生物活性 | |||
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描述 | BCL6, a member of the BTB/POZ family of transcription factors, is the most frequently involved oncogene in diffuse large B cell lymphomas (DLBCLs) [2]. CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM PMID: 20385364. CID5721353 specifically disrupts BCL6 corepressor recruitment and can specifically reactivate BCL6 target genes in BCL6-dependent DLBCLs. It can also Selectively Kill BCL6-Dependent DLBCL Cells [2]. CID5721353 Suppresses Human DLBCL Xenografts in Mice. The levels of serum human β2-microglobulin (a surrogate marker of the xenograft burden) are significantly reduced by CID5721353 in the xenografted mice as compared with their respective controls for the OCI-Ly7 and SU-DHL6 xenografts (p=0.0117 and p=0.0004, respectively) [2]. | ||
作用机制 | CID5721353 binds to a Pocket in the Lateral Groove of the BCL6BTB Domain [2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.93mL 2.19mL 1.09mL |
21.87mL 4.37mL 2.19mL |
参考文献 |
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