BI-D1870 CAS NO.501437-28-1

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BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embry-onic kidney 293 cells and Rat-2 cells. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB .These experiments confirmed strong interaction with BRD4(1) for the PLK inhibitors BI-2536 (Kd = 37 ± 3 nM) and BI-6727 (Kd = 79 ± 3 nM) and the related RSK inhibitor BI-D1870 (Kd = 3.5 ± 0.17 μM). The closely related JAK inhibitors TG-101348 and TG-101209 bound BRD4(1) with nanomolar affinities (Kd values: 164 ± 10 nM and 123 ±18 nM, respectively).