aaa

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).

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

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)

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.

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.

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

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.

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

RUVBL1/2 ATPase-IN-1 is an effective RUVBL1/2 ATPase inhibitor with IC50 values of 6.0 and 7.7 μM, respectively. RUVBL1/2 ATPase-IN-1 can be used in cancer disease studies.

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].

ARN 077 is a selective N-acylethanolamine acid amidase (NAAA) inhibitor (IC50: 7 nM for human NAAA). ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS.

Oseltamivir phosphate (GS 4104) is a neuraminidase (NA) inhibitor with oral activity. Oseltamivir phosphate has antiviral activity and is effective against a wide range of influenza viruses, inhibiting mature influenza viruses from breaking away from host cells.

Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2/3.7/4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM).

2′-Deoxy-2′-fluoroguanosine is a nucleoside analog that potently inhibits influenza virus A and B strains(EC90 <0.35 μM). 2'-Deoxy-2'-fluoroguanosine is an inhibitor of influenza virus replication in the upper respiratory tract, improving fever and nasal inflammation.

5-Ph-IAA-AM, an eggshell-permeable analog of 5-Ph-IAA, enhances protein degradation in laid embryos and can be used to reveal the roles of temporally controlled protein degradation in C. elegans embryogenesis and development [1].

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].

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.

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.

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.