CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells.
IC50 Value: 10±0.7 uM (cellular inhibition of phospho-Ser916-PKD1 activity) [1]
Target: PKD
CID 2011756, has pan-PKD inhibitory effects (PKD2 IC50 = 0.6±0.1 uM; PKD3 IC50 = 0.7±0.2 uM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor. CID 2011756 was the most potent of the inhibitors with a cellular EC50 of 10±0.7 uM (n = 3), an EC50 value comparable to that of our previously described benzoxoloazepinolone.
| Catalog Number | I013940 |
| CAS Number | 638156-11-3 |
| Molecular Formula | C₂₂H₂₁ClN₂O₃ |
| Purity | ≥95% |
| Target | PKD |
| Solubility | 10 mM in DMSO |
| IUPAC Name | 5-(3-chlorophenyl)-N-[4-(morpholin-4-ylmethyl)phenyl]furan-2-carboxamide |
| InChI | InChI=1S/C22H21ClN2O3/c23-18-3-1-2-17(14-18)20-8-9-21(28-20)22(26)24-19-6-4-16(5-7-19)15-25-10-12-27-13-11-25/h1-9,14H,10-13,15H2,(H,24,26) |
| InChIKey | XQJWTJLJEYIUDZ-UHFFFAOYSA-N |
| SMILES | C1COCCN1CC2=CC=C(C=C2)NC(=O)C3=CC=C(O3)C4=CC(=CC=C4)Cl |
| Reference | [1]. Sharlow ER, et al. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134. |
