Kissoone A (compound 1) is a three-membered ring sesquiterpene isolated from valerian root[1].
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca2+-activated K+ channels in various types of neurons[1].
Me-Tet-PEG4-NHS is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-NHS can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.
6-TAMRA-SE is an amine-reactive form of tetramethylrhodamine; one of the traditional fluorophores used for automated DNA sequencing.
Tirabrutinib (ONO-4059) is a highly selective, orally bioavailable BTK inhibitor with an IC50 of 2.2 nM.
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity[1][2][3][4].
(S)-2-Amino-6-((tert-butoxycarbonyl)amino)hexanoic acid is a lysine derivative[1].
BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity[1][2].
JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research[1][2][3].
2-(2-(6-chlorohexyloxy)ethoxy)ethanamine (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Arcyriaflavin A is a fungal metabolite obtained from the fungi, Nocardiopsis sp[1].
Ginsenoside F5, from crude extracts of flower buds of Panax ginseng, remarkably inhibits the growth of HL-60 cells by the apoptosis pathway[1].
J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis[1].
MC-Val-Cit-PAB-retapamulin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-retapamulin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
Coronalolide methyl ester (NSC 680073) is a natural triterpene with anticancer effects. Coronalolide methyl ester shows moderately cytotoxic to KATO-3, SW-620, and Hep-G2 cells., with IC50 values of 8.64 µg/mL, 6.19 µg/mL, and 6.8 µg/mL, respectively[1].
H-Glu-Obzl is a glutamic acid derivative[1].
Obtusilin is a natural product isolated from Eucalyptus camaldulensis leaves[1].
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia[1][2].
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2[1].
Biotin-PEG4-amino-t-Bu-DADPS-C6-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis[1].
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease[1].
Fmoc-Lys(Tfa)-OH is a lysine derivative[1].
ISX-1 is an isoxazole. ISX-1 has anti-adipogenic and pro-osteogenic activities. ISX-1 can be used for the research of osteopenia and osteoporosis[1].
11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
3,5-Bis-O-(4-methylbenzoyl)-2-C-methyl-D-ribonic acid gama-lactone is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
3’,5’-Di-O-benzoyl thymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
PD-1/PD-L1-IN-24 is a highly potent PD-1/PD-L1 inhibitor with IC50 value of 1.57 nM. PD-1/PD-L1-IN-24 can restore T-cell function at the cellular level by significantly elevating the IFN-γ level. PD-1/PD-L1-IN-24 has low toxicity on the PBMCs[1].
Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL)[1][2].