Ferroptosis
抑制剂选择性比较
Ferroptosis产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1077 |
SB202190 (FHPI)SB202190 (FHPI)是一种有效的p38 MAPK抑制剂,靶向作用于p38α/β,无细胞试验中IC50为50 nM/100 nM,有时用于代替SB 203580研究其在体内对SAPK2a/p38的潜在作用。SB202190 可通过诱导自噬和血红素氧化酶1来抑制内皮细胞的凋亡。SB202190可显著抑制Erastin依赖的铁死亡ferroptosis。 |
![]() ![]() C, Jurkat cells with SB202190 at 1, 5, and 10 μM were tested, and a decreased SRP72 expression was found when using at 10 μM (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 μM at 240 versus 0 and 120 versus 0 min (p<0.05).
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S9840New |
SRS16-86SRS16-86 是一种新型的第三代 ferrostatin,是 ferroptosis 的抑制剂。 |
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S9839New |
SRS11-92SRS11-92 (AA9) 是一种 Ferrostatin-1 (Fer-1) 类似物,是一种有效的 ferroptosis 的抑制剂。SRS11-92 可抑制Erastin诱导的HT-1080人纤维肉瘤细胞的铁死亡,其EC50值为6 nM。 |
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S2505 |
Rosiglitazone (BRL-49653) maleateRosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药,是PPARγ的高亲和、选择性的激动剂,IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。 |
![]() ![]() Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast. |
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S2556 |
Rosiglitazone (BRL 49653)Rosiglitazone (BRL 49653) 是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。 |
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S8078 |
Bardoxolone MethylBardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。 |
![]() ![]() Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
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S3031 |
Linagliptin (BI-1356)Linagliptin (BI-1356)是一种高效的,选择性的DPP-4抑制剂,IC50为1 nM。对DPP-4的选择性比对其他二肽基肽酶类如DPP-2、DPP-8和DPP9高10,000倍以上。Linagliptin 在2型糖尿病模型中可激活血小球自噬。DPP4介导TP53缺陷的CRC细胞的铁死亡。 |
![]() ![]() Effect of linagliptin on oxidative stress in rat hearts suffered from 9 h of hypothermic preservation followed by 60 min of reperfusion. (A) Representative image of NOX2 detected by western blotting. (B). Densitometric analysis showing the expression of NOX2 using β‑actin for normalization. Data are mean ± S.E.M. (n = 3) and expressed as fold increase relative to the value of control group. (C-E) Measurement of MnSOD activity, ROS and MDA content. Data are expressed as mean ± S.E.M., n = 8. *P < 0.05, **P < 0.01 vs control group; #P < 0.05, ##P < 0.01 vs Celsior group. NOX2: NADPH oxidase 2; MnSOD: manganese superoxide dismutase; ROS: reactive oxygen species; MDA: malondialdehyde.
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S1623 |
Acetylcysteine (N-acetylcysteine)Acetylcysteine (N-acetyl-l-cysteine, NAC)是ROS抑制剂,拮抗多种蛋白酶体抑制剂的活性。它还是肿瘤坏死因子TNF的抑制剂,主要用作祛痰剂,可通过维持或恢复肝脏中谷胱甘肽的浓度来处理扑热息痛(对乙酰氨基酚过量)。Acetylcysteine(N-acetyl-l-cysteine) 通过抑制IκB kinases抑制TNF诱导的NF-κB活化。Acetylcysteine(N-acetyl-l-cysteine) 通过线粒体依赖性途径诱导凋亡并抑制铁死亡和病毒复制。现配现用。 |
![]() ![]() (C) Double immunolabeling showed CK-labeled cells (green) co-expressed with 40, 6-diamidino-2-phenylindole (DAPI) (blue), scale bars are 50 μm.
