Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Protein kinase D inhibitor 1 (compound 17m) is a potent pan-PKD inhibitor. It exhibits inhibitory activity in the low nanomolar range, with IC50 values ranging between 17 and 35 nM. By inhibiting protein kinase D, this compound effectively suppresses cortactin phosphorylation, which is known to be PKD-dependent [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Protein kinase D inhibitor 1 (compound 17m) is a potent pan-PKD inhibitor. It exhibits inhibitory activity in the low nanomolar range, with IC50 values ranging between 17 and 35 nM. By inhibiting protein kinase D, this compound effectively suppresses cortactin phosphorylation, which is known to be PKD-dependent [1]. |
In vitro | Protein kinase D inhibitor 1 (compound 17m) exhibits potent inhibition of PKD2, rendering virtually no kinase activity at a concentration of 1 μM [1]. Despite its significant inhibitory effect on PKD2, it demonstrates minimal antiproliferative effects, failing to notably impact the proliferation of PANC-1 cells at 5 μM [1]. However, when tested across a range of concentrations (0-100 μM) over 72 hours, it reveals antitumor activity [1]. Through a Cell Viability Assay conducted on various cell lines including LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, and K-562, this compound effectively inhibited the growth of these tumor cells. The inhibitory concentrations (IC50) for achieving 50% growth inhibition were notably diverse across different cell lines, recorded as 80.6 ± 7, 40.7 ± 14.5, 42.7 ± 4.9, 17.9 ± 4.1, 35.3 ± 10.4 for the first five lines respectively, while being greater than 95.8 µM for NCI-H460, and exceeding 100 µM for both HCT-116 and K-562 [1]. |
Molecular Weight | 347.42 |
Formula | C19H21N7 |
CAS No. | 2489320-03-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Protein kinase D inhibitor 1 2489320-03-6 inhibitor inhibit