Activators & Inhibitors

MAT2A-IN-6 is a potent inhibitor of MAT2A. MAT2A-IN-6 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-6 has shown potential research value in cancer diseases.

hCAXII-IN-2 (compound 5i) is a potent inhibitor of human carbonic anhydrase XII (hCA XII) (Ki: 84.2 nM) and hCA IX (Ki: 268.5 nM), with low activity against hCA I and hCA II.

Elimusertib (BAY 1895344) hydrochloride is a potent, selective, orally active ATR inhibitor (IC50: 7 nM) that exhibits antitumour effects. elimusertib hydrochloride can be used to study solid tumours and lymphomas.

COX-2/PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K (IC50: 1.14 nM). COX-2/PI3K-IN-1 is a selective inhibitor of COX-2 (Ki: 3.24 nM).

NS2B/NS3-IN-5 (Compound 25b) is a variant of the DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.67 μM and 4.38 μM for the NS2B/NS3 protease of ZIKV and DENV2, respectively.

NT219 is a dual inhibitor of insulin receptor substrate 1/2 (IRS1/2) and STAT3, enhances the aggregation of misfolded prion protein NT219 affects the levels of certain molecular chaperones and inhibits STAT3 phosphorylation NT219 is useful for the study of cancer and neurodegenerative diseases.

(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP overactivates ERα+-dependent anticipatory unfolded protein responses and exhibits anti-estrogen receptor alpha-positive breast cancer, including its resistant tumours.

E-3620 is a potent antagonist of the 5-HT3 receptor and can be used to study dyskinesia and gastrointestinal dysfunction.

ErSO-DFP is an expected activator of the unfolded protein response (a-UPR). erSO-DFP improves selectivity for oestrogen receptor alpha+ (ERα+) cancer cells with higher selectivity than ErSO. erSO-DFP has anti-tumour effects and significantly eliminates MCF-7 tumours in a mouse model.