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S1848 |
CurcuminCurcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow)是流行的印度香料姜黄的主要姜黄色素,属于姜科(Zingiberaceae)。它是p300 histone acetylatransferase(IC50~25 μM)和Histone deacetylase (HDAC)的抑制剂,能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞,并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体(如流感病毒,丙型肝炎病毒,HIV等)具有抗感染特性。 |
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S1443 |
Zileuton (A-64077)Zileuton (A-64077, Abbott 64077, ZYFLO)是一种口服有效的5-脂氧合酶5-lipoxygenase抑制剂,从而抑制白三烯(LTB 4,LTC 4,LTD 4和LTE 4)的形成,用来缓解哮喘的症状。Zileuton 可诱导凋亡而抑制铁死亡。 |
![]() ![]() CD19+ B cells (A) or PBMCs (B) from a healthy donor were treated with zileuton (10 μM) prior to 17-HDHA or RvD1 treatment, followed by stimulation with the IgE-inducing cocktail. Cell culture supernatants were collected at day 7, and IgE levels were measured. The experiment was done in one representative donor (mean ± SEM). Data were analyzed by 1-way ANOVA with Tukey’s post test, **P ≤ 0.01, ***P ≤ 0.001. PBMC, peripheral blood mononuclear cell.
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S2046 |
Pioglitazone HClPioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂,对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。 |
![]() ![]() Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination. |
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S7243 |
Ferrostatin-1 (Fer-1)Ferrostatin-1 (Fer-1)是一种有效的选择性的ferroptosis抑制剂,EC50为60 nM。 |
![]() ![]() Indicated HCC cells were treated with sorafenib (5 µM) and erastin (10 µM) with or without cell death inhibitors (ferrostatin-1, 1 µM; liprostatin-1, 100nM; ZVAD-FMK,10 µM; necrosulfonamide, 0.5 µM) for 24 hours and cell viability was assayed (n=3, *p < 0.05 versus sorafenib or erastin treatment group).
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S3984 |
Nordihydroguaiaretic acid (NDGA)Nordihydroguaiaretic acid (NDGA)是一种天然存在的酚类防老剂。它是公认的脂肪氧合酶 lipoxygenase抑制剂,具有抗氧化、清除自由基的活性。Nordihydroguaiaretic acid (NDGA) 是一种具有细胞毒性的 insulin-like growth factor-I receptor (IGF-1R)/HER2 的抑制剂,可诱导细胞凋亡。Nordihydroguaiaretic acid (NDGA) 可抑制 p300 并激活自噬。Nordihydroguaiaretic acid (NDGA) 可保护细胞免于铁死亡。 |
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S7699 |
Liproxstatin-1Liproxstatin-1是一种有效的ferroptosis抑制剂,IC50为22 nM。 |
![]() ![]() (D) Indicated NRF2 knockdown HCC cells were treated with erastin (10 μM) and sorafenib (5 μM) with or without indicated inhibitors (ferrostatin-1, 1 μM; liproxstatin-1, 100 nM; ZVAD-FMK, 10 μM; necrostatin-1, 10 μM; necrosulfonamide, 0.5 μM) for 24 hours, and cell viability was assayed (n 5 3, *P < 0.05). Abbreviation: GAPDH, glyceraldehyde 3-phosphate dehydrogenase. |
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S8432 |
Troglitazone (CS-045)Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 是PPAR的有效激动剂,PPAR是配体激活的转录因,可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。 |
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S8792 |
UAMC-3203UAMC-3203是ferroptosis抑制剂,在IMR-32神经母细胞瘤细胞中IC50为10 nM。 |
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S7171 |
Setanaxib (GKT137831)Setanaxib (GKT137831, GKT831) 是一种有效的双NADPH oxidase NOX1/NOX4抑制剂,Ki分别为110 nM和140 nM。GKT137831 处理可抑制 reactive oxygen species (ROS) 的产生。GKT137831 可一定程度上抑制铁死亡。 |
![]() ![]() (C) Indicated macrophages were treated with LPS (100 ng/mL) in the absence or presence of GKT137831 (1 μmol/L) for 24 h. PKM2 mRNA and lactate levels were assayed (n = 3, *, p < 0.05 versus LPS group). |
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S5742 |
Deferoxamine mesylate (Ba 33112)Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468)是Deferoxamine的甲磺酸盐,它可形成铁络合物并用作螯合剂。Deferoxamine 是一种铁死亡的抑制剂,可在体外低氧和高血糖状态下稳定 HIF-1α 的表达并改善HIF-1α的活性。Deferoxamine 可降低 beta-amyloid (Aβ) 的沉积并诱导自噬。 |
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S1040 |
