Activators & Inhibitors

AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor. AChE/BChE-IN-8 shows Ki of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 has blood-brain barrier permeability and low cytotoxicity.

Y-29794 (Compound 2) is a potent, covalent inhibitor of prolyl oligopeptidase (POP) (Ki= 0.95 nM). Y-29794 has research value in neurodegenerative diseases and cancer.

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound. Antiproliferative agent-6 shows antiproliferative activity. Antiproliferative agent-6 inhibits cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI 50 s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively.

UGM-IN-3 (compound 10a) is a inhibitor of UDP-galactopyranose mutase (UGM) with a Kd of 66 μM. UGM-IN-3 inhibits the growth of Mycobacterium tuberculosis (MIC= 6.2 μg/mL).

Quinidine is a potent, orally active, selective inhibitor of cytochrome P450db. Quinidine hydrobromide is a K + channel blocker (IC 50= 19.9 μM). Quinidine hydrobromide shows antiarrhythmic activity. Quinidine hydrobromide can be used for malaria research.

ABBV-318 can be used as small molecule Nav1.7/Nav1.8 blockers for the treatment of pain, with IC50 values of 2.8 μM for hNav1.7 and 3.8 μM for hNav1.8. ABBV-318 can be used to study pain-related disorders.

Pim-1 kinase inhibitor 2 (Compound 13), a potent inhibitor of Pim-1 kinase, has the potential for cancer research due to its ability to induce apoptosis [1].

Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants.

SOS1-IN-13 is a potent inhibitor of son of sevenless homolog 1 (SOS1). SOS1-IN-13 shows IC 50 s of 6.5 nM and 327 nM for SOS1 and pERK, respectively. SOS1-IN-13 has research value in anticancer.