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DCLK1-IN-1

Chemical Structure : DCLK1-IN-1

CAS No.: 2222635-15-4

DCLK1-IN-1 (DCLK1 inhibitor)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 527.552
Formula C26H28F3N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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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