Sorafenib (BAY 43-9006) tosylateSorafenib (BAY 43-9006) tosylate是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib Tosylate 可诱导autophagy、apoptosis并激活ferroptosis,并具有抗肿瘤活性。 |
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Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells. |
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S1166 |
Cisplatin (NSC 119875)Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP)是一种无机铂络合物,在肿瘤细胞中能够通过形成DNA加合物抑制 DNA synthesis。Cisplatin 可激活ferroptosis并诱导autophagy。建议现配现用。 |
![]() ![]() Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05. |
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S1007 |
Roxadustat (FG-4592)Roxadustat (FG-4592)在无细胞试验中是一种HIF-α脯氨酰羟化酶抑制剂,并能稳定HIF-2,同时诱导EPO产生。Roxadustat可加强RSL3诱导的 ferroptosis。Phase 3。 |
![]() ![]() Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
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S2111 |
Lapatinib (GW-572016)Lapatinib (GW-572016, GSK572016, GW2016),以 Lapatinib Ditosylate的形式使用,是一种有效的EGFR和ErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。Lapatinib 可诱导 ferroptosis 和细胞自噬。 |
![]() ![]() Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies. |
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E0375New |
Ammonium ferric citrateAmmonium ferric citrate (Ferric ammonium citrate, Ammonium iron(III) citrate, Iron ammonium citrate, FerriSeltz) 通过抑制 GPX4-GSS/GSR-GGT 轴活性诱导非小细胞肺癌中的铁死亡。 |
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S1792 |
Simvastatin (MK 733)Simvastatin (MK-0733, MK 733)是一种HMG-CoA reductase竞争性抑制剂,无细胞试验中Ki为0.1-0.2 nM。Simvastatin可诱导铁死亡、线粒体自噬、细胞自噬和凋亡。 |
![]() ![]() Statin-Related Inhibition of Dehydroepiandrosterone Sulfate (DHEAS) Uptake by SLCO2B1 in Prostate Cancer (PC) Cells. B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated. C, Uptake of DHEAS in PC cells before (scrambled short hairpin RNA) and after (short hairpin RNA 2B1) SLCO2B1 is knocked down when incubated with 2.5 μM DHEAS and 100 μM atorvastatin for 10 and 60 minutes. Statistical analysis was performed by comparing each condition with scrambled short hairpin RNA after 10 minutes with DHEAS except when indicated. P = .02 for the comparison between scrambled short hairpin RNA with 10 vs 60 minutes of DHEAS incubation for LNCaP and .01 for 22RV1. Other P values are indicated in the figure. Bars indicate means and error bars indicate standard deviation. |
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S1712 |
Deferasirox (ICL-670)Deferasirox (ICL-670, CGP-72670)是一种铁螯合剂,是cytochrome P450 3A4诱导剂,Cytochrome P450 2C8的抑制剂,Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。 |
![]() ![]() U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox. |
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S7397 |
Sorafenib (BAY 43-9006)Sorafenib (BAY 43-9006, NSC-724772)是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib 可诱导autophagy、apoptosis并激活ferroptosis,Sorafenib 具有抗肿瘤活性。 |
![]() ![]() Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.
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S7242 |
ErastinErastin是一种ferroptosis激活剂,通过作用于线粒体VDAC而起作用,选择性作用于携带致癌基因RAS的肿瘤细胞。现配现用。 |
![]() ![]() Western blot analysis indicated protein expression in PDAC cells following treatment with erastin (2.5-40 μmol/L) for 24 hours (n=3, * P < 0.05 vs. untreated group) |
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S1576 |
Sulfasalazine (NSC 667219)Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)、TGF-β 和 COX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。 |
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S7309 |
BAY 87-2243BAY 87-2243 是一种有效的选择性hypoxia-inducible factor-1 (HIF-1)抑制剂。BAY 87-2243 可抑制 mitochondrial complex I 的活性,从而触发依赖线粒体的ROS升高,导致细胞坏死和铁死亡ferroptosis。BAY 87-2243 具有抗肿瘤活性。Phase 1。 |
![]() ![]() Cells were plated at low density, treated with the indicated compounds and scored for resistance. Abbreviations: osimertinib (Osi), phenformin (Phen), metformin (Met), buformin (Buf), BAY 87-2243 (BAY), oligomycin (Oligo).
