Activators & Inhibitors

GABA-AT-IN-1 (Compound 6) is an inhibitor of γ-aminobutyric acid transaminase (GABA-AT) that crosses the blood-brain barrier.

ART615 is a related isomer of ART558. ART615 inhibits Polθ by <10% at 12 μM and is able to act as a control for ART558 (IC50:7.9 nM).

CSF1R-IN-6 is a potent inhibitor of CSF1R. CSF1R-IN-6 is a potent inhibitor of CSF1R, which is expressed in macrophages and is dependent on the CSF-1/CSF-1R signalling pathway for survival and differentiation of macrophages. Compound 5).

PIM1-IN-6 (compound 5h) is a potent inhibitor of PIM-1 (IC50: 0.60 μM).PIM1-IN-6 has a high cytotoxic effect on HCT-116 and MCF-7 cells with IC50 values of 1.51 and 15.2 μM, respectively.

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).