Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.
Condurango glycoside E is a glycoside compound that can be isolated from the bark extract of Marsdenia cundurango[1].
NK007 is a novel anti-SARS-CoV-2 agent with an EC50 value of 30 nM.
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease[1].
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1][2].
p97-IN-1 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07)[1].
(R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.
Valspodar is a P-glycoprotein (P-gp) inhibitor widely used as overcoming multidrug resistance modulator.
Dabigatran etexilate mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1
Tyrosinase-IN-5 (compound 16c) is a potent inhibitor of tyrosinase with an IC50 of 0.02 μM. Tyrosinase-IN-5 efficiently suppresses the melanogenesis without significant toxicity on cells[1].
Caesalmin E is a natural cassane furanoditerpene with anti-Para3 (Parainfluenza virus type 3) virus activities[1].
Odoratone (Dehydroodoratol) has insecticidal activity (LC50: 154 ppm)[1].
CG-806 is a pan FLT3/BTK Multi-Kinase inhibitor.
TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.
Dimethylurea/citric acid is a highly efficient deep eutectic solvent (DES). Dimethylurea/citric acid can be used as a catalyst and a green reaction medium for the synthesis of bis(indolyl)methanes, quinolines and aryl-4, 5-diphenyl-1H-imidazoles.
UNC-1062 is a potent and selective Mer kinase inhibitor with IC50 of 1.1 nM, Ki of 0.33 nM; shows improved selectivity and activity against Mer relative to other TAM family RTKs (78-fold selectivity over Axl and 36-fold over Tyro3); inhibits Mer auto-phosphorylation in human pre-B leukemia 697 cells with IC50 of 6.4 nM, also inhibits colony formation in soft agar in tumor cells.
Medronic Acid (Methylenediphosphonic acid) is a methylene-substituted bisphosphonate. Medronic acid has affinity for and adheres to the surface of hydroxyapatite crystals in the bone matrix. This agent accumulates at sites of osteoid mineralization and can be used, complexed with radioisotopes in bone imaging.
Rafoxanide 13C6 is a labeled Rafoxanide (HY-17598). Rafoxanide is a salicylanilide used as an antiparasitic agent[1].
Hellebrigenol is a metabolite of bufadienolides with antitumor activity[1].
IR5790 is a herbicide. IR5790 strongly inhibits protoporphyrinogen oxidase with an IC50 of 3 nM[1].
CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
Antibacterial agent 159 (Compound 6d) is an antibiotic. Antibacterial agent 159 can effective against impetigo and C. difficile infection (CDI). Antibacterial agent 159 has no observed recurrence for C. difficile and exertes a minimal impact on the beneficial gut microbiome[1].
AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases[1].
Biotin-PEG8-Me-Tet is a biotin labeling.
Stachyose is a prebiotic, a non-reducing tetrasaccharide in the rafnose family of oligosaccharides with few side efects.
11β-HSD1-IN-7 (compound c10a) is a 11β‑HSD1 inhibitor with an IC50 value of 1.9 μM for human 11β‑HSD1. 11β-HSD1-IN-7 can be used for the research of diabetes and cognitive decline[1].
10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM[1][2].
Sibiricose A5 is an oligosaccharide ester isolated from Polygalae Radix with potent antioxidant activity[1][2].
Coprine is a mycotoxin isolated from Coprinopsis atramentaria. Coprine is an acetaldehyde dehydrogenase inhibitor that causes the buildup of acetaldehyde, causing the alcohol flushing reaction[1].