Activators & Inhibitors

sRANKL-IN-1 (compound S3) is an inhibitor of sRANKL (soluble RANKL). sRANKL-IN-1 is a strong inhibitor of osteoclasts (IC50: 0.096 μM, Kd: 34.80 μM). sRANKL-IN-1 can be used in the study of osteoporosis.

CSF1R-IN-7 (Formula I) is a CSF-1R inhibitor that can be used to study Alzheimer's disease.

DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits the activity of DNA-PKcs, significantly reduces tumour DNA repair and induces apoptosis. DNA-PK-IN-5 improves the sensitivity of tumour tissue to radiotherapy, overcomes drug resistance problems and improves the inhibition of many solid and haematological tumours (Information (Information from patent WO2021204111A1, compound 2).

CDK4/6-IN-9 (compound 10) is a selective inhibitor of CDK4/6, capable of acting on CDK6/cyclin D1 (IC50: 905 nM). CDK4/6-IN-9 has potential research value in multiple myeloma (MM).

PD-1/PD-L1-IN 5 is a potent PD-1/PD-L1 protein/protein interaction inhibitor (IC50 ≤ 100 nM) (from patent WO2017222976A1, compound example 1).

MEIS-IN-3 is a potent inhibitor of MEIS.

Analgesic agent-1 is a potent analgesic that exhibits significant analgesic activity.

CEP-9722 is a prodrug of CEP-8983, a selective, orally active inhibitor of PARP-1 (IC50: 20 nM) and PARP-2 (IC50: 6 nM).CEP-9722 exhibits anticancer activity.

Influenza virus-IN-4 (compound 11e) is a potent inhibitor of influenza virus neuraminidase, acting on H5N1 (IC50: 3.4 μM), H5N2 (IC50: 0.094 μM), H5N6 (IC50: 0.79 μM) and H5N8 (IC50: 0.077 μM). Influenza virus-IN-4 inhibits NA (neuraminidase) and has low cytotoxicity (CC50 > 200 μM). influenza virus-IN-4 is not significantly toxic to mice at 1500 mg/kg.