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 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.

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。

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

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。

IBL-302 (AMU302) 是一种口服有效的PIM和PI3K AKT mTOR双信号抑制剂，具有抗乳腺癌和成神经细胞瘤的活性。在裸鼠异种移植模型中，IBL-302 显示出体内效力，并能抑制曲妥珠单抗的耐药性问题。此外，IBL-302 还能增强顺铂、阿霉素和依托泊苷等常见细胞毒性化疗药物的效果。

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.

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.

H-Gly-Leu-Phe-OH (GLF)为源于α-乳白蛋白的三肽，具有免疫刺激性，能够抑制抗癌药物依托泊苷所引起的脱发、表皮增厚以及脂肪细胞层的变薄。

Oliveroline, 一种存在于植物中的生物碱，表现出对Topo I的强效抑制以及对Topo II的卓越抑制能力，其效果超过了类似化合物如topotecan和etoposide。与Topo II形成的复合物相比Topo I显示出更好的稳定性，表明其作为癌症治疗进一步研究的有力候选物。

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。

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

NK-611 free acid is a new semisynthetic analogue of etoposide, which presumably also acts through inhibition of topoisomerase II, and has been found to be more potent against several cancer cell lines in vitro than etoposide.

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).

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.

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

17(R)-Resolvin D3 (17(R)-RvD3) is an aspirin-triggered epimer of resolvin D3, produced from docosahexaenoic acid (DHA) through the action of COX-2 in the presence of aspirin, via a 17(R)-hydroperoxy DHA (17(R)-HDHA) intermediary. Identified in mouse inflammatory exudates, 17(R)-RvD3 notably inhibits the transmigration of isolated human polymorphonuclear cells (PMNs) and fosters the efferocytosis of apoptotic PMNs by macrophages. Furthermore, in a mouse model of zymosan-induced peritonitis, 17(R)-RvD3 administration (10 ng animal) significantly curtails neutrophil infiltration into the peritoneal cavity and modulates cytokine levels by reducing IL-6 and increasing IL-10 in the inflammatory exudate. It engages GPR32, evidenced by activation in a β-arrestin reporter assay and augments phagocytosis more effectively in CHO cells overexpressing GPR32 compared to controls. Additionally, 17(R)-RvD3 enhances the clearance of etoposide-induced tumor cell debris by monocyte-derived macrophages in H460 human lung carcinoma.

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.

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。