MrgprX2 antagonist-1 is an MrgprX2 antagonist extracted from patent WO2021092264A1, example E23. MrgprX2 antagonist-1 can be used for the research of inflammatory disorders of the skin[1].
GKT137831 is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.
N4-Methylcytidine (Nsc518744) is a cytidine nucleoside 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].
SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with Ki of 9.7 nM.
RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.
Dieckol, is a naturally occurring phlorotannin found in some brown algal species. Dieckol has anti-bacterial, anti-cancer, anti-oxidant, anti-aging, anti-diabetic, neuroprotective actions[1].
RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.
Bumadizone is a non-steroidal anti-inflammatory drug (NSAID) and can relieve pain[1].
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research[1].
Hydroxylamine-d3 (hydrochloride) is the deuterium labeled Hydroxyamine hydrochloride[1]. Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis[2].
Thalidomide-O-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology.
ML358 is a first in class, selective small molecule inhibitor of the SKN-1 pathway with IC50 of 0.24 uM; shows inactivity against Nrf2, the homologous mammalian detoxification pathway, and is not toxic to C. elegans (LC50 > 64 uM) and Fa2N-4 immortalized human hepatocytes (LC50 > 5.0 uM); sensitizes the model nematode C. elegans to oxidants and anthelmintics; exhibits good solubility, permeability, and chemical and metabolic stability in human and mouse liver microsomes; a valuable chemical probe to study regulation and function of SKN-1 in vivo.
Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples.
2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural product found in the leaves and stem bark of M. glabra. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one displays binding affinities with dipeptidyl peptidase-4 (DPP-4) and α-Amylase. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one has potential antidiabetic activities[1].
m-PEG6-C6-phosphonic acid ethyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).IC50 value: 58 pM (Ki)Target: PDE1in vitro: ITI-214 exhibits picomolar inhibitory potency for PDE1, demonstrates excellent selectivity against all other PDE families. ITI214 exhibits excellent selectivity over other PDE familymembers. For instance, the Ki values of ITI214 against recombinant full-length human PDE1A, PDE1B, and PDE1C are 33 pM, 380 pM, and 35 pM, respectively. ITI214 is profiled in a panel of enzymes, receptors, transporters, and ion channels from Caliper at 10 μM, which is over 170000 times higher than its Ki for PDE1, and demonstrates good selectivity. [1]in vivo: ITI214 possesses a good overall profile with balanced physicochemical properties, excellent potency and selectivity, and good pharmacokinetics. ITI214 is found to significantly enhance memory performance in the test with a minimum effective dose of 3 mg/kg. [1]
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively[1].
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities[1][2].
2-Chloro-N6-methyladenosine 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].
(-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent[1].
Thiodicarb is a carbamate insecticide used to control flies in animal and poultry houses and dairies. Thiodicarb is metabolized into methomyl in animals and plants, and subsequently degraded into carbon dioxide and acetonitrile[1].
Mulnitorsen is an antisense non-coding mitochondrial RNA (ASncmtRNA) synthesis reducer. Mulnitorsen is an antitumor agent[1].
Mal-PEG4-Val-Cit-PAB-OH is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
GPR34 receptor antagonist 2 (Compound D2) is a GPR34 receptor antagonist. GPR34 receptor antagonist 2 can be used for immune diseases, inflammatory diseases research[1].
Oxytocin (α-Hypophamine) acetate is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
MRS 2179 is a potent, selective, competitive P2Y1 receptor antagonist with Kb of 100 nM; displays no appreciable activity at P2Y2, P2Y4, or P2Y6 receptors (>30 uM); inhibits ADP-induced platelet shape change, aggregation and Ca2+ rise but has no effect on ADP-induced inhibition of adenylyl cyclase; decreases platelet count in mice.
36-Dioxaoctanedioic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
MmpL3-IN-2 is an MmpL3 inhibitor with low cytotoxicity and moderate metabolic stability for tuberculosis research[1].
JNJ-678 (JNJ-53718678) is a novel fusion protein inhibitor in clinical trials for the treatment of respiratory syncytial virus.
Boditrectinib is a potent tyrosine kinase inhibitor. Boditrectinib serves as an antineoplastic agent. Boditrectinib is useful in the research of cancer, inflammation, neurodegenerative diseases and certain infectious diseases[1][2].