| Name | Crisaborole |
| Description | Crisaborole (AN-2728) is a phosphodiesterase 4 inhibitor. |
| In vitro | AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. AN-2728 inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD. |
| In vivo | AN-2728 is well tolerated and significantly impacts efficacy markers, showing comparable results to positive controls in clinical trials. It effectively inhibits ear edema induced by phorbol ester with a dosing of 1 mg/ear×2 (78% and 68%, respectively), mirroring the efficacy of dexamethasone. This suggests AN-2728 possesses notable anti-inflammatory properties and skin penetration capabilities. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7.97 mM), Sonication is recommended.
DMSO : 250 mg/mL (995.82 mM), Sonication is recommended.
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| Keywords | Phosphodiesterase (PDE) | phosphodiesterase | PF06930164 | PF 06930164 | PDE4 | Inhibitor | inhibit | Crisaborole | AN2728 | AN 2728 |
| Inhibitors Related | Balipodect | Theophylline monohydrate | D(+)-Raffinose pentahydrate | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Drug-Fragment Library | Inhibitor Library | NO PAINS Compound Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Metabolism Disease Compound Library |
United States
