Activators & Inhibitors

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.

CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator (EC 50= 100 nM). CXCR4 modulator-1 has research value in anti-inflammatory, anticancer and anti-HIV.

Mazaticol is an anticholinergic agent, which blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol potently inhibits 3H-QNB and 3H-PZ binding. Mazaticol can bind to the M2 receptors with high affinity. Mazaticol shows inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol has research in parkinsonian syndrome.

EGFR-IN-71 is a potent inhibitor of epidermal growth factor receptor (EGFR) (IC50= 3.7 μM). EGFR-IN-71 has research value in chordoma.

HIV-1 inhibitor-20 is a potent HIV-1 inhibitor.