Phenanthrene is a polycyclic aromatic hydrocarbon (PAH) and has been frequently used as an indicator for monitoring PAH contaminated matrices[1]. Phenanthrene induces oxidative stress and inflammation[2].
H-DL-Glu(Ome)-OMe.HCl is a glutamic acid derivative[1].
α-2,3-sialyltransferase-IN-1 is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM.
BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.IC50 value: 200 nM (EC50, for LSCe cells)Target: DNA gyraseBRD7116 is a bis-aryl sulfone, shows evidence of stroma-mediated anti-LSCe activity. BRD7116 exhibits an EC50 of 200 nM for LSCe cells in co-culture, whereas it displays limited activity against normal HSPCs and AML cell lines (~50% inhibition at 20 μM). BRD7116 also shows activity against patient-derived, primary human leukemia cells. [1] BRD7116 inhibits LSCs via non-cell-autonomous effects on stromal cells as well as cell-autonomous induction of myeloid differentiation genes in LSCs.
DDAO is a promising near-infrared (NIR) red fluorescent probe with tunable excitation wavelength (600-650 nm) and long emission wavelength (λem = 656 nm). DDAO can de desiged for detection of the activities of different enzymes such as β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin and esterases[1].
5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities[1].
1-Octacosanoyl glyceride is a natural compound that can be found in the wood of Catalpa ovate[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.
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].
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].
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].
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].
(S)-2-((S)-2-((S)-2-Aminopropanamido)propanamido)propanoic acid is an alanine derivative[1].
264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action[1].