ACX-362E is an orally available DNA polymerase IIIC (pol IIIC) inhibitor, acts as an antimicrobial agent to treat Gram-positive infections, with a MIC50 of 2 μg/mL for C. difficile. ACX-362E displays very potent in vitro and in vivo activities against broad spectrum of C. difficile pathogens[1].
Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 µM[1][2].
1-Octacosanoyl glyceride is a natural compound that can be found in the wood of Catalpa ovate[1].
H2N-PEG2-CH2COOH belongs to a polyethylene glycol (PEG) linker covalently bound to E3 Ligase binding group (E3LB) and protein binding group (PB)[1].
PE 22-28 is a TREK-1 inhibitor with IC50 value of 0.12 nM. PE 22-28 also is a 7 amino-acid peptide that is used as a core sequence for preparing analogs by chemical modifications and also by substitution of amino-acids. PE 22-28 can be used for the research of depression[1].
5-BrdUTP sodium salt is a TdT substrate which can be used to label the DNA double-strand breaks.
β,β-Trehalose is a analog of trehalose. β,β-Trehalose can support the growth of shoot tips of Cuscuta. β,β-Trehalose can be cleaved by nonspecific β-glucosidase[1].
FH1(BRDK4477) is a small molecule that can enhance the functions of cultured hepatocytes.IC50 value:Target: In vitro: FH1(BRD-K4477) enhances hepatocyte functions, and promotes the maturation of well-differentiated cultures of iHeps, which potentially alleviates a major obstacle to the use of iPS cells as a renewable source of functional human hepatocytes.
Galanin-Like Peptide (rat) is a 60 amino acid neuropeptide. Galanin-Like Peptide (rat) plays an important role in the regulation of feeding, body weight and energy metabolism[1].
ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders[1][2].
Schisandrin C epoxide (compound 1) is a natural lignan found in Clerodendron inerme seeds[1].
KM02894 is an inhibitor of glutamate release. Cancer cells release high levels of glutamate, which disrupts normal bone turnover and may lead to cancer-induced bone pain. KM02894 can be used for cancer related research[1].
Vanillylmandelic acid is the endproduct of epinephrine and norepinephrine metabolism. Vanillylmandelic acid can be used as an indication of the disorder in neurotransmitter metabolism as well. Vanillylmandelic acid has antioxidant activity towards DPPH radical with an IC50 value of 33 μM[1].
Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV[1].
1-Bromoheptane-d3 is the deuterium labeled 1-Bromoheptane[1].
(S)-2-(tert-butoxycarbonylamino)-3-(4-carbamoyl-2,6-dimethylphenyl)propanoic acid is a phenylalanine derivative[1].
N-Feruloyloctopamine, isolated from Garlic skin, is an antioxidant constituent. N-Feruloyloctopamine significantly decreases the phosphorylation levels of Akt and p38 MAPK[1].
Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells[1].
Domvanalimab (AB154) is an anti-TIGIT humanized monoclonal antibody. Domvanalimab binds human TIGIT9 and blocks the TIGIT-CD155 interaction. Domvanalimab can be used in research of cancer[1].
UPF-648 sodium salt is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.IC50 value: 1 uM(81 ± 10 % inhibition) [1]Target: KMO inhibitorin vitro: BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity [1]. UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design [3].in vivo: Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA [1]. Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels [2]. UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation [3].
H-Gly-Leu-Phe-OH (GLF), an immunostimulatory tripeptide derived from α-lactalbumin, inhibits anticancer agent Etoposide-induced alopecia, epidermal thickening, and thinning of the adipocyte layer[1].
(2S)-5-Methoxyflavan-7-ol (compound 2) is a nature product that could be isolated form Dragon's blood resin[1].
Cyclohexanoyl coenzyme A is the active form of cyclohexane carboxylic acid (CHC) from anaerobic degradation in Rhodopseudomonas palustris[1].
Trilepisflavan is a flavan, which can be isolated from Trilepisium madagascariense. Trilepisflavan derivates serval analogues with anti-cancer activity against human cancer cells[1][2].
EC330 is a leukemia inhibitory factor (LIF) inhibitor.
Dirucotide (MBP8298) is a synthetic peptide that consists of 17 amino acids linked in a sequence identical to that of a portion of human myelin basic protein. Dirucotide can be used for the research in autoimmune disorder of the central nervous system, such as Multiple sclerosis (MS)[1].
Sograzepide (Netazepide;YF476) is a gastrin/cholecystokinin 2 receptor (CCK2) antagonist.
360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
FPH1(BRD-6125) increases the number and activity of primary human hepatocytes in vitro and promotes the differentiation of iPS cells towards a hepatic lineage[1].