Cannabisin G is developed as a nutritional dietary supplement for immunocompromised individuals.
Antitubercular agent-25 (Compound 28) is an anti-tubercular agent with an extracellular IC50 of 0.42 μM and an intracellular IC50 of 0.20 μM against M. tuberculosis H37Rv. Antitubercular agent-25 exhibits good metabolic stability[1].
MS-PEG3-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
7-Acetoxy-1-methylquinolinium iodide (AMQI) is a fluorogenic substrate for cholinesterase (Ex = 320 nm, Em = 410 nm). Hydrolysis of 7-acetoxy-1-methylquinolinium iodide is used at the fluorometric flow system for the detection and identification of inhibitors.[1].
Bcl-2/Bcl-xl inhibitor 1 (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Bcl-2/Bcl-xl inhibitor 1 exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively[1].
LSP4–2022 is a novel potent, selective, brain-penetrant mGluR4 agonist with EC50 of 0.11 uM in cell-based assays; displays >100-fold selectivity over mGlu7 and mGlu8 (IC50=11.6 and 29.2 uM), no activity at the group I and -II mGlu receptors (EC50>100 uM); inhibits neurotransmission in cerebellar slices from mice, and possesses antiparkinsonian properties in a haloperidol-induced catalepsy test.
(R)-5-Hydroxy-1,7-diphenyl-3-heptanone is a diarylheptanoid that can be found in Alpinia officinarum. (R)-5-Hydroxy-1,7-diphenyl-3-heptanone ameliorates oxidative stress and insulin resistance via activation of Nrf2/ARE pathway[1].
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1].
Isoarundinin II is a stilbenoid compound[1].
m-PEG3-OMs is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977), inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively.
E3 ligase Ligand-Linker Conjugates 39 incorporates a cIAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 39 can be used to design PROTAC degrader[1].
2’-O-Me-2-thio-U-3’-phos phoramidite 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].
Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
N-(2-Pyrazinylcarbonyl)-D-phenylalanine is a phenylalanine derivative[1].
Goniodiol 8-acetate is a styrylpyrones that can be isolated from the leaves of Goniothalamus amuyon. Goniodiol 8-acetate has cytotoxic activity[1].
CL2 Linker is an ADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours)[1][2].
Bidenoside C (compound 10) is a polyacetylene glycoside (Polyacetylene Glycoside), which can be isolated from the flowers of Coreopsis lanceolata (Asteraceae)[1].
FABP-IN-2 is a novel FABP3 ligand. FABP-IN-2 inhibits FABP3/FABP4 with an IC50 of 1.16 μM and 4.27 μM respectively[1].
IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases[1][2].
Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders[1][2].
Drinidene can be used for the research of pain disorders extracted from patent AU2018254530A1[1].
Dasatinib D8 is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.
Bis(2-cyanoethyl) diisopropylphosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides[1].
BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research[1].
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glyc
Dim16 is a dual PCSK9/HMG-CoAR inhibitor, with an IC50 value of 19 nM for PCSK9. Dim16 inhibits PCSK9-LDLR binding with an IC50 value of 0.8 nM. Dim16 increases LDL uptake in HepG2 cells[1].
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
7-Cyano-7-deaza-2'-deoxy guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].