Chemical Structure : DCLK1-IN-1
CAS No.: 2222635-15-4
货号: 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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥1980 | In stock | |
10 mg | ¥2980 | In stock | |
25 mg | ¥4880 | In stock | |
50 mg | Get quote | ||
100 mg | 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.
分子量 | 527.552 | |
分子式 | C26H28F3N7O2 | |
外观性状 | Solid | |
储存条件 |
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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 |
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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