SML4079
BI-3802
≥98% (HPLC)
别名:
2‐[(6‐{[5‐Chloro‐2‐(cis-3,5‐dimethylpiperidin‐1‐yl)pyrimidin‐4‐yl]amino}‐1-methyl‐2‐oxo‐1,2‐dihydroquinolin‐3‐yl)oxy]‐N-methylacetamide, BI 3802, BI3802
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (Warmed)
储存温度
-10 to -25°C
SMILES字符串
CN1C2=CC=C(NC3=NC(N4C[C@H](C[C@H](C4)C)C)=NC=C3Cl)C=C2C=C(C1=O)OCC(NC)=O
生化/生理作用
Potent and selective BCL6 degrader that targets BTB domain with high-affinity.
BI-3802 is a potent and selective BCL6 degrader that targets BTB domain with high-affinity (IC50 ≤3 nM by ULight assay). BI-3802 induces BCL6 polymerization (filaments formation) and SIAH1 E3 ligase-mediated ubiquitination, leading to proteasomal degradation (by 80% post 90 min 5 µM treatment in SU-DHL-4 cells) and inhibition of BCL6-dependent proliferation in a dose-depenent manner (typical dosing range 0.04 - 3 µM).
BI-3802 is a potent and selective BCL6 degrader that targets BTB domain with high-affinity (IC50 ≤3 nM by ULight assay). BI-3802 induces BCL6 polymerization (filaments formation) and SIAH1 E3 ligase-mediated ubiquitination, leading to proteasomal degradation (by 80% post 90 min 5 µM treatment in SU-DHL-4 cells) and inhibition of BCL6-dependent proliferation in a dose-depenent manner (typical dosing range 0.04 - 3 µM).
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