etoposide

Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂，通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性，可以诱导细胞凋亡、自噬。

M50054 是一种有效的细胞凋亡抑制剂，可用于研究抗 Fas 抗体引起的肝炎和化疗引起的脱发。它抑制 Etoposide 诱导的 U937 细胞 caspase-3 活化，IC50为 79 μg/mL。

Etoposide phosphate disodium (BMY-40481 disodium), a phosphate ester prodrug of etoposide, functions as a potent chemotherapeutic agent by selectively inhibiting topoisomerase II, hindering the re-ligation of DNA strands. It is regarded as the active equivalent of etoposide, effectively inducing cell cycle arrest, apoptosis, and autophagy in cancer cells.

Etoposide Phosphate是一种选择性和可口服的topoisomerase II抑制剂和癌症化疗药品，通过DNA损伤、p53通路和细胞周期G2/M阻滞,抑制癌细胞的生长和诱导凋亡

Etoposide-13C,D3是一种带有 13C 和氘标记的Etoposide (T0132)。Etoposide (VP-16; VP-16-213)是广泛使用的抗肿瘤化疗剂，通过抑制拓扑异构酶 II (topoisomerase-II)来阻止 DNA 复制。它可诱导细胞周期停滞、凋亡 (apoptosis)和自噬 (autophagy)。

Etoposide (Standard) 是一种可用于分析的标准物质，通常用作 Etoposide 的研究和分析中参考的标准样品。Etoposide (VP-16-213) 是一种拓扑异构酶 II 的抑制剂，通过与拓扑异构酶 II 和 DNA 形成复合物来抑制 DNA 合成 (IC50=60.3 μM)。Etoposide 具有抗肿瘤活性，可以诱导细胞凋亡、自噬。

Etoposide-[13C,D3] (Standard) 是 Etoposide-[13C,D3] 的标准品，适用于定量分析、质量控制及生化实验等相关研究。

ProTAME is an inhibitor of APC/CFzr and APC/CCdc20. Combinations of proTAME with topoisomerase inhibitors, doxorubicin and etoposide, significantly increase cell death in primary cells and Multiple Myeloma (MM) cell lines, particularly if TOPIIα levels are first increased through pre-treatment with ProTAME.This compound is unstable in powder form and other related salt forms are recommended.

Pifithrin-α, p-Nitro, Cyclic (PFN-α) 是 p53 的细胞渗透性和活性形式抑制剂。它对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级，ED50为30 nM。它也作为 p53 转录后的活性抑制剂。

BRD-K20733377作为一种Bcl-2抑制剂，对IMR-90衰老细胞显示了选择性的细胞毒性，并能抑制这些由Etoposide诱导的细胞，具有10.7 μM的IC50。此外，该化合物在老年小鼠模型中能有效降低与衰老相关的基因p16、p21和KI67的mRNA表达水平。

NecroX-2 是一种可透过细胞膜的坏死抑制剂，具有抗氧化特性。NecroX-2 能够选择性抑制由氧化应激诱导的坏死性细胞死亡。NecroX-2 对由 staurosporine 或 etoposide 诱导的凋亡无保护作用，但在冷休克、缺氧及氧化应激条件下能够有效发挥细胞保护作用。

P-gp inhibitor 24 (Compound 10) 是一种用于抑制 P-糖蛋白 (P-gp) 的抑制剂，能够阻止 P-gp 介导的荧光染料外排过程。该化合物在逆转多药耐药 (MDR) 方面显示出显著效果，能够增强 Vincristine 和 Etoposide 对癌细胞的细胞毒性作用。

TMPO (3,3,5,5-Tetramethyl-1-pyrroline 1-oxide) 是一种自旋捕获剂，针对自由基 (free radicals) 发挥作用。它能够清除超氧阴离子和羟基自由基，并抑制胸腺细胞的凋亡。其抑制 DNA 碎片化的 EC50 值在诱导 DNA 片段化过程中为 19.1 mM (MPS 诱导) 至 30.7 mM (Etoposide 诱导)。TMPO 能与细胞内自由基反应，生成稳定的硝基氧自由基产物，从而减轻氧化应激（例如降低过氧化物水平、维持谷胱甘肽含量），并阻断细胞凋亡途径中的氧化事件。TMPO 在研究如胸腺细胞等免疫细胞凋亡方面具有潜力。

PNR-3-80 是一种选择性 EndoG 抑制剂，其对 EndoG 的 IC50 值为 0.67 μM，优于对 DNase I 的抑制。PNR-3-80 对 DNase II、RNase A、蛋白酶、乳酸脱氢酶以及超氧化物歧化酶 1 无抑制作用。它展现出显著的细胞保护活性，能够有效保护人前列腺癌细胞不受 Cisplatin 和 Docetaxel 引发的细胞死亡影响，并抑制 Etoposide 引起的 DNA 损伤和自噬 (autophagy)。PNR-3-80 适用于细胞损伤的研究。

MS-073 (CP-162398) is a P-glycoprotein inhibitor (P-gp). The in vitro resistance to vincristine (VCR) was almost completely reversed in VCR-resistant P388 cells, and the resistance of VCR, adriamycin (ADM), etoposide, and actinomycin D in ADM-resistant hu

NK 611 is a new semisynthetic analogue of etoposide and has been found to be more potent against several cancer cell lines in vitro than etoposide.

NSC 660028 is a novel γ-lactone ring modified arylamino etoposide analogram with strong antitumor activity as an inhibitor of human DNA topoisomerase II.

10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).

Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793

ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。

Heptelidic acid (Koningic acid) 是一种源自益生菌米曲霉的倍半萜内酯倍半萜类抗生素，是一种选择性 GAPDH 抑制剂，通过下调 caspase 从而抑制 Etoposide 诱导的细胞凋亡。Heptelidic acid 以浓度依赖性方式抑制 tau 纤维化，通过控制甘油醛-3-磷酸脱氢酶活性对肠外黑色素瘤发挥抗肿瘤作用。

AZD6918 is a novel potent and selective inhibitor of the Trk tyrosine kinases. AZD-6918 attenuates the BDNF/TrkB-induced protection of neuroblastoma cells from etoposide in vitro and in vivo. AZD6918 inhibited wild-type TrkB-induced cell migration and cell growth.

NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. The DNA breaks occurred within 1h after treatment with NK314 even without digestion of topoisomerase II by proteinase K, whereas etoposide required digestion of the enzyme protein in cleavable complex to detect DNA breaks. Pretreatment with topoisomerase II catalytic inhibitors, ICRF-193 and suramin, reduced both cleavable complex-mediated DNA breaks and proteinase K-independent DNA breaks, but protease inhibitors and nuclease inhibitors only decreased the latter.

CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, doxorubicin in 47%, etoposide in 38% and Ara-C in 14% of AML samples.