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S0788 |
ML 210ML-210 (CID 49766530)是一种选择性的 glutathione peroxidase 4 (GPX4) 的共价抑制剂,其EC50值为0.04 μM,可诱导铁死亡。ML-210 可以选择性地杀死诱导表达突变型 RAS 的细胞,并具有抗癌活性。 |
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S8254 |
FIN56FIN56是ferroptosis的特异性诱导剂。 |
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S8155 |
RSL3RSL3 ((1S,3R)-RSL3)是一种ferroptosis的激活剂,不依赖于VDAC,对携带致瘤性RAS的肿瘤细胞具有选择性。它结合并使GPX4失活,介导GPX4所调节的铁死亡。 |
![]() ![]() (D) Representative western blot and (E) densitometry showing protein levels of HO-1 in HO-1+/+ PTCs treated with RSL3 over time. Data shown represent the Mean ± SEM of three independent experiments performed each time in triplicate; * = p<0.05, ** = p<0.01 compared to lower concentration at each time point. |
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S9663 |
iFSP1iFSP1 是一种有效的、选择性的且不依赖谷胱甘肽的 ferroptosis suppressor protein 1 (FSP1/AIFM2) 的抑制剂,EC50值为103 nM。iFSP1 可在过表达FSP1的GPX4基因敲除的Pfa1细胞和HT1080细胞中选择性诱导铁死亡。 |
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S4452 |
ML162ML162 是一种细胞磷脂 glutathione peroxidase (GPX-4) 的共价抑制剂,可诱导铁死亡。 |
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S8661 |
CA3 (CIL56)CA3 (CIL56) 对YAP1/Tead转录活性具有有效的抑制作用,主要靶向高表达YAP1、具有癌症干细胞属性的、难治疗的食管腺癌细胞。CA3(CIL56)可诱导铁死亡和铁依赖的活性氧自由基。 |
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S8790 |
ML385ML385是一种新型的、特异的NRF2抑制剂,IC50为1.9 μM。它能抑制NRF2的下游靶基因的表达。NRF2 可调节多种铁死亡和脂质过氧化相关蛋白的活性。 |
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S8877 |
Imidazole ketone erastin (PUN30119)Imidazole ketone erastin (PUN30119, IKE)是一种有效的、代谢稳定的、选择性system xc–抑制剂以及ferroptosis诱导剂。 |
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E1063New |
Piperazine ErastinPiperazine Erastin是Erastin的类似物,可诱导癌细胞的铁死亡,铁死亡是一种铁依赖的非凋亡细胞死亡形式。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1077 |
SB202190 (FHPI)SB202190 (FHPI)是一种有效的p38 MAPK抑制剂,靶向作用于p38α/β,无细胞试验中IC50为50 nM/100 nM,有时用于代替SB 203580研究其在体内对SAPK2a/p38的潜在作用。SB202190 可通过诱导自噬和血红素氧化酶1来抑制内皮细胞的凋亡。SB202190可显著抑制Erastin依赖的铁死亡ferroptosis。 |
![]() ![]() C, Jurkat cells with SB202190 at 1, 5, and 10 μM were tested, and a decreased SRP72 expression was found when using at 10 μM (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 μM at 240 versus 0 and 120 versus 0 min (p<0.05).
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S9840New |
SRS16-86SRS16-86 是一种新型的第三代 ferrostatin,是 ferroptosis 的抑制剂。 |
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S9839New |
SRS11-92SRS11-92 (AA9) 是一种 Ferrostatin-1 (Fer-1) 类似物,是一种有效的 ferroptosis 的抑制剂。SRS11-92 可抑制Erastin诱导的HT-1080人纤维肉瘤细胞的铁死亡,其EC50值为6 nM。 |
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S2505 |
Rosiglitazone (BRL-49653) maleateRosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药,是PPARγ的高亲和、选择性的激动剂,IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。 |
![]() ![]() Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast. |
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S2556 |
Rosiglitazone (BRL 49653)Rosiglitazone (BRL 49653) 是有效的降糖药,也是有效的噻唑烷二酮类胰岛素增敏剂,在大鼠,3T3-L1和人体脂肪细胞中IC50分别为12,4和9 nM。Rosiglitazone是PPAR-gamma的配体,对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。 |
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S8078 |
Bardoxolone MethylBardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。 |
![]() ![]() Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
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S3031 |
Linagliptin (BI-1356)Linagliptin (BI-1356)是一种高效的,选择性的DPP-4抑制剂,IC50为1 nM。对DPP-4的选择性比对其他二肽基肽酶类如DPP-2、DPP-8和DPP9高10,000倍以上。Linagliptin 在2型糖尿病模型中可激活血小球自噬。DPP4介导TP53缺陷的CRC细胞的铁死亡。 |
![]() ![]() Effect of linagliptin on oxidative stress in rat hearts suffered from 9 h of hypothermic preservation followed by 60 min of reperfusion. (A) Representative image of NOX2 detected by western blotting. (B). Densitometric analysis showing the expression of NOX2 using β‑actin for normalization. Data are mean ± S.E.M. (n = 3) and expressed as fold increase relative to the value of control group. (C-E) Measurement of MnSOD activity, ROS and MDA content. Data are expressed as mean ± S.E.M., n = 8. *P < 0.05, **P < 0.01 vs control group; #P < 0.05, ##P < 0.01 vs Celsior group. NOX2: NADPH oxidase 2; MnSOD: manganese superoxide dismutase; ROS: reactive oxygen species; MDA: malondialdehyde.
