SML4032
CPSF3-IN-1
≥98% (HPLC)
别名:
3-(1,3-Ddihydro-1-hydroxy-2,1-benzoxaborol-7-yl)-N-(40- acetyl-1,10-biphenyl-3-yl) propanamide, N-(4′-Acetyl[1,1′-biphenyl]-3-yl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole-7-propanamide; benzoxaborole 1
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(NC1=CC(C2=CC=C(C=C2)C(C)=O)=CC=C1)CCC3=CC=CC4=C3B(OC4)O
InChI
1S/C24H22BNO4/c1-16(27)17-8-10-18(11-9-17)20-5-3-7-22(14-20)26-23(28)13-12-19-4-2-6-21-15-30-25(29)24(19)21/h2-11,14,29H,12-13,15H2,1H3,(H,26,28)
InChI key
KANKQAZGSKQFCK-UHFFFAOYSA-N
相关类别
生化/生理作用
Cell penetrant, potent and selective inhibitor of endonuclease activity of CPSF3 in vitro that limits transcriptional termination in cells.
CPSF3-IN-1 (3-(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl)-N-(40- acetyl-1,10-biphenyl-3-yl) propenamide) is a cell penetrant, potent and selective inhibitor of endonuclease activity of CPSF3 (cleavage and polyadenylation specific factor 3) in vitro that limits transcriptional termination in cells. CPSF3-IN-1 binds to CPSF3 active site and causes transcription readthrough. It potently inhibits growth of numerous cancer cell lines (IC50 = 0.28 µM HCT116 cells).
CPSF3-IN-1 (3-(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl)-N-(40- acetyl-1,10-biphenyl-3-yl) propenamide) is a cell penetrant, potent and selective inhibitor of endonuclease activity of CPSF3 (cleavage and polyadenylation specific factor 3) in vitro that limits transcriptional termination in cells. CPSF3-IN-1 binds to CPSF3 active site and causes transcription readthrough. It potently inhibits growth of numerous cancer cell lines (IC50 = 0.28 µM HCT116 cells).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Ye Tao et al.
Cell chemical biology, 31(1), 139-149 (2023-11-16)
A novel class of benzoxaboroles was reported to induce cancer cell death but the mechanism was unknown. Using a forward genetics platform, we discovered mutations in cleavage and polyadenylation specific factor 3 (CPSF3) that reduce benzoxaborole binding and confer resistance.
Jiong Zhang et al.
Journal of medicinal chemistry, 62(14), 6765-6784 (2019-07-03)
Benzoxaboroles, as a novel class of bioactive molecules with unique physicochemical properties, have been shown to possess excellent antimicrobial activities with tavaborole approved in 2014 as an antifungal drug. Although urgently needed, the investigation of benzoxaboroles as anticancer agents has
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