aaa

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor ( IC50=11 nM).

Suc-AAA-pNA is a synthetic peptide substrate commonly used for protease activity assays and widely applied in biochemical experiments.

MC-AAA-NHCH2OCH2COOH (compound 20) is a cleavable antibody-drug conjugate (ADC) linker primarily used in the synthesis of ADCs.

MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a) is a camptothecin payload used in the synthesis of a camptothecin antibody-drug conjugate (ADC) by conjugating it to a monoclonal antibody (mAb).

AAA-10 formic is an orally active inhibitor of intestinal bacterial bile salt hydrolase (BSH), with an IC50 of 10 nM against B. thetarBSH and 80 nM against B. longumrBSH.

NAAA-IN-2 (Compound 9), a potent and selective inhibitor of NAAA, exhibits an IC50 of 50 nM. NAAA, a cysteine amidase, primarily breaks down the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). This compound demonstrates promise for inflammation and pain research [1].

NAAA-IN-3 (Compound 17a) is a potent and selective NAAA inhibitor with an IC50 of 50 nM. NAAA is a cysteine amidase that preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). PEA is an endogenous agonist of the nuclear peroxisome proliferator-activated receptor-α (PPAR-α), a key regulator of inflammation and pain. The potential role of NAAA-IN-3 is as a therapeutic agent for the treatment of inflammation and pain.

NAAA-IN-1 (Compound 1) is a potent and selective NAAA inhibitor (IC50 = 7 nM) that can be used in inflammation and pain research. NAAA, a cysteine amidase, preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA) [1].

LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values ​​of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.

UPCDC30245 is an AAA ATPase p97 allosteric inhibitor.

3-methyl-1,2-dihydroquinolin-2-one is the first known micromolar inhibitors of the ATAD2 bromodomain.

MSC1094308 is a reversible, non-ATP-competitive alterative inhibitor targeting type II AAA ATPase (VCP p97) and type I AAA ATPase (VPS4B), which affects the intracellular protein degradation process by binding to a specific hotspot region of p97 and inhibiting D2 ATPase activity.

BAY-850 is a selective and potent inhibitor of adenosine triphosphatase family protein 2 (ATAD2) (IC50: 166 nM) that inhibits ovarian cancer growth and metastasis in in vitro and in vivo models.

Ciliobrevin D is a AAA+ ATPase motor cytoplasmic dynein inhibitor. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation and it also inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

Diazaborine inhibits maturation of rRNAs for the large ribosomal subunit. Diazaborine blocks ribosome biogenesis by inhibiting the AAA-ATPase Drg1. Diazaborine treatment causes, within minutes, a rapid redistribution of the protein from the nucleolus to t

Rbin-2 is a cell-permeable, potent, selective and reversible inhibitor of Midasin (Mdn1).Rbin-2 directly targets the AAA+ ATPase Midasin and inhibits eukaryotic ribosome production, making it a potent probe for the study of eukaryotic ribosome assembly processes.

PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor. This chemical compound specifically impedes the activity of PRMT5, an enzyme involved in the methylation of arginine residues on target proteins, which plays a critical role in various cellular processes.

ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization and serves as a probe molecule with low micromolar inhibitory activity.

AAA-10 is an orally active inhibitor of bile salt hydrolase (BSH) in B. intestinalis, targeting B. thetarBSH (IC50: 10 nM) and B. longumrBSH (IC50: 80 nM).

SCFSkp2-IN-2, a Skp2 inhibitor, exhibits a dissociation constant (K_D) of 28.77 μM. It demonstrates antitumor activities by inducing apoptosis in non-small cell lung cancer (NSCLC) cells.

OF-02, an alkenyl amino alcohol (AAA) ionizable lipid, demonstrates high potency for in vivo mRNA delivery.

7-Aminomethyl-10-methyl-11-fluoro camptothecin, serving as a cytotoxic component of the antibody-drug conjugate (ADC) MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin, is employed in the synthesis of camptothecin ADCs [1].

Spastazoline is a potent and selective inhibitor of spastin(Human spastin with IC50 of 99 nM ).