Activators & Inhibitors

MEK4 Inhibitor-2, a novel MEK4 inhibitor, demonstrates efficacy against pancreatic adenocarcinoma, exhibiting an IC50 value of 83 nM.

GSK3494245 (DDD01305143) is a potent, selective, orally active inhibitor of chymotrypsin-like activity that binds to the proteasome of WTL.donovani at an IC50 of 0.16 μM, sandwiched between the β4 and β5 subunits. GSK3494245 exhibits good biosafety properties. GSK3494245 is a suitable inhibitor of the chymotrypsin-like activity of the human proteasome (IC50: 26S=13 μM; enriched THP-1 extract IC50=40 μM).

Mt KARI-IN-5 (compound 6c) was a potent inhibitor of Mycobacterium tuberculosis ketohydrin reductase I (MtbKARI) (Ki: 4.72 μM). Mt KARI-IN-5 exhibited inhibition of MtbH37Rv activity with a MIC value of 1.56 μM, low cytotoxicity and an IC50 value for HEK The IC50 value for HEK was greater than 64 μg/mL.

FPPQ is a dual antagonist of the 5-HT3 and 5-HT6 receptors with Ki values of 0.9 nM and 3 nM, respectively, and exhibits antipsychotic and pro-cognitive activity.

Camonsertib (RP-3500) is a selective, orally active ATR kinase inhibitor (ATRi) with an IC50: 1.00 nM in biochemical assays and exhibits potent antitumour effects. Camonsertib is 30 times more selective for ATR than mTOR (IC50: 120 nM) and is a more active inhibitor of ATM, DNA-PK and PI3Kα kinases. PK and PI3Kα kinases.

ATR-IN-8 is a potent inhibitor of ATR. ATR-IN-8 has shown potential research value in cancer diseases.

Enpp-1-IN-5 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). enpp 1 shows broad specificity and is able to cleave a wide range of substrates (including phosphodiester bonds of nucleotides and nucleotides, and pyrophosphate bonds of nucleotides and nucleotides). Enpp-1-IN-5 has potential for cancer and infectious disease research.

Tuberculosis inhibitor 5 (Compound 11i) is a potent anti-tuberculosis agent with no apparent cytotoxicity. tuberculosis inhibitor 5 is an antimycobacterial biphenyl analogue.

Tuberculosis inhibitor 4 (compound 16) is a spirothiazolidinone based on mandelic acid that exhibits potent antimycobacterial action. The inhibitor inhibited 98% of Mycobacterium tuberculosis strain H37Rv at concentrations below 6 μg mL.