Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors[1].
Azido-PEG4-nitrile is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Boracic acid is an antiseptic agent. Boracic acid is bland and unirritating[1].
Moracin O is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin O exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects[1][2][3].
SMS2-IN-1 is a highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM.
3,8''-Biapigenin is a biflavone in Hypericum perforatum L.[1].
2,2′-Binaphthyl-d14 is the deuterium labeled 2,2′-Binaphthyl[1].
Cy5-DBCO (DBCO-Sulfo-Cy5) is a near-infrared (NIR) red fluorescent dye with λabs and λem of 646 nm and 670 nm, respectively. Cy5-DBCO (DBCO-Sulfo-Cy5) is not suitable for staining intracellular components of permeabilezed cell, it may exhibits a high background.
SARS-CoV-2-IN-19 (Compound 6g) is a potent inhibitor of SARS-CoV-2 with an EC50 of 8.8 μM. SARS-CoV-2-IN-19 shows potent activity against SARS-CoV-2 helicase (nsp13), a highly conserved enzyme, highlighting a potentiality against emerging HCoVs outbreaks. SARS-CoV-2-IN-19 has the potential for the research of infection diseases[1].
Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
N-(NBD-Aminolauroyl)safingol is a fluorescent group.
Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively. Frovatriptan succinate hydrate is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine[1][2].
Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways[1].
Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively.
BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.IC50 Value: 6-35 nM [1]Target: SmoothenedSMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.in vitro: In vitro, BMS-833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) in cell lines that express wild-type SMO and those which express activated mutant forms of SMO (IC50values of 6-35 nM). In FACS-based binding assays, BMS-833923 inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM [1]. in vivo: Pharmacodynamic studies show that BMS-833923 robustly inhibits HH pathway activity with along duration of action after a single oral dose in medulloblastoma and pancreatic carcinoma xenograft models. The pharmacodynamic effects of BMS-833923 observed in these models translate into tumor growth inhibition at well-tolerated doses [1].Clinical trial: Dasatinib Combo With Smoothened (SMO) Antagonist (BMS-833923). Phase 2
4-Chloronaphthalen-1-ol is a substrate of horseradish peroxidase. 4-Chloronaphthalen-1-ol can be used to visualize protein bands in western blotting[1][2].
Digadoglucitol is a diagnostic agent in the field of imaging, especially as a contrast agent for the field of magnetic resonance imaging (MRI)[1].
Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM[1].
Sec61-IN-2 (A3) is a protein secretion inhibitor (extracted from patent WO2020176863)[1].
Light green SF yellowish (Acid Green 5) is a triarylmethane dye. Light green SF yellowish is a highly selective mitochondrial stain. Light green SF yellowish is usually available as a disodium salt and has a maximum absorption value as 629 nm. Light green SF yellowish can be used as a histological stain for collagen and a critical component of Papanicolaou stains[1][2].
Cadherin Peptide, avian is a calcium-dependent glycoprotein. Cadherin Peptide, avian takes part in homophilic cell-cell adhesion and dose-dependently inhibits bovine brain microvessel endothelial cells (BBMECs) adhesion[1].
H-Met-Glu-OH is a biologically active peptide.
Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.
Acetylcysteine-d3 (N-Acetylcysteine-d3) is the deuterium labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor[1]. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases[5]. Acetylcysteine induces cell apoptosis[2][3]. Acetylcysteine also has anti-influenza virus activities[7].
EB-3D is a novel potent and selective choline kinase ChoKα inhibitor with IC50 of 1.0 uM (purified ChoKα1), strongly impairs cell proliferation in a variety of different cancer cell lines; demonstrates in vitro antiproliferative effects against HeLa (IC50=79 nM), RS4,11 (IC50=45 nM), A549 (IC50=27 nM) and MDA-MB-231 (IC50=100 nM); displays excellent antiproliferative activity against a wide cohort of T-leukemic cell lines with GI50 of 0.9 nM (MOLT-16 cell)-479 nM (CCRF-CEM), reduces the intracellular pool of PCho, but also inhibits the synthesis of choline-containing lipids; induces G0/G1 arrest that lead to apoptosis in leukemia cell lines; affects AMPK-mTOR signaling pathway, synergizes with both dexamethasone and L-asparaginase.
ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122[1].
NCX 1000 is a liver-specific NO donor compound derived from ursodeoxycholic acid (UDCA).
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM[1].
Bis(8-methyl-1-nonyl) Phthalate-3,4,5,6-d4 is the deuterium labeled Bis(8-methyl-1-nonyl) Phthalate[1].