Protein kinase D (PKD)

CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively).

kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively).

CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

CID797718 is a structural analog of CID755673 (Adooq Catalog No. A13804). It was a 10-time less potent PKD1 inhibitor with an IC50 value of 7.0 +/-0.8 uM.

CRT-0066101, potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively).

CRT5 (CRT0066051), a pyrazine benzamide, is a potent and selective PKD inhibitor with IC50 of 1 nM, 2 nM, and 1.5 nM for PKD1, PKD2, and PKD3, respectively.

CRT0066101 is a PRKDs inhibitor. CRT0066101 suppressed the proliferation and migration of four bladder cancer cell lines in vitro. CRT0066101 blocked tumor growth in a mouse flank xenograft model of bladder cancer.

BPKDi is a potent inhibitor of Protein Kinase D (PKD), targeting PKD1, PKD2, and PKD3 with IC50 values of 1 nM, 9 nM, and 1 nM, respectively. This compound effectively disrupts signal-dependent phosphorylation and nuclear export of class IIa histone deacetylases (HDACs) in cardiomyocytes, consequently attenuating cellular hypertrophy. BPKDi serves as a valuable tool for investigating the role of PKD in cardiovascular research and therapeutic interventions.

CRT0066101 is a potent and orally active inhibitor of Protein Kinase D (PKD) with IC50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively. Additionally, it serves as an effective PIM2 inhibitor with an IC50 of approximately 135.7 nM. This compound exhibits notable anti-inflammatory activity demonstrated in LPS-induced lung injury models in mice, as well as anticancer effects, making it a valuable tool for research in cancer and inflammation-related studies.

CRT0066101 trihydrochloride is a potent inhibitor of Protein Kinase D (PKD), exhibiting IC50 values of 1 nM, 2.5 nM, and 2 nM against PKD1, PKD2, and PKD3, respectively. In addition to its PKD-inhibitory properties, it also targets PIM2 with an IC50 of approximately 135.7 nM. This compound demonstrates significant anti-inflammatory effects in lipopolysaccharide (LPS)-induced lung injury models in mice and exhibits potential anticancer activity, making it a valuable reagent for research in oncology and inflammation.

PKC/PKD-IN-1 is a potent dual inhibitor of protein kinase C and protein kinase D, exhibiting an IC50 of 0.6 nM against PKD1. This compound demonstrates the ability to mitigate cardiac hypertrophy induced by high-salt diets, making it a valuable tool for investigating mechanisms related to heart failure. Its specificity and efficacy position it as a significant reagent for researchers focused on cardiac disease and kinase signaling pathways.

3-IN-PP1 is a selective inhibitor of protein kinase D (PKD), demonstrating potent inhibition across PKD isoforms PKD1, PKD2, and PKD3 with IC50 values of 108 nM, 94 nM, and 108 nM, respectively. This compound exhibits broad-spectrum anticancer activity, effectively inhibiting the proliferation of various tumor cell lines. 3-IN-PP1 serves as a valuable tool for cancer research, particularly in studying the role of PKD signaling pathways in tumor growth and development.

Protein kinase D inhibitor 1 is a potent pan-PKD inhibitor that exhibits IC50 values between 17 to 35 nM. This compound selectively inhibits the phosphorylation of cortactin mediated by Protein kinase D, thereby influencing cellular processes related to cytoskeletal dynamics and signal transduction. It is valuable for research applications focused on studying PKD signaling pathways and their impact on various cellular functions.