CRT0066101
For research use only. Not for use in humans.
Catalog No.S8366
Molecular Weight(MW): 411.33
CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple.
Purity & Quality Control
Choose Selective Serine/threonin kinase Inhibitors
Biological Activity
| Description | CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple. | ||||||
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| Targets |
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| In vitro |
CRT0066101 reduces BrdU incorporation, increases apoptosis, blocks neurotensin (NT)-induced PKD1/2 activation, reduces NT-induced PKD-mediated Hsp27 phosphorylation, attenuates PKD1-mediated NF-κB activation, and abrogates expression of NF-κB-dependent-dependent proliferative and pro-survival proteins. CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 μM. It also significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. Thus, CRT0066101 significantly blocks proliferation of PaCa cells that express moderate to high endogenous levels of PKD1/2. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells, also abrogates NT-induced phosphorylation of Hsp27 (pS82-Hsp27), which is a physiological substrate of PKD1/2 in a dose-dependent manner[1]. |
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| Assay |
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| In vivo | CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67+ proliferation index (p< 0.01), increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1. CRT0066101 blocks Panc-1 cell proliferation and growth in multiple xenograft models[1] |
Protocol
| Cell Research: |
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| Animal Research: |
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Solubility (25°C)
| In vitro | Water | 82 mg/mL (199.35 mM) |
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| DMSO | 25 mg/mL warmed (60.77 mM) | |
| Ethanol | 2 mg/mL warmed (4.86 mM) |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 411.33 |
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| Formula | C18H22N6O.2HCl |
| CAS No. | 1883545-60-5 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
| Smiles | Cl.Cl.CCC(N)CNC1=NC(=NC=C1)C2=C(O)C=CC(=C2)C3=C[N](C)N=C3 |
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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