Moxalactam (Latamoxef) is a synthetic oxa-β-lactam antibiotic. Moxalactam has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Moxalactam inhibits production of β-lactamases[1].
Tubulin polymerization-IN-52 (compound SC23) is a potent tubulin polymerization inhibitor, with an IC50 of 2.9 μM[1].
Ro 64-6198 is a nonpeptidic, selective, brain-penetrant agonist of nociceptin/orphanin FQ receptor (NOP receptor/ORL1) with pKi of 9.41; displays >100-fold selectivity for ORL1 over other members of opioid receptor family; elicits dose-dependent anxiolytic-like effects in models of distinct types of anxiety states in rata, with no efficient anti-panic-like activity, absence of anticonvulsant properties, and lack of effects on motor performance and cognitive function at anxiolytic doses (0.3 to 3 mg/kg i.p.). Anxiety Discontinued
Bevasiranib sodium is a siRNA designed to silence the genes that produce vascular endothelial growth factor (VEGF). It is widely accepted that vascular endothelial growth factor (VEGF) is a key component in the pathogenesis of choroidal neo-vascularization (CNV), which is a precursor to wet age-related macular degeneration (wet AMD).
Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia[1][2].
Gymnoside I (compound 1) is a glycosidoxybenzyl 2-isobutylmalic acid. Gymnoside I shows antiallergic activity in passive cutaneous allergic reaction (PCA) in mice. Gymnoside I can be used in research to treat asthma, neurasthenia and chronic hepatitis[1].
Cys-Gly-Tyr-Gly-Pro-Lys-Lys-Lys-Arg-Lys-Val-Gly-Gly is a13-mer synthetic peptide containing seven amino acids homologous to SV40 T antigen. Cys-Gly-Tyr-Gly-Pro-Lys-Lys-Lys-Arg-Lys-Val-Gly-Gly is capable of inducing nuclear transport[1].
PMQA (Zn-green), an 8-aminoquinoline-based ratiometric fluorescent sensor, demonstrates the Zn2+-induced redshift of emission (85 nm). PMQA (Zn-green) is a cell membrane-permeable probe and suitable for imaging Zn2+ in living cells[1].
Eciskafusp alfa is a programmed cell death 1 (PDCD1, best known as PD-1) cis-targeted IL2v immunocytokine. Eciskafusp alfa preferentially targets antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells and differentiates them towards a novel population of better effectors. Eciskafusp alfa can be used for the research of cancer and chronic infections[1].
JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively[1].
PROTAC Linker 7 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 7 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
ART-IN-1 (compound 7) is a selective PARP inhibitor with IC50s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively[1].
PARPi-FL is a small molecule and fluorescent inhibitor of PARP1. PARPi-FL is a highly selective probe and can be used as an imaging agent to detect glioblastomas in vivo[1].
CI-943 is a potential antipsychotic agent.
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity[1][2].
(-)-Catechin, isolated from green tea, is an isomer of Catechin having a trans 2S,3R configuration at the chiral center. Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain[1][2][3].
6-Acetyl-2,2-dimethylchroman-4-one is a natural compound with low anti-cancer activity[1].
Benazepril-d5 (hydrochloride) is deuterium labeled Benazepril (hydrochloride).
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity[1]. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase[2].
111-Trifluoroethyl-PEG4-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Famitinib malate (SHR1020 malate), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer[1][2].
Betamethasone 17-benzoate is a representative steroid, which can be used in the treatment of recurrent aphothous ulcers (RAU).
PROT-IN-1 (Compound 2) is a proline transporter (PROT) inhibitor (IC50: 1.48 μM). PROT-IN-1 can be used for research of cognitive disorders[1].
Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively[1].
AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.
Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation[1].
12-Oxograndiflorenic acid is a natural product that can be isolated from vegetative Ambrosia hispida. Synonyms is ent-12-oxokaura-9(11),16-dien-19-oic acid[1].
Chrysophanol-1-O-β-gentiobioside, an anthraquinone glycoside isolated from Cassia obtusifolia seeds. Chrysophanol-1-O-β-gentiobioside shows selective inhibition of hMAO-A isozyme activity (IC50=96.15 μM)[1].