Activators & Inhibitors

PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50= 2 nM). In hepatocellular carcinoma models, PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis.

(R,R)-BAY-Y 3118, the R-enantiomer of BAY-Y 3118, exhibits weak bactericidal activity.

PqsR/LasR-IN-1 (Compound 2a) is a potent inhibitor of LasR and PqsR systems in P. aeruginosa. PqsR/LasR-IN-1 is also a inhibitor of hERG (IC50= 6.77 μM).

CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor). Adenosine receptor inhibitor 2 exhibits dual affinity toward A 1 /A 2A ARs with higher affinity for the A 1 - than the A 2A AR. Adenosine receptor inhibitor 2 exhibits Ki values of 52.2 nM for the A 1 AR and 167 nM for the A 2A AR.

Sheng Gelieting (CGT-8012) is a inhibitor of dipeptidy peptidase-IV enzyme (DP-IV) with an IC 50 value of 87 nM. Sheng Gelieting can be used for researching to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete.

Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D (IC50= 14.3 nM). Pelecopan can prevent both intravascular and extravascular hemolysis in PNH.

TrxR-IN-2 is a potential thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 has research value in the chemotherapy of drug-resistant hepatocellular carcinoma.

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK). SKI-I shows an IC 50 of 1.2 μM for ST-hSK. SKI-I is also a hERK2 inhibitor( IC 50 =11 μM). SKI-I induces apoptosis in tumor cell lines.