CID755673（Cat No.:I003896） is a highly potent and selective small molecule inhibitor of protein kinase D (PKD). With an IC50 of 182 nM, it effectively inhibits PKD activity. Importantly, CID755673 demonstrates selectivity for PKD1 over other kinases such as AKT, PLK1, CAK, CAMKIIα, and various PKC isoforms. This selectivity profile indicates its specificity for PKD1 inhibition. CID755673 is considered a cell-active inhibitor, meaning it can penetrate cells and exert its inhibitory effects on PKD, making it a valuable tool for studying PKD signaling pathways and potential therapeutic applications.
| Catalog Number | I003896 |
| CAS Number | 521937-07-5 |
| Synonyms | 7-hydroxy-2,3,4,5-tetrahydro-[1]benzofuro[2,3-c]azepin-1-one |
| Molecular Formula | C₁₂H₁₁NO₃ |
| Purity | ≥95% |
| Target | PKD |
| Solubility | DMSO: ≥ 40 mg/mL |
| Storage | 2-8°C |
| IC50 | 182 nM |
| IUPAC Name | 7-hydroxy-2,3,4,5-tetrahydro-[1]benzofuro[2,3-c]azepin-1-one |
| InChI | InChI=1S/C12H11NO3/c14-7-3-4-10-9(6-7)8-2-1-5-13-12(15)11(8)16-10/h3-4,6,14H,1-2,5H2,(H,13,15) |
| InChIKey | AACFPJSJOWQNBN-UHFFFAOYSA-N |
| SMILES | C1CC2=C(C(=O)NC1)OC3=C2C=C(C=C3)O |
| Reference | </br>1:The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. Venardos K, De Jong KA, Elkamie M, Connor T, McGee SL.PLoS One. 2015 Mar 23;10(3):e0120934. doi: 10.1371/journal.pone.0120934. eCollection 2015. PMID: 25798941 Free PMC Article</br>2:Protein Kinase Inhibitors CK59 and CID755673 Alter Primary Human NK Cell Effector Functions. Scheiter M, Bulitta B, van Ham M, Klawonn F, König S, Jänsch L.Front Immunol. 2013 Mar 18;4:66. doi: 10.3389/fimmu.2013.00066. eCollection 2013. PMID: 23508354 Free PMC Article</br>3:CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway. Torres-Marquez E, Sinnett-Smith J, Guha S, Kui R, Waldron RT, Rey O, Rozengurt E.Biochem Biophys Res Commun. 2010 Jan 1;391(1):63-8. doi: 10.1016/j.bbrc.2009.11.002. Epub 2009 Nov 5. PMID: 19896460 Free PMC Article |
