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).

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 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).

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.

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.

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.

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

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.

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.

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

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.

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 ).

7-Aminomethyl-10-methyl-11-fluoro camptothecin TFA, a cytotoxin variant of MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin, is employed in the synthesis of camptothecin antibody-drug conjugates (ADC) [1].