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S1623 |
Acetylcysteine (N-acetylcysteine)Acetylcysteine (N-acetyl-l-cysteine, NAC)是ROS抑制剂,拮抗多种蛋白酶体抑制剂的活性。它还是肿瘤坏死因子TNF的抑制剂,主要用作祛痰剂,可通过维持或恢复肝脏中谷胱甘肽的浓度来处理扑热息痛(对乙酰氨基酚过量)。Acetylcysteine(N-acetyl-l-cysteine) 通过抑制IκB kinases抑制TNF诱导的NF-κB活化。Acetylcysteine(N-acetyl-l-cysteine) 通过线粒体依赖性途径诱导凋亡并抑制铁死亡和病毒复制。现配现用。 |
![]() ![]() (C) Double immunolabeling showed CK-labeled cells (green) co-expressed with 40, 6-diamidino-2-phenylindole (DAPI) (blue), scale bars are 50 μm.
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S1848 |
CurcuminCurcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow)是流行的印度香料姜黄的主要姜黄色素,属于姜科(Zingiberaceae)。它是p300 histone acetylatransferase(IC50~25 μM)和Histone deacetylase (HDAC)的抑制剂,能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞,并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体(如流感病毒,丙型肝炎病毒,HIV等)具有抗感染特性。 |
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S1443 |
Zileuton (A-64077)Zileuton (A-64077, Abbott 64077, ZYFLO)是一种口服有效的5-脂氧合酶5-lipoxygenase抑制剂,从而抑制白三烯(LTB 4,LTC 4,LTD 4和LTE 4)的形成,用来缓解哮喘的症状。Zileuton 可诱导凋亡而抑制铁死亡。 |
![]() ![]() CD19+ B cells (A) or PBMCs (B) from a healthy donor were treated with zileuton (10 μM) prior to 17-HDHA or RvD1 treatment, followed by stimulation with the IgE-inducing cocktail. Cell culture supernatants were collected at day 7, and IgE levels were measured. The experiment was done in one representative donor (mean ± SEM). Data were analyzed by 1-way ANOVA with Tukey’s post test, **P ≤ 0.01, ***P ≤ 0.001. PBMC, peripheral blood mononuclear cell.
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S2046 |
Pioglitazone HClPioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂,对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。 |
![]() ![]() Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination. |
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S7243 |
Ferrostatin-1 (Fer-1)Ferrostatin-1 (Fer-1)是一种有效的选择性的ferroptosis抑制剂,EC50为60 nM。 |
![]() ![]() Indicated HCC cells were treated with sorafenib (5 µM) and erastin (10 µM) with or without cell death inhibitors (ferrostatin-1, 1 µM; liprostatin-1, 100nM; ZVAD-FMK,10 µM; necrosulfonamide, 0.5 µM) for 24 hours and cell viability was assayed (n=3, *p < 0.05 versus sorafenib or erastin treatment group).
