2. Apoptosis
  3. PKD
  4. Protein kinase D inhibitor 1

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.

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Protein kinase D inhibitor 1 Chemical Structure

Protein kinase D inhibitor 1 Chemical Structure

CAS No. : 2489320-03-6

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Protein kinase D inhibitor 1 Related Antibodies

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Description

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[1].

IC50 & Target

PKD3

17 ± 8 nM (IC50)

PKD2

35 ± 5 nM (IC50)

PKD1

35 ± 10 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
CAPAN-1 IC50
40.7 μM
Compound: 17m
Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
HCT-116 IC50
> 100 μM
Compound: 17m
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
HL-60 IC50
17.9 μM
Compound: 17m
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
K562 IC50
> 100 μM
Compound: 17m
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
LN-229 IC50
80.6 μM
Compound: 17m
Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
NCI-H460 IC50
> 95.8 μM
Compound: 17m
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
Z-138 IC50
35.3 μM
Compound: 17m
Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis
[PMID: 32835918]
In Vitro

Protein kinase D inhibitor 1 (compound 17m) displays excellent PKD2 inhibition with almost no remaining kinase activity at 1 μM[1].
Protein kinase D inhibitor 1 displays only weak antiproliferative activity, and does not significantly affect PANC-1 cell proliferation at a concentration of 5 μM[1].
Protein kinase D inhibitor 1 (0-100 μM, 72 h) shows antitumor activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Protein kinase D inhibitor 1 Related Antibodies

Cell Viability Assay[1]

Cell Line: LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, K-562
Concentration: 0-100 μM
Incubation Time: 72 h
Result: Inhibited of tumor cell growth of LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, and K-562, with IC50 values of 80.6 ± 7, 40.7 ± 14.5, 42.7 ± 4.9, 17.9 ± 4.1, 35.3 ± 10.4, >95.8, >100, and >100, respectively.
Molecular Weight

347.42

Formula

C19H21N7
CAS No.
SMILES

NC1=C2C(N(CC3CCNCC3)N=C2C4=CNC5=C4C=CC=C5)=NC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Protein kinase D inhibitor 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Protein kinase D inhibitor 12489320-03-6Protein kinase D inhibitor1Protein kinase D inhibitor-1PKDProtein kinase DAnticancerLN-229Capan-1DND-41HL-60Z-138NCI-H460HCT-116K-562cortactin phosphorylationInhibitorinhibitorinhibit

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