N4-Benzoyl-7’-O-(4,4’-dimethoxytrityl oxy)morpholinocytosine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Acetyl dipeptide-1 cetyl ester (Calmosensine) is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
Cilostazol(OPC 13013; OPC 21) is a potent inhibitor of PDE3A, the isoform of PDE 3 in the cardiovascular system (IC50=0.2 uM).IC50 Value: 0.2 uM [1]Target: PDE3Ain vitro: Cilostazol caused a concentration-dependent increase in the cAMP level in rabbit and human platelets with similar potency. Furthermore, cilostazol and milrinone were equally effective in inhibiting human platelet aggregation with a median inhibitory concentration (IC50) of 0.9 and 2 microM, respectively. In rabbit ventricular myocytes, however, cilostazol elevated cAMP levels to a significantly lesser extent (p < 0.05 vs. milrinone) [2]. Cilostazol inhibited SIPA dose-dependently in vitro. The IC50 value of cilostazol for inhibition of SIPA was 15 +/- 2.6 microM (m +/- SE, n=5), which was very similar to that (12.5 +/- 2.1 microM) for inhibition of ADP-induced platelet aggregation. Cilostazolpotentiates the inhibition of SIPA by PGE1 and enhances its ability to increase cAMP concentrations [3].in vivo: A single oral adminstration of 100 mgcilostazol to healthy volunteers produced a significant inhibition of SIPA [3]. Male C57BL/6J mice were assigned to five groups: mice fed a normal diet (groups 1 and 2); 0.1% or 0.3% cilostazol-containing diet (groups 3 and 4, respectively); and 0.125% clopidogrel-containing diet (group 5). Two weeks after feeding, groups 2-5 were intraperitoneally administered carbon tetrachloride (CCl4 ) twice a week for 6 weeks, while group 1 was treated with the vehicle alone [4].Toxicity: Cilostazol in addition to dual antiplatelet therapy appears to be effective in reducing the risk of restenosis and repeat revascularization after PCI without any significant benefits for mortality or stent thrombosis [5].
SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.IC50 value: 3.76 nM (Kd)Target: OX1 receptorSB-674042 has no effect at serotonergic, dopaminergic, adrenergic or purinergic receptors. Inhibits orexin 1-induced Ca2+ mobilization in CHO-DG44 cells stably transfected with the OX1 receptor.
Werner syndrome RecQ helicase-IN-1 (example 42) is a potent Werner syndrome RecQ DNA helicase enzyme (WRN) inhibitor and can be used in cancer research[1].
Folate-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47)[1].
Salvifaricin is an orally active diterpenoid compound that can be isolated from Salvia leucantha Cav. and Salvia hispanica L.. Salvifaricin significantly reduces fasting blood glucose and serum triglyceride (TG) levels, and has anti-diabetic effect[1][2].
AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines[1].
1-O-Acetyl 2,3,5-tri-O-benzoyl-beta-D-ribofuranoside-13C is the 13C labeled 1-O-Acetyl-2,3,5-Tri-O-benzoyl-beta-D-Ribofuranose[1].
N-Succinyl-Ile-Ile-Trp-AMC is a peptide-based fluorescent substrate or probe for carboxypeptidase Y (CPY)[1].
4-Fluorobenzyl chloride-d6 is the deuterium labeled 4-Fluorobenzyl chloride[1].
Tidiacic is a hepatoprotective agent that acts as an antioxidant and a sulfur donor[1].
UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC50s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively. UCN-02 (7-epi-Hydroxystaurosporine) displays cytotoxic effect on the growth of HeLa S3 cells[1][2].
Kanosamine hydrochloride is an antibiotic which inhibits the growth of plant-pathogenic oomycetes, certain fungi and a few bacterial species. Kanosamine inhibits Phytophthora medicaginis M2913 and Aphanomyces euteiches WI-98 with MICs of 25 and 60 µg/mL, respectively.
1-(2-C-β-Methyl-β-D-ribofuranosyl)-5-nitropyridine-2(1H)-one is a nitropyridine nucleoside analogue.
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CLpro. 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases[1].
OSMI-1 is a cell-permeable, small molecule O-GlcNAc transferase (OGT) inhibitor with IC50 of 2.7 uM; inhibits protein O-GlcNAcylation in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans; also significantly decreases HSV replication.
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction[1][2][3].
Z-L-Dap(N3)-OH is a click chemistry reagent containing an azide group. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity[1].
Tucatinib (Irbinitinib; ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with an IC50 of 8 nM.
GSK-2793660 is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis[1][2].
(D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH is an analogue of luteinizing hormone-releasing hormone (LHRH). LHRH plays a central role in the control of reproduction by stimulating the release of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH)[1].
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism[1].
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
Sialylglyco peptide is a N-Glycan and sialate glycopeptide[1].
Biotin-PEG4-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1].
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects[1][2].