2. Signaling Pathways
  3. Apoptosis
  4. PKD
  5. PKD3 Isoform

PKD3

Protein kinase D3 (PKD3, PRKD3) is a serine/threonine kinase of the protein kinase D family that functions downstream of diacylglycerol and protein kinase C signaling, integrating signals from growth factors, hormones, and G-protein-coupled receptor agonists to regulate cellular proliferation, survival, migration, and gene expression[1][2]. Mechanistically, PKD3 participates in oncogenic signaling networks that control cell-cycle progression, metabolic reprogramming, and tumor-associated transcriptional responses, including activation of ERK1/c-MYC and NF-κB-associated pathways[3][4][5]. In disease models, elevated PKD3 expression has been reported in prostate cancer, hepatocellular carcinoma, gastric cancer, and triple-negative breast cancer, where PKD3 promotes tumor growth, survival, invasion, and metastatic potential[4][6][7]. PKD3 also contributes to glycolytic regulation through the p65/PFKFB3 axis, linking kinase signaling to cancer cell metabolic adaptation[5]. Compared with related isoforms, PKD3 displays distinct biological properties, including constitutive localization in both the cytoplasm and nucleus and the absence of the C-terminal PDZ-binding motif present in PKD1 and PKD2, supporting isoform-specific signaling functions[2]. Furthermore, PKD3 lacks the C-terminal autophosphorylation site found in other PKD family members, a feature associated with divergent regulatory behavior and downstream signaling outputs[2]. For experimental applications, pharmacological PKD inhibitors such as CRT0066101 suppress PKD-dependent signaling, reduce proliferation and tumor growth in multiple cancer models, and are widely used to investigate PKD3-mediated mechanisms and therapeutic vulnerabilities[8][9].

PKD3 Related Products (12):

Cat. No. Product Name Effect Purity
  • HY-13687
    IKK 16
    		Inhibitor 99.88%
    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.
  • HY-15698A
    CRT0066101 dihydrochloride
    		Inhibitor 99.97%
    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.
  • HY-15698
    CRT0066101
    		Inhibitor 99.88%
    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.
  • HY-13941
    1-Naphthyl PP1
    		Inhibitor 99.36%
    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.
  • HY-12239
    CID755673
    		Inhibitor 99.13%
    CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.
  • HY-13687A
    IKK 16 hydrochloride
    		Inhibitor 99.95%
    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.
  • HY-118052
    BPKDi
    		Inhibitor 99.74%
    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.
  • HY-13454
    CID 2011756
    		Inhibitor
    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.
  • HY-15528
    kb NB 142-70
    		Inhibitor 98.02%
    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.
  • HY-151374
    3-IN-PP1
    		Inhibitor 99.37%
    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.
  • HY-151372
    Protein kinase D inhibitor 1
    		Inhibitor
    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.
  • HY-15698B
    CRT0066101 trihydrochloride
    		Inhibitor
    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.