2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
Boc-L-Tyr(PEG(3)-N3)-OH is a click chemistry agent containing azide.
Piketoprofen is a non-steroidal anti-inflammatory reagent that can be used as a cream preparation for the study of soft tissue rheumatism[1].
Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.IC50 value: Target: microtubuleTubulysin A is a novel antibiotic, which is anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative. Tubulysins are cytotoxic peptides, which include 9 members (A-I). Tubulysin A has potential application as an anticancer agent. It arrests cells in the G2/M phase. Tubulysin A inhibits polymerization more efficiently than vinblastine and induces depolymerization of isolated microtubules. Tubulysin A has potent cytostatic effects on various tumor cell lines with IC50 in the picomolar range.
TC11 is a MCL1 degradator and Caspase-9 and CDK1 activator. TC11 structurally relates to immunomodulatory drugs as phenylphthalimide derivative. TC11 induces apoptotic death caused by degradation of MCL1 during prolonged mitotic arrest[1][2].
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research[2].
Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
SARS-CoV-2 nsp13-IN-5 (compound C6) is a potent SARS-CoV-2 nsp13 inhibitor with IC50 values of 50 and 55 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-5 can be used for researching anti-COVID-19[1].
THR-β agonist 5 (compound 54) is a potent THR-β agonist, with an EC50 of <50 nM[1].
LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC50s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively[1].
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3].
5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) can be isolated from Dendrobium infundibulum (D. infundibulum). 5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl has no inhibitory activity against α-glucosidase and pancreatic lipase[1].
EUK-118 is an analog of EUK 8 and EUK 134 with reduced activity. EUK-118 exhibits superoxide dismutase (SOD) mimetic activity[1][2].
EB1 peptide (Penetrating analog), a Penetratin peptide derivative, is an amphipathic cell-penetrating peptide (CPP). EB1 peptide has the potential for intracellular drug delivery research[1].
Hygric acid (N-Methyl-L-proline) is a proline analogue found in the citrus juices and the juice of bergamot[1].
SW 71425 inhibits cell growth against breast, colon, non-small cell lung, and ovarian tumors.[1].
Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects[1].
Acipimox (K-9321) sodium, a nicotinic acid analogue, is an antilipolytic compound. Acipimox sodium stimulates leptin releas, inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity[1][2][3].
Trans-Trimethoxyresveratrol is a derivative of Resveratrol (RSV),and it may be a more potent anti-inflammatory, antiangiogenic and vascular-disrupting agent when compared with resveratrol.In vitro: The in vitro study of resveratrol and trans-Trimethoxyresveratrol showed rather weak cytotoxic effects on three cancer cell lines (HepG2, MCF-7, and MDA-MB-231), which contradicted a previous study reporting that resveratrol inhibited MCF-7 cells with an IC50 of about 10?μM. This discrepancy might be explained by the fact that the measurements were made 24?h after drug treatment, whereas the measurements of the previous study were taken 6 days after. The fact that the cytotoxic effect of trans-Trimethoxyresveratrol was lower than that of resveratrol is surprising, because in many studies, trans-Trimethoxyresveratrol is the most active analogue of resveratrol , although resveratrol shows much stronger antioxidant effects than that of trans-Trimethoxyresveratrol.[1]In vivo: Zebrafish embryos offer great advantage over their adults as well as other in vivo models because of the external development and optical transparency during their first few days, making them invaluable in the inspection of developmental processes. These unique advantages can even be made more useful when specific cell types are labeled with fluorescent probes. Zebrafish embryo in vivo, suggests that trans-Trimethoxyresveratrol has both more potent antiangiogenic activity and more importantly, stronger specific cytotoxic effects on endothelial cells than does resveratrol.[1]
WAY-301398 is an active molecule for the study of amyloid diseases and synucleinopathies.
RBC6 is an inhibitor of GTPases RalA. RBC6 inhibits binding of Ral to its effector RALBP1. RBC6 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts, as well as anchorage-independent growth of human cancer celllines[1].
Azido-PEG3-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG3-maleimide is also a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Methyl-PEG2-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research[1].
Nezukone is a derivative of hinokitiol. Hinokitiol can restore iron transports, however, Nezukone cannot bind or transport iron.
BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity[1].
(-)-Conocarpan is a natural compound that can be isolated from various species of Krarneria[1].
Cionin is a disulfotyrosyl hybrid of cholecystokinin and gastrin[1].
STING agonist-8 is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells (WO2021239068A1, compound 5-AB)[1].
H-Glu(OMe)-OH hydrochloride is a protonated glutamic acid derivative[1].