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S3984 |
Nordihydroguaiaretic acid (NDGA)Nordihydroguaiaretic acid (NDGA)是一种天然存在的酚类防老剂。它是公认的脂肪氧合酶 lipoxygenase抑制剂,具有抗氧化、清除自由基的活性。Nordihydroguaiaretic acid (NDGA) 是一种具有细胞毒性的 insulin-like growth factor-I receptor (IGF-1R)/HER2 的抑制剂,可诱导细胞凋亡。Nordihydroguaiaretic acid (NDGA) 可抑制 p300 并激活自噬。Nordihydroguaiaretic acid (NDGA) 可保护细胞免于铁死亡。 |
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S7699 |
Liproxstatin-1Liproxstatin-1是一种有效的ferroptosis抑制剂,IC50为22 nM。 |
![]() ![]() (D) Indicated NRF2 knockdown HCC cells were treated with erastin (10 μM) and sorafenib (5 μM) with or without indicated inhibitors (ferrostatin-1, 1 μM; liproxstatin-1, 100 nM; ZVAD-FMK, 10 μM; necrostatin-1, 10 μM; necrosulfonamide, 0.5 μM) for 24 hours, and cell viability was assayed (n 5 3, *P < 0.05). Abbreviation: GAPDH, glyceraldehyde 3-phosphate dehydrogenase. |
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S8432 |
Troglitazone (CS-045)Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 是PPAR的有效激动剂,PPAR是配体激活的转录因,可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。 |
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S8792 |
UAMC-3203UAMC-3203是ferroptosis抑制剂,在IMR-32神经母细胞瘤细胞中IC50为10 nM。 |
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S7171 |
Setanaxib (GKT137831)Setanaxib (GKT137831, GKT831) 是一种有效的双NADPH oxidase NOX1/NOX4抑制剂,Ki分别为110 nM和140 nM。GKT137831 处理可抑制 reactive oxygen species (ROS) 的产生。GKT137831 可一定程度上抑制铁死亡。 |
![]() ![]() (C) Indicated macrophages were treated with LPS (100 ng/mL) in the absence or presence of GKT137831 (1 μmol/L) for 24 h. PKM2 mRNA and lactate levels were assayed (n = 3, *, p < 0.05 versus LPS group). |
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S5742 |
Deferoxamine mesylate (Ba 33112)Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468)是Deferoxamine的甲磺酸盐,它可形成铁络合物并用作螯合剂。Deferoxamine 是一种铁死亡的抑制剂,可在体外低氧和高血糖状态下稳定 HIF-1α 的表达并改善HIF-1α的活性。Deferoxamine 可降低 beta-amyloid (Aβ) 的沉积并诱导自噬。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1040 |
Sorafenib (BAY 43-9006) tosylateSorafenib (BAY 43-9006) tosylate是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib Tosylate 可诱导autophagy、apoptosis并激活ferroptosis,并具有抗肿瘤活性。 |
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Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells. |
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S1166 |
Cisplatin (NSC 119875)Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP)是一种无机铂络合物,在肿瘤细胞中能够通过形成DNA加合物抑制 DNA synthesis。Cisplatin 可激活ferroptosis并诱导autophagy。建议现配现用。 |
![]() ![]() Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05. |
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S1007 |
Roxadustat (FG-4592)Roxadustat (FG-4592)在无细胞试验中是一种HIF-α脯氨酰羟化酶抑制剂,并能稳定HIF-2,同时诱导EPO产生。Roxadustat可加强RSL3诱导的 ferroptosis。Phase 3。 |
![]() ![]() Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
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S2111 |
Lapatinib (GW-572016)Lapatinib (GW-572016, GSK572016, GW2016),以 Lapatinib Ditosylate的形式使用,是一种有效的EGFR和ErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。Lapatinib 可诱导 ferroptosis 和细胞自噬。 |
![]() ![]() Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies. |
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E0375New |
Ammonium ferric citrateAmmonium ferric citrate (Ferric ammonium citrate, Ammonium iron(III) citrate, Iron ammonium citrate, FerriSeltz) 通过抑制 GPX4-GSS/GSR-GGT 轴活性诱导非小细胞肺癌中的铁死亡。 |
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S1792 |
Simvastatin (MK 733)Simvastatin (MK-0733, MK 733)是一种HMG-CoA reductase竞争性抑制剂,无细胞试验中Ki为0.1-0.2 nM。Simvastatin可诱导铁死亡、线粒体自噬、细胞自噬和凋亡。 |
![]() ![]() Statin-Related Inhibition of Dehydroepiandrosterone Sulfate (DHEAS) Uptake by SLCO2B1 in Prostate Cancer (PC) Cells. B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated. C, Uptake of DHEAS in PC cells before (scrambled short hairpin RNA) and after (short hairpin RNA 2B1) SLCO2B1 is knocked down when incubated with 2.5 μM DHEAS and 100 μM atorvastatin for 10 and 60 minutes. Statistical analysis was performed by comparing each condition with scrambled short hairpin RNA after 10 minutes with DHEAS except when indicated. P = .02 for the comparison between scrambled short hairpin RNA with 10 vs 60 minutes of DHEAS incubation for LNCaP and .01 for 22RV1. Other P values are indicated in the figure. Bars indicate means and error bars indicate standard deviation. |
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S1712 |
Deferasirox (ICL-670)Deferasirox (ICL-670, CGP-72670)是一种铁螯合剂,是cytochrome P450 3A4诱导剂,Cytochrome P450 2C8的抑制剂,Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。 |
![]() ![]() U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox. |
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S7397 |
Sorafenib (BAY 43-9006)Sorafenib (BAY 43-9006, NSC-724772)是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib 可诱导autophagy、apoptosis并激活ferroptosis,Sorafenib 具有抗肿瘤活性。 |
![]() ![]() Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.
