TopBP1 inhibitor CS18

Chemical Structure : TopBP1 inhibitor CS18

加入收藏

货号: PC-27615Not For Human Use, Lab Use Only.

TopBP1 inhibitor CS18 is a potent and selective C-terminal BRCT7/8 domains of topoisomerase IIβ-binding protein 1 (TopBP1) inhibitor, competes with pS1159 peptide for binding to TopBP1-BRCT7/8 with IC50 of 2.47 nM.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

TopBP1 inhibitor CS18 is a potent and selective C-terminal BRCT7/8 domains of topoisomerase IIβ-binding protein 1 (TopBP1) inhibitor, competes with pS1159 peptide for binding to TopBP1-BRCT7/8 with IC50 of 2.47 nM.
CS18 selectively disrupts TopBP1 interactions with E2F1, mutp53, MIZ1, PLK1, and CIP2A, but not RPA2 or Rad9.
CS18 promotes MIZ1 binding to the p21Cip1 promoter and inhibits the expression of MYC target genes, such as Cyclin D1, Rad51, and ACTL6A.
CS18 exhibits potent on-target inhibitory activity in cell growth across a broad spectrum of cancer cell lines MDA-MB-468 TNBC cells (IC50 = 0.15 μM), MDAH-2774 ovarian cancer cells (IC50 = 0.18 μM), and cisplatin-resistant A2780cis ovarian cancer cells (IC50 = 0.46 μM), CS18 also markedly decreased cell proliferation in lung cancer cell lines, including A549 (IC50 = 0.5 μM), HCC95 (IC50 = 0.54 μM), HCC2814 (IC50 = 0.67 μM), and EGFR-mutated H1975 cells (IC50 = 0.32 μM).
CS18 inhibits clonogenic survival of different cancer cell lines and the growth of breast tumor spheres. CS18 synergizes with PARP inhibitor talazoparib and osimertinib, synergistically induces apoptosis and inhibits cell viability, overcomes osimertinib resistance in H1975 cells.
CS18 (40 mg/kg, intraperitoneally) inhibits tumor growth in a breast cancer PDX model and combines with osimertinib to overcome osimertinib resistance in lung cancer xenografts.

物理化学性质&存储条件

分子量	378.43
分子式	C22H22N2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-hydroxy-4-((4-(4-hydroxyphenyl)piperazin-1-yl)methyl)-6-phenyl-2H-pyran-2-one

参考文献

1. Lin FT, et al. Sci Adv. 2026 Aug 7;12(32):eaeg1996.