Activators & Inhibitors

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.

(Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective antagonist of β1-adrenergic receptor (IC 50= 0.8 nM). Nebivolol shows Vasodilatory activity. In the early stages of ethanol-induced cardiac toxicity, Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation.

Imidapril (TA-6366 free base) is an orally active inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril inhibits the conversion of angiotensin I to angiotensin II, thereby reduces total peripheral resistance and systemic blood pressure. Imidapril has research value in hypertension, type 1 diabetic, nephropathy and chronic heart failure.

HDAC-IN-30 is a multi-target HDAC inhibitor. HDAC-IN-30 inhibits HDAC1 (IC50 =13.4 nM), HDAC2 (IC50 =28.0 nM), HDAC3 (IC50 =9.18 nM), HDAC6 (IC50 =42.7 nM), HDAC8 (IC50 =131 nM). HDAC-IN-30 shows potent antitumor efficacy.