BTA-EG4 is a catalase-amyloid interaction inhibitor, which can significantly enhance the neurotoxicity of amyloid peptides in catalase-overexpressing neuronal cells, and can be used in the study of neurodegenerative diseases[1].
Ac-Gly-Lys-OMe is a substrate for urokinase. Ac-Gly-Lys-OMe can be used to measure the effects of small molecule inhibitors on urokinase activity[1].
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile[1].
A dual inhibitor of TNF-α and TGF-β1 by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation; attenuates the LPS/GaIN-induced hepatic inflammation in the mice, and downregulates TGF-β1-induced fibrotic gene expression; attenuates renal inflammation and fibrosis with the downregulation of inflammatory cytokines and fibrotic gene expressions in renal fibrosis model.
Bromo-PEG2-acetic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
XmAb 5592 is a humanized, Fc-engineered anti-HM1.24 antibody with enhanced binding to FcγRIIIa and FcγRIIa receptors, augments HM1.24-specific multiple myeloma (MM) cells lysis in vitro via antibody-dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP)[1].
Phosphatase Binder-1 (comppund i-196) provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Phosphatase Binder-1 plays an important role in cancer[1].
5-Methyl-5,6-dihydrouridine is a minor constituent in the chromosomal RNA of the rat ascites tumor. 5-Methyl-5,6-dihydrouridine can be used for nucleic acid modification[1].
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader (WO2020163823A2, compound 44)[1].
Furazolidone-d4 is deuterium labeled Furazolidone.
CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC50 of 2.9 μM. CDK2-IN-15 can be used for cancer research[1].
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
(4-Hydroxy-1,1-dioxidotetrahydrothiophen-3-yl)glycine is a Glycine (HY-Y0966) derivative[1].
Pravastatin is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.Target: HMG-CoA reductasePravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used in combination with diet, exercise, and weight-loss for lowering cholesterol and preventing cardiovascular disease.Pravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.The evidence for the use of pravastatin is generally weaker than for other statins. The antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT), failed to demonstrate a difference in all-cause mortality or nonfatal myocardial infarction/fatal coronary heart disease rates between patients receiving pravastatin 40mg daily (a common starting dose) and those receiving usual care.
Amicarbazone(BAY-MKH3586; BAY314666) is a potent inhibitor of photosynthetic electron transport via binding to the Qb domain of photosystem II (PSII); herbicide with a broad spectrum of weed control.IC50 value:Target: PSII inhibitorThe phenotypic responses of sensitive plants exposed to amicarbazone include chlorosis, stunted growth, tissue necrosis, and death. Its efficacy as both a foliar- and root-applied herbicide suggests that absorption and translocation of this compound is very rapid. As a result, its efficacy is susceptible to the most common form of resistance to PSII inhibitors. Nonetheless, amicarbazone has a good selectivity profile and is a more potent herbicide than atrazine, which enables its use at lower rates than those of traditional photosynthetic inhibitors.
C-021 dihydrochloride is a potent and orally bioavailable CCR4 antagonist with IC50 of 0.14 uM and 0.039 uM for inhibition of chemotaxis in human and mouse, respectively.
OSU-03012 is a PDK-1 inhibitor with an IC50 of 5 μM.
[(tert-butoxycarbonyl)amino](3-chlorophenyl)acetic acid is a Glycine (HY-Y0966) derivative[1].
FAS-IN-1 is a potent inhibitor of Fatty acid synthase (FAS) wtih IC50 of 10 nM, extracted from Patnet WO2012/064642Al.
Lucigenin(L-6868; NSC-151912) is a chemiluminescent probe used to indicate the presence of endogenously generated superoxide anion radicals in cells.Upon single-electron reduction of Lucigenin by a radical species the subsequent form of Lucigenin presents an amplified chemiluminescence which is measurable and can be correlated to the respective amount of reactive radical species present in the system. This approach can be used to probe the natural generation of these species as well as the natural functioning of superoxide dismutase and other enzymes responsible for scavenging radicals. In addition to indicating the presence of radicals in cells, Lucigenin shows interaction with redox-active oxidoreductase enzymes. Lucigenin is shown to mediate the reduction of cytochrome C by xanthine oxidase and to increase the rate of NADPH oxidation. These observations indicate that use of Lucigenin for superoxide analysis is precluded in the presence of high levels of NAD(P)H-oxidoreductases.
N-Boc-N-bis(PEG4-azide) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
l-Naproxen ((R)-Naproxen) is an enantiomer of (S)-Naproxen. l-Naproxen can inhibit Cdc42 and Rac1 (EC50=96 μM and 212 μM, respectively), and show anti-tumor activity[1][2][3].
Soyasaponin Ac is a triterpenoid isolated from the seeds of Glycine max.
PF-6274484 is an inhibitor of the EGF receptor (EGFR; IC50s = 0.18 and 0.14 nM for wild-type EGFR and inhibitor-resistant EGFRL858R/T790M, respectively).
Hexachloroparaxylene could be used in the study of in fascioliasis in swine[1].
Pentacosane is one of the major components in the acetone extract from Curcuma raktakanda and is also in the essential oil from the leaves of Malus domestica. Pentacosane exhibit anti-cancer activities[1].
Lagotisoide D is a lridoid glycoside from Lagotis yunnanensis[1].
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.