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S7242 |
ErastinErastin是一种ferroptosis激活剂,通过作用于线粒体VDAC而起作用,选择性作用于携带致癌基因RAS的肿瘤细胞。现配现用。 |
![]() ![]() Western blot analysis indicated protein expression in PDAC cells following treatment with erastin (2.5-40 μmol/L) for 24 hours (n=3, * P < 0.05 vs. untreated group) |
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S1576 |
Sulfasalazine (NSC 667219)Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)、TGF-β 和 COX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。 |
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S7309 |
BAY 87-2243BAY 87-2243 是一种有效的选择性hypoxia-inducible factor-1 (HIF-1)抑制剂。BAY 87-2243 可抑制 mitochondrial complex I 的活性,从而触发依赖线粒体的ROS升高,导致细胞坏死和铁死亡ferroptosis。BAY 87-2243 具有抗肿瘤活性。Phase 1。 |
![]() ![]() Cells were plated at low density, treated with the indicated compounds and scored for resistance. Abbreviations: osimertinib (Osi), phenformin (Phen), metformin (Met), buformin (Buf), BAY 87-2243 (BAY), oligomycin (Oligo).
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S0788 |
ML 210ML-210 (CID 49766530)是一种选择性的 glutathione peroxidase 4 (GPX4) 的共价抑制剂,其EC50值为0.04 μM,可诱导铁死亡。ML-210 可以选择性地杀死诱导表达突变型 RAS 的细胞,并具有抗癌活性。 |
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S8254 |
FIN56FIN56是ferroptosis的特异性诱导剂。 |
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S8155 |
RSL3RSL3 ((1S,3R)-RSL3)是一种ferroptosis的激活剂,不依赖于VDAC,对携带致瘤性RAS的肿瘤细胞具有选择性。它结合并使GPX4失活,介导GPX4所调节的铁死亡。 |
![]() ![]() (D) Representative western blot and (E) densitometry showing protein levels of HO-1 in HO-1+/+ PTCs treated with RSL3 over time. Data shown represent the Mean ± SEM of three independent experiments performed each time in triplicate; * = p<0.05, ** = p<0.01 compared to lower concentration at each time point. |
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S9663 |
iFSP1iFSP1 是一种有效的、选择性的且不依赖谷胱甘肽的 ferroptosis suppressor protein 1 (FSP1/AIFM2) 的抑制剂,EC50值为103 nM。iFSP1 可在过表达FSP1的GPX4基因敲除的Pfa1细胞和HT1080细胞中选择性诱导铁死亡。 |
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S4452 |
ML162ML162 是一种细胞磷脂 glutathione peroxidase (GPX-4) 的共价抑制剂,可诱导铁死亡。 |
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S8661 |
CA3 (CIL56)CA3 (CIL56) 对YAP1/Tead转录活性具有有效的抑制作用,主要靶向高表达YAP1、具有癌症干细胞属性的、难治疗的食管腺癌细胞。CA3(CIL56)可诱导铁死亡和铁依赖的活性氧自由基。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S8790 |
ML385ML385是一种新型的、特异的NRF2抑制剂,IC50为1.9 μM。它能抑制NRF2的下游靶基因的表达。NRF2 可调节多种铁死亡和脂质过氧化相关蛋白的活性。 |
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S8877 |
Imidazole ketone erastin (PUN30119)Imidazole ketone erastin (PUN30119, IKE)是一种有效的、代谢稳定的、选择性system xc–抑制剂以及ferroptosis诱导剂。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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E1063New |
Piperazine ErastinPiperazine Erastin是Erastin的类似物,可诱导癌细胞的铁死亡,铁死亡是一种铁依赖的非凋亡细胞死亡形式。 |