产品描述:
Senexin B is an inhibitor of Cdk8 and Cdk19.{42922} 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.{42923} 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.{42924} 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.