| Description |
BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinases MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells, Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.
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| Related Catalog |
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| Target |
IC50: 64 nM (MRCKβin SCC12 cells), Ki: 0.0136 nM/ 0.0233 nM (MRCKα/β)[1].
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| In Vitro |
BDP9066 shows antiproliferative effects with greatest activity in hematologic cancer cells. BDP9066 inhibits MLC phosphorylation and blocks SCC12 squamous cell carcinoma motility and invasion[1].
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| In Vivo |
BDP9066 topical application significantly decreases phosphorylated MRCKα S1003 staining and tumor volumes[1].
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| References |
[1]. Unbekandt M, et al. Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer. Cancer Res. 2018 Apr 15;78(8):2096-2114.
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