ht-1080

Ferrostatin-1 (Fer-1) 是一种铁死亡抑制剂，具有强效性和选择性。Ferrostatin-1 有效抑制 Erastin 诱导的 HT-1080 细胞铁死亡 (EC50=60 nM)。Ferrostatin-1 还具抗氧化和抗真菌活性。

3-Methylcarbazole (NSC-10154) 是具有抗癌作用的咔唑生物碱化合物。3-Methylcarbazole 对人纤维肉瘤 HT-1080 细胞具有生长抑制活性 (IC50 为 25 μg mL)。

CIL56 (CA3) 是一种选择性铁死亡诱导剂，可通过产生铁依赖性活性氧来诱导细胞铁死亡。

Ridaforolimus (AP23573) 是亲脂性大环内酯类抗生素雷帕霉素的小分子非前药类似物，具有潜在的抗肿瘤活性。它是一种有效和选择性的 mTOR 抑制剂，在 HT-1080 细胞中抑制 S6 磷酸化的 IC50值为 0.2 nM。

5'-Fluoroindirubinoxime (5'-FIO) 是一种 Indirubin 的衍生物，是一种 FLT3 的抑制剂(IC50:15 nM)。

SRS11-92 (AA9) 是一种铁死亡抑制剂和 Ferrostatin-1 的衍生物。它抑制 Erastin 诱导的 HT-1080 人纤维肉瘤细胞铁致细胞死亡，EC50为6 nM。

Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.1 Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC50s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft model in a dose-dependent manner. |1. Callmann, C.E., Leguyader, C.L.M., Burton, S.T., et al. Antitumor activity of 1,18-octadecanedioic acid-paclitaxel complexed with human serum albumin. J. Am. Chem. Soc. 141(30), 11765-11769 (2019).

Erastin2 是一种铁死亡诱导剂，通过与亲脂性自由基捕获抗氧化剂ferrostatin-1或铁螯合剂去铁胺（DFO）来诱导细胞死亡。

9,10-Dimethoxycanthin-6-one shows cytotoxic activity against a HT-1080 human fibrosarcoma cell line( IC50 = 5.0 microM).

Ferroptosis-IN-3（Compound 25）是一款抑制RSL3引起的铁死亡（HT-1080细胞中EC50为8.6nM）的铁死亡抑制剂。此外，Ferroptosis-IN-3能有效清除DPPH和ABTS自由基（EC50分别为3.94μM与6.3μM），并且能降低脂质过氧化水平。

PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM. PRLX-93936 inhibits tumor growth in PANC-1 and HT-1080 xenograft models when administered at a dose of 50 mg/kg and induces tumor regression when administered at a dose of 100 mg/kg.

CC-3060为Cereblon调节剂，专门促进ZBTB16蛋白的降解。在HT-1080细胞中，CC-3060的ZBTB16降解半数有效浓度（DC50）为0.47 nM。其主要机制是通过针对ZBTB16上的不同锌指结构域的异构结构实现靶向降解。

icFSP1是一种抑制剂，针对的是铁死亡抑制蛋白1（FSP1）。在2.5 µM的浓度下使用时，能够引发FSP1在细胞中的凝聚和相分离，但在无细胞测试中并不抑制FSP1的酶活性（IC50 = > 30 µM）。icFSP1以浓度依赖的方式诱导HT-1080纤维肉瘤细胞的铁死亡。在体内，icFSP1（50 mg/kg）通过使用人类过表达FSP1，Gpx4-/-Fsp1-/-的B16/F10细胞，在B16/F10鼠黑色素瘤模型中减少肿瘤体积和重量。

GPX4 24是(1S,3R)-RSL3的衍生物，具有抑制谷胱甘肽过氧化物酶4（GPX4）的作用。它能够在浓度依赖的方式中与4T1小鼠乳腺癌细胞中的GPX4形成共价结合。在GPX4依赖的HT-1080成纤维细胞中，GPX4 24诱导铁死亡（EC50 = 0.16 µM）。当以200 mg/kg剂量给予小鼠时，它能够增加小鼠肾脏和血浆中丙二醛（MDA）的水平。

DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2 M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14 tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated with DAT-230. Apoptosis induced by DAT-230 was related with the activation of caspase-9, caspase-3 and PARP cleavage, which were at the downstream of mitochondria.

Calyxin B exhibits potent activity against human HT-1080 fibrosarcoma cells with an ED50 value of 0.69 microM. A methylated product of calyxin A and an epimeric mixture of Calyxin B, showed greatly reduced activity suggesting that phenolic hydroxyl groups

Dihydroniloticin shows cytotoxic activity against a HT-1080 human fibrosarcoma cell line( IC50 = 8.2 microM).