r18

Antagonist of 14.3.3 proteins (KD ≈80 nM). Competitively inhibits 14.3.3-ligand interactions without requiring phosphorylation. Blocks the ability of 14.3.3 to bind to target proteins such as Raf-1, Bad, ASK1 and exoenzyme S.

R18 TFA, a peptide antagonist of 14-3-3, exhibits a dissociation constant (K_D) of 70-90 nM. It efficiently inhibits the interaction between 14-3-3 and its physiological ligand, the kinase Raf-1, thereby significantly impeding the protective effect of 14-3-3 on Raf-1 against phosphatase-induced deactivation [1].

SSR180711 hydrochloride (SSR-180711A HCl) is a selective Alpha7 nicotinic acetylcholine partial agonist for the study of neurodegenerative and cognitive disorders.

FR183998 free base is an inhibitor of Na+/Ca2+ Exchanger.

SMER18 is a small molecule enhancer of rapamycin, functioning as an mTOR-independent autophagy inducer.

GPR183 antagonist-3 (compound 33) is an orally active GPR183 antagonist with an IC50 value of 8.7 μM. It demonstrates significant in vitro anti-migration and anti-inflammatory activity in monocytes and can alleviate pathological symptoms in experimental colitis induced by dextran sulfate sodium.

GPR183 inverse agonist-1 (Compound 78) is an inverse agonist of GPR183. It inhibits GPR183-mediated Gi activation and β-arrestin2 recruitment while blocking PBMC migration. This compound is utilized in research concerning inflammation, autoimmune, and cancer-related diseases.

SR18662, an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM, reduces the viability of multiple colorectal cancer cell lines and induces apoptosis.

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

Zoldonrasib (RMC-9805) is a mutant-selective covalent KRAS G12D inhibitor with oral activity and significant antitumor activity, inducing tumor cell apoptosis in preclinical models of various KRAS-mutant cancers.

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.OR-1896 can be used to study heart failure and vascular dysfunction. OR-1896 can be used to study heart failure and vascular dysfunction.

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.

Niguldipine Free Base is a calcium channel blocker and antagonist with an IC₅₀=0.9 μM for Cav 3.2, suitable for cardiovascular system research.

SSR 180 is a potent and subtype-selective α7 agonist with applications in the study of Alzheimer;s disease and schizophrenia.

Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.

Miconazole (R18134) is an imidazole antifungal agent used both topically and via intravenous infusion.

Miconazole nitrate (R18134 nitrate), an imidazole antifungal agent, selectively affects the integrity of fungal cell membranes, high in ergosterol content and different in composition from mammalian cells membranes.

Tetraethylene glycol is a PEG-based PROTAC linker that can be oxidised as a substrate of polyethylene glycol dehydrogenase (Km = 10 mM).

Levosimendan (OR1259) is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner.

GSK682753A is a selective and highly potent inverse agonist of the Epstein-Barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

Loperamide-D6 hydrochloride, a deuterium-labeled variant of Loperamide hydrochloride (T0209), acts as an opioid receptor agonist utilized for diarrhea treatment.

Migalastat hydrochloride (GR181413A) is an orally available, potent and competitive inhibitor of alpha-galactosidase A. It promotes the transport of alpha-galactosidase A to the lysosome and can be used in the study of Fabry disease.

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

OR-1855 is an active Levosimendan metabolite, has effect on human myometrial contractility.