An inhibitor of Cdk8 and Cdk19; inhibits Cdk8 (IC50s = 24-50 nM

Senexin B – 25 mg

Brand:
Cayman
CAS:
1449228-40-3
Storage:
-20
UN-No:
Non-Hazardous - /

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.  

 

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Description

An inhibitor of Cdk8 and Cdk19; inhibits Cdk8 (IC50s = 24-50 nM, depending on assay); selectively inhibits Cdk19 and Cdk8 by 98.6 and 97.8%, respectively, in a panel of >450 kinases at 2 μM but does inhibit MAP4K2 and YSK4 by 69 and 59%, respectively; inhibits cell growth in MCF-7, BT474, and T47D-ER/Luc breast cancer cells in estrogen-containing media at 1.25-5 μM; reduces tumor growth in an MCF-7 mouse xenograft model at 100 mg/kg twice per day; inhibits RANKL-induced differentiation of murine BMDMs into osteoclasts at 1 and 1.5 μM; 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 1 μg

Formal name: 4-[[2-[6-[(4-methyl-1-piperazinyl)carbonyl]-2-naphthalenyl]ethyl]amino]-6-quinazolinecarbonitrile

Synonyms:  SNX2-1-165

Molecular weight: 450.5

CAS: 1449228-40-3

Purity: ≥98%

Formulation: A crystalline solid

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