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.
For research use only. We do not sell to patients.
- CAS No.: 2489320-03-6
- Formula: C19H21N7
- Molecular Weight:347.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PKD3 17 ± 8 nM (IC50) |
PKD2 35 ± 5 nM (IC50) |
PKD1/PKCμ 35 ± 10 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | IC50 |
40.7 μM
Compound: 17m
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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
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[PMID: 32835918] |
| HCT-116 | IC50 |
>100 μM
Compound: 17m
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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
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[PMID: 32835918] |
| HL-60 | IC50 |
17.9 μM
Compound: 17m
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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
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[PMID: 32835918] |
| K562 | IC50 |
>100 μM
Compound: 17m
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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
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[PMID: 32835918] |
| LN-229 | IC50 |
80.6 μM
Compound: 17m
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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
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[PMID: 32835918] |
| NCI-H460 | IC50 |
>95.8 μM
Compound: 17m
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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
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[PMID: 32835918] |
| Z-138 | IC50 |
35.3 μM
Compound: 17m
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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
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[PMID: 32835918] |
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.
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Cell Line:LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, K-562
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Concentration:0-100 μM
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Incubation Time:72 h
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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.
Chemical Information
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CAS No. 2489320-03-6
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Molecular Weight 347.42
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Formula C19H21N7
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SMILES
NC1=C2C(N(CC3CCNCC3)N=C2C4=CNC5=C4C=CC=C5)=NC=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protein kinase D inhibitor 1 Related Classifications
HY-151372 Related Classifications
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