erastin

Erastin 是一种作用于线粒体 VDAC 的铁死亡激活剂，具有 ROS 和铁依赖性。Erastin 具有抗肿瘤活性，选择性作用于 RAS 致癌突变的肿瘤细胞。

Levobupivacaine 是一种氨基酰胺类局麻药，属于n-alkylsubstituted pipecoloxylidide 家族。它是bupivacaine 的 S-对映异构体。

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是有效的钠通道阻滞剂。

Piperazine Erastin 是erastin 的类似物。它会导致一种铁依赖形式的非凋亡性细胞死亡，称为铁死亡。

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。

Imidazole ketone erastin (IKE) 是一种铁死亡诱导剂，对 system Xc-胱氨酸 谷氨酸转运蛋白具有抑制作用。Imidazole ketone erastin 具有抗肿瘤活性，可以诱导谷胱甘肽耗竭和脂质过氧化。

Noberastine (R 64947) 是一种新型组胺 H1拮抗剂，具有强效和特异性的外周抗组胺活性。

Cloperastine fendizoate (Hustazol) 是 hERG K+ 电流的抑制剂，IC50 为 27 nM。

Cloperastine hydrochloride (HT-11 hydrochloride) 是 hERG K+电流的抑制剂，IC50为 27 nM，具有浓度依赖性。

Perastine is a biochemical.

Noberastine citrate, a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.

Noberastine maleate, a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.

Esterastin is an Inhibitor of esterases.

Liproxstatin-1 是一种铁死亡抑制剂 (IC50=22 nM)，具有强效性和选择性。Liproxstatin-1 可以保护细胞免受铁死亡诱导剂 (如 Erastin、RSL3) 诱导的铁死亡。

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。

PRLX-93936 HCL 是 erastin 的类似物，并显示出与顺铂对非小细胞肺癌 (NSCLC) 细胞的协同作用。

1(R)-(Trifluoromethyl)oleyl alcohol is an analog of oleic acid .1It inhibits ferroptosis induced by erastin in primary fibroblasts isolated from patients with Friedreich ataxia, a neuro- and cardiodegenerative disorder characterized by loss or impaired activity of frataxin (FXN), when used at concentrations of 5, 10, or 20 μM. 1(R)-(Trifluoromethyl)oleyl alcohol (5 μM) reduces lipid peroxidation induced byFXNsiRNA knockdown in NBT human myoblasts. 1.Cotticelli, M.G., Forestieri, R., Xia, S., et al.Identification of a novel oleic acid analog with protective effects in multiple cellular models of Friedreich ataxiaACS Chem. Neurosci.11(17)2535-2542(2020)

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。

Ferroptosis-IN-11(compound 43)作为一种铁死亡 (ferroptosis) 抑制剂,能够有效抑制Erastin诱导的HT-1080人纤维细胞铁死亡,其EC50为36 nM.此化合物对于心血管疾病和神经退行性疾病的研究具有潜在应用价值.

Ferroptosis-IN-12（Cpd-A1）作为一种ferroptosis抑制剂，能有效抑制Erastin处理的小鼠肾小管上皮细胞（mTECs）中的ferroptosis。该化合物在缺血 再灌注（I R）或盲肠结扎穿刺（CLP）诱导的急性肾损伤（AKI）小鼠模型中显示出剂量依赖性的肾功能改善效果，能减轻肾小管损伤并消除炎症。在药代动力学的研究中，Ferroptosis-IN-12展示了良好的血浆稳定性和在肾脏组织中的高分布性。此外，Ferroptosis-IN-12在急性肾损伤（AKI）研究领域显示出应用潜力。

hMAO-B-IN-9(Compound 25c) 作为非竞争性单胺氧化酶 B (MAO-B) 抑制剂,展现IC50为1.58 µM (hMAO-B)的效力.此化合物与铁离子形成螯合复合物,有效抑制Erastin引发的铁死亡(ferroptosis),并通过降低活性氧(ROS)水平,发挥抗氧化作用.hMAO-B-IN-9 还能改善小鼠认知功能,同时在30 mg kg剂量下未见明显毒性.血脑屏障的通透性经计算机模拟预测表明,该化合物具备良好的穿透能力.

Pantothenate Kinase Inhibitor (PANKi) is a reversible inhibitor of pantothenate kinase (PanK; IC50s = 70, 92, and 25 nM for PanK1β, PanK2, and PanK3, respectively), the rate-limiting enzyme in the synthesis of coenzyme A .1It binds to the ATP-PanK3 complex with an apparent binding constant of 300 nM and exhibits mixed-type inhibition with respect to ATP and pantothenate. PANKi inhibits CoA biosynthesis in C3A cells (IC50= 0.9 μM) with no effect on cell viability when used at concentrations up to 8 μM. PANKi (5 μM) synergizes with BSO to induce ferroptosis in PANC-1 cells and sensitizes the cells to imidazole ketone erastin-induced ferroptosis.2 1.Sharma, L.K., Leonardi, R., Lin, W., et al.A high-throughput screen reveals new small-molecule activators and inhibitors of pantothenate kinasesJ. Med. Chem.58(3)1563-1568(2015) 2.Badgley, M.A., Kremer, D.M., Maurer, H.C., et al.Cysteine depletion induces pancreatic tumor ferroptosis in miceScience368(6486)85-89(2020)

SLC7A11-IN-2 (Compound 1) 是一种有效的SLC7A11 xCT抑制剂，通过下调细胞内谷胱甘肽水平并增加氧化应激来破坏 HeLa 细胞的氧化稳态，从而诱导细胞死亡，其 IC50 值为 10.23 μM。分子动力学模拟表明，该化合物的 SLC7A11 结合能力优于 Erastin。SLC7A11-IN-2 主要应用于宫颈癌的研究领域。

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.