Wilfordinine D is a natural sesquiterpene alkaloid[1].
S-(4-Nitrophenyl)-L-cysteine is a cysteine derivative[1].
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively[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].
4-Methylherniarin (7-Methoxy-4-methylcoumarin) is a coumarin derivative and fluorescent label, has an antimicrobial activitiy against both gram positive and gram negative bacterial stains. 4-Methylherniarin displays good activity against B. subtilis and S.sonnei with IC50 values of 11.76 μg/ml and 13.47 μg/ml[1].
NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC50 of 0.15 nM. NSC81111 has anticaner effects[1].
SMS2-IN-1 is a highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM.
Ro 60-0175 is a potent, selective 5-HT2C receptor agonist with pKi of 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively; induces hypolocomotion in rats at doses greater than 0.5 mg/kg s.c.; (0.3 and 1 mg/kg s.c.) simultaneously reduces both unpunished and punished lever pressing, a profile consistent with sedation, induces sedative-like responses via 5-HT(2C) receptor activation in vivo.
ISIS 416858, a single-stranded antisense oligodeoxynucleotide, is a potent and selective inhibitor of FXI mRNA expression.
3,8''-Biapigenin is a biflavone in Hypericum perforatum L.[1].
2,2′-Binaphthyl-d14 is the deuterium labeled 2,2′-Binaphthyl[1].
Fmoc-Gln(Trt)-Ser(psi(Me,Me)pro)-OH is a dipeptide.
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].
CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer[1].
Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect[1].
GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17)[1].
BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain[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.
Dibromochloronitromethane is one of Halonitromethanes, which are a recently identified class of disinfection by-products (DBPs) in drinking water[1].
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].
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity[1][2].
VU6028418 (VU 6028418) is a potent, highly selective, orally bioavailable M4 mAChR antagonist for the treatment of dystonia and other movement disorders.
HBT1 is a novel potent AMPA receptor potentiator with lower agonistic effect compared with LY451395 and OXP1.
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
Muramic acid is a component in many Gram-positive bacterial cell walls, as marker for Gram-positive bacteria[1].