Senexin B is an inhibitor of Cdk8 and Cdk19.1 It inhibits Cdk8 with IC50 values ranging from 24 to 50 nM, depending on the assay used. It selectively inhibits Cdk19 and Cdk8 by 98.6 and 97.8%, respectively, in a panel of greater than 450 kinases at 2 μM but does inhibit MAP4K2 and YSK4 by 69 and 59%, respectively. Senexin B (1.25-5 μM) inhibits cell growth in MCF-7, BT474, and T47D-ER/Luc breast cancer cells in estrogen-containing media in a concentration-dependent manner.2 It reduces tumor growth in an MCF-7 mouse xenograft model when administered at a dose of 100 mg/kg twice per day. Senexin B (1 and 1.5 μM) also inhibits RANKL-induced differentiation of murine bone marrow-derived macrophages (BMDMs) into osteoclasts.3 It increases the bone volume fraction and bone mineral density in injured tibiae in a rat model of cancellous bone injury and regeneration when administered locally at a dose of 1 μg.
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