triggered by DSDNA with IC50 of 10.2 nM.G150 is an effective and highly selective inhibitor of human cyclic GMP-AMP synthase (H-CGAS).

NSC 601980 analog, an analog of NSC601980, demonstrates antitumor activity in yeast screening experiments.

NSC601980 demonstrates antitumor potency, as evidenced by its ability to inhibit cell proliferation in the COLO 205 and HT29 cancer cell lines, achieving Log GI 50 values of -6.6 and -6.9, respectively, in yeast screening experiments.

Bentiromide acetate is a peptide used as a screening test for exocrine pancreatic insufficiency and to monitor the adequacy of supplemental pancreatic therapy. It is broken down by the pancreatic enzyme chymotrypsin, yielding p-aminobenzoic acid (PABA).

CCT251236 is a cell-based phenotypic high-throughput screening (HTS) chemical probe developed to screen for inhibitors of the HSF1 stress pathway.CCT251236 exhibits antimyeloma activity and inhibits HSF1.

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

Glutarylcarnitine (O-glutaroyl-L-carnitine) is a diagnostic metabolite for malonic aciduria and glutaric aciduria type I monitored in most tandem mass spectrometry newborn screening programmes.

2-Azaadamantane-N-oxyl (AZADO) is a compound known for its antioxidative activity, capable of efficiently scavenging free radicals. It has been extensively studied in compound development, demonstrating potential inhibitory effects against various diseases. The structure of AZADO lends itself to excellent biocompatibility, making it suitable for screening in innovative compound development.

Emavusertib Mesylate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, demonstrating antitumor activity. In cell lines of ABC DLBCL and AML, CA-4948 shows significant cellular activity. Moreover, it exhibits moderate to high selectivity in screening assays of 329 kinases and has impressive pharmacokinetic and pharmacodynamic profiles (ADME and PK), with good oral bioavailability in mice, rats, and dogs. In pertinent tumor models, CA-4948 achieves over 90% tumor growth inhibition and shows excellent correlation with in vivo PD modulation.

TC-AQP1-1 is a blocker of the aquaporin 1 channel identified by virtual screening and inhibits water flux through hAQP1 in Xenopus laevis oocyte swelling assays at low micromolar concentrations.

Isamfazone is utilized in the chemical and pharmacological studies on substituted pyridazones, the discovery of novel anti-inflammatory agents by aligning screening.

(+)-Biotin 4-amidobenzoic acid is a substrate of biotinidase, which cleaves biotin amide to give biotin in vivo. Biotin is an essential coenzyme for certain carboxylases and is used to modify histones and regulate gene transcription. Biotinidase has key roles in intestinal absorption of biotin, the transport of biotin in plasma, and in the regulation of histone biotinylation. (+)-Biotin 4-amidobenzoic acid is hydrolyzed by biotinidase to release 4-aminobenzoic acid (PABA), which can be quantified by either fluorescent or colorimetric methods. This approach is used in biotinidase activity assays in newborn screening protocols to evaluate biotinidase deficiency.

25-Desacetyl rifampicin is a major active metabolite of the rifamycin antibiotic rifampicin .125-Desacetyl rifampicin is active againstM. smegmatis(MIC99= 2.66 μM). 1.Kigondu, E.M., Njoroge, M., Singh, K., et al.Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolitesMed. Chem. Commun.5502-506(2014)

NSC 15364 (1,3-Bis(4-aminophenyl)urea) can be used for screening of ALR inhibitors by detection of hydrogen peroxide production Measured in Biochemical System.

Oasomycin B is a bacterial metabolite that has been found inS. baldaciiand has antiprotozoal activity.1It is active againstT. vaginalis(MIC = 62.5 μg/ml). 1.Grabley, S., Kretzschmar, G., Mayer, M., et al.Secondary metabolites by chemical screening, 24. Oasomycins, new macrolactones of the desertomycin familyLiebigs Ann. Chem.5573-589(1993)

TAS-103 is a dual inhibitor of DNA topoisomerase I II, utilized in cancer research.