CID 2011756
CID-2011756 (CAS 638156-11-3) is a novel and potent inhibitor of protein kinase D1 (PKD1), one of three PKD isoforms of a novel family of serine/threonine kinases involved in cell proliferation, survival, invasion, and protein transport, with a value of 50% inhibition concentration IC50 of 3.2 in vitro. CID-2011756 also exhibits pan-PKD inhibitory effects that ATP-competitively inhibit PKD2 and PDK3 with values of IC50 of 0.6 μM and 0.7 μM, respectively. Study results have shown that CID-2011756 is a cell-active PKD1 inhibitor that concentration-dependently inhibits phorbolester-induced endogenous PKD1 activation in LNCap prostate cancer cells with a value of half maximal effective concentration EC50 of 10 μM.
References:
[1] Sharlow ER, Mustata Wilson G, Close D, Leimgruber S, Tandon M, Reed RB, Shun TY, Wang QJ, Wipf P, Lazo JS. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.
| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 396.87 |
| Cas No. | 638156-11-3 |
| Formula | C22H21ClN2O3 |
| Solubility | ≥39.7 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥2.34 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 5-(3-chlorophenyl)-N-[4-(morpholin-4-ylmethyl)phenyl]furan-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | O=C(c1ccc(-c2cccc(Cl)c2)[o]1)Nc1ccc(CN2CCOCC2)cc1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | CID-2011756 is a cell-active ATP competitive and specific inhibitor of PKD1. | |||||
| Targets | PKD | |||||
| IC50 | 10±0.7 μM | |||||
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