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Chemical Structure : DCLK1-IN-1
CAS No.: 2222635-15-4
Catalog No.: PC-38227Not For Human Use, Lab Use Only.
DCLK1-IN-1 is the first potent, selective inhibitor of the DCLK1 and DCLK2 kinases with IC50 of 9.5 nM and 31 nM in binding assays, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $268 | In stock | |
| 25 mg | $468 | In stock | |
| 100 mg | Get quote | ||
| 200 mg | Get quote | ||
| 1 g | Get quote |
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DCLK1-IN-1 is the first potent, selective inhibitor of the DCLK1 and DCLK2 kinases with IC50 of 9.5 nM and 31 nM in binding assays, respectively.
DCLK1-IN-1 exclusively inhibited DCLK1 and DCLK2 across a panel of 489 human kinases, significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lysates and live cells, did not inhibit any kinases under these conditions.
DCLK1-IN-1 displays pronounced on-target DCLK1 activity in vitro, and is suitable probe for in vivo evaluation.
Proteins associated with cell motility, including HN1, ZIP8 and FYN, were significantly downregulated after DCLK1-IN-1 treatment in the organoid cultures.
| M.Wt | 527.552 | |
| Formula | C26H28F3N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-11-methyl-5-(2,2,2-trifluoroethyl)-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one |
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1. Fleur M Ferguson, et al. Nat Chem Biol. 2020 Jun;16(6):635-643.
2. Fleur M Ferguson, et al. J Med Chem. 2020 Jul 23;63(14):7817-7826.
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