Activators & Inhibitors

PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor that exhibits anticancer effects without toxicity to normal cells. PI3Kα-IN-6 increases ROS production, decreases mitochondrial membrane potential and induces apoptosis.

MYF-03-176 is an orally active anticancer agent. MYF-03-176 exhibits strong antitumour effects in the MPM mouse xenograft tumour model following oral administration.

HSV-1/HSV-2-IN-1 is an HSV-1 and HSV-2 inhibitor that acts against HSV-1 (KOS) (EC50: 7.6 μM), HSV-2 (G) (EC50: 7.6 μM), HSV-1 TK-KOS ACVr (EC50: 4 μM) and cowpox virus (EC50: 12 μM).

LPM4870108 is a potent, orally active pan-Trk (WT/MT) inhibitor that acts on TrkC (IC50: 0.2 nM), TrkA (IC50: 2.4 nM), TrkAG595R (IC50: 3.5 nM) and TrkAG667C (IC50: 2.3 nM), and is more selective for Trk than ALK (IC50: 2.3 nM). LPM4870108 showed anti-tumour effects.

VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP/TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP/TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer.

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide production (IC50: 3.15 μM) and shows anti-inflammatory effects.

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.