Activators & Inhibitors

(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.

LDN-209929 dihydrochloride is a potent and selective inhibitor of haspin kinase (IC50= 55 nM). LDN-209929 dihydrochloride shows180-fold selectivity verses DYRK2 (IC50= 9.9 μM).

Antiproliferative agent-8 (Compound 5a) is an anti-cancer compoundwith antiproliferative activity. Antiproliferative agent-8 can significantly increase the P53 levels.