double-strand dna breaks

UNC-2170 (UNC2170 Maleate) 是53BP1(IC50=29 µM;Kd=22 µM) 选择性的、功能活性的片段状配体，对 53BP1 的选择性比其他九种甲基赖氨酸读取器蛋白质高出至少17倍。53BP1 是 Kme 结合蛋白，在 DNA 损伤修复途径中起核心作用，并被招募到双链断裂位点。

Irinotecan (CPT-11) 是喜树碱的衍生物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接，并导致双链 DNA 断裂和细胞死亡，具有抗肿瘤活性。

COH29 (RNR Inhibitor COH29) 是一种口服可用的芳香族取代噻唑，是人类核糖核苷酸还原酶 (RNR) 的抑制剂，具有潜在的抗肿瘤活性。它抑制核糖核苷酸还原酶的IC50为 16 μM。

Calicheamicin (Calicheamicin γ1) 是肿瘤抗生素，可引起DNA 双链断裂，抑制DNA 合成。

Calicheamicin (GMP)是 Calicheamicin 的 GMP 级别试剂。Calicheamicin 是一种肿瘤抗生素，可引起DNA 双链断裂，抑制DNA 合成。

Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic. It recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin leads to apoptosis. Neocarzinostatin has potential for EpCAM-positive cancer treatment.

5-BrdUTP sodium salt is a TdT substrate used for labeling DNA double-strand breaks.

XSJ05，一种喜树碱 (CPT) 衍生物，能有效抑制拓扑异构酶 I (Topo I) 以发挥抗癌作用。该化合物能促使 DNA 双链断裂，进而引起 DNA 损伤。此外，XSJ05 对抑制结直肠癌 (CRC) 生长具有显著效果，能使细胞周期在 G2 M 期暂停，并能诱导细胞凋亡 (apoptosis)。

PARP1-IN-27 (Compound 9B)，作为PARP1和PARP2的有效抑制剂，在SUM149PT细胞中的IC50分别达到2.53 nM和6.45 nM。此外，PARP1-IN-27对BRCA突变癌细胞系SUM149PT、HCC1937和Capan-1的增殖抑制效果显著，相应的IC50值为0.62、1.91和4.26 μM。该化合物能够加剧DNA双链断裂，促进ROS生成，并在G2 M期阻滞细胞周期，最终在SUM149PT细胞中触发细胞凋亡(apoptosis)。

GSK_WRN4 作为一种 WRN 解旋酶抑制剂，具有抗癌活性，通过引发 DNA 双链断裂抑制 MSI 肿瘤细胞的生长，可用于研究癌症。

AcBut-N-Ac-γ-Calicheamicin 是一种 ADC 毒素，通过引发 DNA 双链断裂导致细胞周期停滞和凋亡 (Apoptosis)。其主要用于抗体药物偶联物 (ADC) 的合成，有潜力应用于癌症研究，特别是急性淋巴细胞白血病 (ALL) 和其他血液系统恶性肿瘤的研究。

Tilatamig samrotecan (AZD9592) 是一种抗体偶联药物（ADC），用于递送拓扑异构酶I抑制剂（TOP1i），以靶向表皮生长因子受体（EGFR）和c-MET，展现抗肿瘤作用。Tilatamig samrotecan (AZD9592) 能诱导DNA双链断裂，增加pRAD50和γH2AX的表达，从而抑制非小细胞肺癌的生长。

HDAC-IN-85 (Compound 1) 是一种能够通过血脑屏障的HDAC抑制剂，对脑肿瘤细胞系表现出抑制作用。它可以诱导乙酰化，导致DNA双链断裂，并诱导RAD51泛素化，从而破坏DNA修复过程。HDAC-IN-85 可用于胶质母细胞瘤的研究。

Etoposide phosphate is a phosphate salt of Etoposide, which binds to the enzyme topoisomerase II, then induces double-strand DNA breaks and inhibits DNA repair, leading to decreased DNA synthesis and tumor cell proliferation.

Cylindrospermopsin, a tricyclic uracil derivative, is a cyanobacterial toxin that was first discovered in an algal bloom contaminating a local drinking supply on Palm Island in Queensland, Australia after an outbreak of a mysterious disease. Cylindrospermopsin targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), leading to cell death. [1] It has been shown to inhibit the activity of the uridine monophosphate synthase complex with a Ki value of 10 µM.[2] Cylindrospermopsin is genotoxic, inducing DNA damage as evidenced by double strand breaks and reducing cell viability in HepG2 cells at 0.1-0.5 µg ml.[3]

Topoisomerase II inhibitor 6 (Compound 5) 是色胺酮的衍生物。它是一种有效的拓扑异构酶的选择性抑制剂。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA 双链断裂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系具有抗增殖活性，在癌症疾病研究中具有潜力。

p53 Activator 2 (compound 10ah) 插入DNA，导致显著的DNA双链断裂。该化合物通过增加p53、p-p53、CDK4、p21的表达，使细胞周期在G2 M期停滞，诱导细胞凋亡，并显著降低抗凋亡蛋白Bcl-2、Bcl-xL和cyclin B1的水平。此外，p53 Activator 2表现出对MGC-803细胞的抗增殖效果，其IC50为1.73 μM，且在MGC-803异种移植肿瘤模型中展示出有效的抗癌活性。

Simmiparib (SMOCL-9112) 是一种新型有效的 PARP1 和 PARP2 抑制剂，是一种Olaparib 衍生物。Simmiparib 在同源重组修复 (HR) 缺陷细胞中诱导 DNA 双链断裂 (DSB) 和 细胞周期阻滞，从而促使细胞凋亡 (apoptosis)。Simmiparib 可用于研究帕金森病、阿尔茨海默病、乳腺癌和黑色素瘤。

Amsacrine Isothionate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S G2 phase of the cell cycle, and cell death.

Amsacrine lactate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S G2 phase of the cell cycle, and cell death.

Amsacrine gluconate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S G2 phase of the cell cycle, and cell death.

Amonafide L-malate is the malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis.

PARP1-IN-12 是一种有效的PARP1抑制剂，其IC50值为 2.99 nM。PARP1-IN-12 具有较好的抗癌细胞增殖活性，可诱导细胞凋亡并使细胞周期停滞在 G2 M 期。PARP1-IN-12 能在BRCA 缺陷的细胞中诱导 DNA 双链断裂 (DSBs)。

Selenocystine为一种广谱抗癌剂，能诱导HepG2细胞发生DNA损伤，尤其是 DNA 双链断裂(DSBs)。Selenocystine在靶向DNA修复领域，作为癌症治疗的潜在治疗或辅助剂，展现出显著的应用前景。