PKD1 Inhibitor

IKK 16 is an orally active IKK inhibitor. IKK 16 shows IC₅₀s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC₅₀s of 153.9, 115, and 99.7 nM, respectively. IKK 16 is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.

CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC₅₀ values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC₅₀ of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.

1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC₅₀s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.

CRT0066101 is a potent and orally active PKD inhibitor with IC₅₀ values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 is also a potent PIM2 inhibitor with an IC₅₀ of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.

IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC₅₀s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC₅₀s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.

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

BPKDi is an inhibitor of PKD. BPKDi inhibits three members of the PKD family, PKD1, PKD2, and PKD3, with IC₅₀ values of 1 nM, 9 nM, and 1 nM, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes and concomitantly suppresses hypertrophy of these cells.

CID 2011756 is an ATP competitive PKD inhibitor, with an IC₅₀ of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC₅₀, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.

kb NB 142-70 is a potent PKD inhibitor, with IC₅₀s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.

PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC₅₀ value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure.

3-IN-PP1 is a protein kinase D (PKD) inhibitor. 3-IN-PP1 has potent pan-PKD inhibitory activity for PKD1, PKD2 and PKD3 with IC₅₀ values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research of cancer.

CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC₅₀ values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC₅₀ of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.

Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC₅₀ values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation.