RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites.
Raltitrexed is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. Raltitrexed is used as an antimetabolite drug used in the treatment of colorectal cancer, and may be beneficial for malignant mesothelioma treatment.
Raltegravir is a potent, selective, and orally bioavailable inhibitor of HIV integrase (IC50 = 15 nM). It is metabolized primarily by uridine diphosphate glucuronosyltransferase 1A. Raltegravir has long-term efficacy and safety in managing HIV-1 infection in adults, children, and adolescents.
Rafigrelide is a platelet aggregation inhibitor, which plays a central role in atherothrombotic events. It could prolonge clot formation time and reduce clot strength.
Radotinib, also known as IY-5511, is an orally available, hydrochloride salt form of radotinib, a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib. PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. Check for active clinical trials or closed clinical trials using this agent.
Radiprodil is an orally active and selective NMDA NR2B antagonist as a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions, blocking pain signaling without interacting with other NMDA receptor subtypes thus potentially improving therapeutic index and side effect profile.
An impurity of Vildagliptin. Vildagliptin is a new dipeptidyl peptidase-4 (DPP-4) inhibitor that is used as an anti-hyperglycemic agent. Vildagliptin could reduce hyperglycemia in type 2 diabetes mellitus via the suppressive effect of inactivation of GLP-1 and GIP by DPP-4.
Rac-cis-Sertraline Hydrochloride is an extensively utilized pharmacological compound within the biomedical sector used in studying psychiatric afflictions, including depression, panic disorder and obsessive-compulsive disorder. Its mechanism of action entails selective inhibition of serotonin reuptake, thereby reestablishing homeostasis of this pivotal neurotransmitter within the cerebral research.
Rac (8-Hydroxyquinolin-3-yl)alanine Dihydrochloride is used in the genetic incorporation of a metal-ion chelating amino acid into proteins as a biophysical probe.
R788 sodium salt hydrate, a methylene phosphate prodrug of the active metabolite R406, is a potent Syk inhibitor. It can be rapidly converted to R406 in vivo. It effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals.
R162 is a potent, selective inhibitor of glutamate dehydrogenase 1 (GDH1) (Ki = 28.6 µM), with anti-cancer properties. It does not inhibit the activity of other NADPH enzymes such as 6-phosphogluconate dehydrogenase and fumarate hydratase.
This active molecular also known as AC220 and AC010220, is developed as a new second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, ten fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Now Quizartinib is in Phase-III clinical trials in Acute myeloid leukaemia.
Quinine Hydrochloride Dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste. It is a stereoisomer of quinidine, which, unlike quinine, is an antiarrhythmic. Quinine contains two major fused-ring systems: the aromatic quinoline and the bicyclic quinuclidine.
A metabolite of Quetiapine. Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.
An impurity of Quetiapine. Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.
Quercetin-3-O-D-glucosyl]-(1-2)-L-rhamnoside is a remarkable natural compound renowned in the biomedical research.Its perfect value lies in the fact that it has been effectively studied for a wide range of diseases with its powerful antioxidant, anti-inflammatory, anti-tumor and neuroprotective potential.
Quaternium-73 has excellent antistatic, bactericidal, antibacterial, antiseptic, emulsifying, dispersing, solubilizing, and corrosion-inhibiting properties. It is a powerful bactericidal acne-removing agent, especially for closed acne. It is a safe long-term fungicide that kills bacteria and various fungi at lower concentrations (2 parts per 100,000) and improves acne, pimples, and polyacne symptoms. Quaternium 73 is an antibacterial agent used as a preservative in cosmetics.
Quarfloxin, also known as Quarfloxacin and CX-3543, is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells. Disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.
Q203, also known as IAP6, was active against the reference strain M. tuberculosis H37Rv at a minimum concentration required to inhibit the growth of 50% of organisms (MIC50) of 2.7 nM in culture broth medium and at a MIC50 of 0.28 nM inside macrophages.
PZM-21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM. PZM21 is an experimental opioid analgesic that is being studied for the treatment of pain.
Pyrvinium pamoate, a nonabsorbed anthelmintic drug, is a potent androgen receptor inhibitor and a selective WNT pathway inhibitor. Pyrvinium pamoate is a potential drug candidate for the treatment of cryptosporidiosis in both immunocompetent and immunocompromised individuals.
Pyrrolidinyl diaminopyrimidine oxide is structurally similar to minoxidil and is an innovative and clinically proven 100% water soluble alcohol-free hair growth promoter. Pyrrolidinyl diaminopyrimidine oxide improves the skin surface blood circulation, to the hair roots to provide the required nutrients and oxygen, to achieve the effect of inhibiting hair loss, strengthening the hair roots, and promoting hair growth. By opening potassium ion channels, it can transform hair follicles from resting period to growth period and prolong the growth period of hair.
Pyrotinib, also known as SHR-1258, is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. Upon oral administration, pyrotinib binds to and inhibits both EGFR and HER2, which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumor cells.
Pyronaridine tetraphosphate is an antimalarial agent with an inhibitory effect on P-glycoprotein mediated drug resistance. It inhibits B-hematin formation and Ebola virus (EBOV).
Pyronaridine is an antimalarial drug. Pyronaridine was first synthesized in 1970 and has been in clinical use in China since the 1980s. It is one of the components of the artemisinin combination therapy pyronaridine artesunate (Pyramax).
Pyromellitic diimide is a high-temperature, thermally stable, and photostable intramolecular hydrogen acceptor that has been used in the synthesis of a variety of organic compounds.
PXS 4728A is a VAP-1 (aka SSAO/AOC3) inhibitor with IC50 values 5 nM in the clinical trial for the treatment of non-alcoholic steatohepatitis (NASH). Studies show that it inhibits neutrophil rolling and tethering in mouse cremaster model, and alleviates respiratory inflammation in multiple models.
PX-478 is an HIF-1alpha inhibitor and an orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha inhibitor PX-478 appears to inhibit hypoxia-inducible factor 1-alpha (HIF1A) expression, which may result in decreased expression of HIF1A downstream target genes important to tumor growth and survival, a reduction in tumor cell proliferation, and the induction of tumor cell apoptosis. The inhibitory effect of this agent is independent of the tumor suppressor genes VHL and p53 and may be related to derangements in glucose uptake and metabolism due to inhibition of glucose transporter-1 (Glut-1). PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity. It is rapidly absorbed following oral and i.p. administration and gives excellent Cmax and AUC via these routes.
Purvalanol B is a potent, selective, reversible and ATP-competitive inhibitor of CDK with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1 and CDK5-p35, respectively.
