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BI-3802

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Chemical Structure| 2166387-65-9 同义名 : -
CAS号 : 2166387-65-9
货号 : A464286
分子式 : C24H29ClN6O3
纯度 : 99%+
分子量 : 484.978
MDL号 : MFCD31692350
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(10.31 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 BCL6 is a transcriptional repressor required in mature B cells during the germinal center (GC) reaction. Multiple mechanisms act coordinately to timely modulate BCL6 expression at transcriptional and post-transcriptional levels. BCL6 prevents premature activation and differentiation of GC B cells and provides an environment tolerant of the DNA breaks associated with immunoglobulin gene remodeling mechanisms involved in the production of high-affinity antibodies of different isotypes[1]. Bcl6 knockdown under physiological conditions caused increased oxidative stress, apoptosis, and expression of pro-inflammatory cytokines.[2]. BI-3802 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3802 has antitumor activity[3]. BI-3802 is a small molecule that binds to the Broad-complex, Tramtrack and Bric-à-brac (BTB) domain of the oncogenic transcription factor B cell lymphoma 6 (BCL6) and leads to the proteasomal degradation of BCL6. It induces polymerization coupled to highly specific protein degradation, which in the case of BCL6 leads to increased pharmacological activity compared to the effects induced by other BCL6 inhibitors[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.31mL

2.06mL

1.03mL

20.62mL

4.12mL

2.06mL
参考文献

[1]Katia Basso,et al. Roles of BCL6 in normal and transformed germinal center B cells. Immunol Rev. 2012. 247(1), 172-83.

[2]Yang Gu,et al. Bcl6 knockdown aggravates hypoxia injury in cardiomyocytes via the P38 pathway. Cell Biol Int. 2019. 43(2), 108-116.

[3]Kerres N, et al. Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6. Cell Rep. 2017. 20(12), 2860-2875.

[4]Slabicki, M., Yoon, H. et al. Small-molecule-induced polymerization triggers degradation of BCL6. Nature. 2020. 588, 164-168.