Mitophagy
抑制剂选择性比较
Mitophagy产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1102 |
U0126-EtOHU0126-EtOH是一种高度选择性的MEK1/2抑制剂，无细胞试验中IC50为0.07 μM/0.06 μM，作用于ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。U0126可抑制细胞自噬和线粒体自噬并具有抗病毒的活性。 |
Cells were stimulated with TPA (10 nM) for 15 min in the presence of the indicated concentrations of U0126. Samples were collected and analyzed by Western blot to detect phosphorylated p42/p44 MAPK. |
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| S2767 |
3-Methyladenine (3-MA)3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。3-Methyladenine (3-MA)可成功应用于抑制线粒体自噬。现配现用（加热助溶）。 |
granulosa cells (GCs) with 24 h of melatonin (10 μM) treatment were rinsed in PBS, and then exposed to H2O2 (200 μM) for 2 h. The autophagy inhibitor 3-MA (10 mM), or the apoptosis inhibitor Z-VAD-FMK (50 μM) were added 1 h prior to H2O2 incubation. Cell viability was determined using the CCK-8 assay. Data represent mean ± S.E; n = 3 in each group. *P < 0.05 (**P < 0.01) vs. vehicle group at 0 h. # Represents P < 0.05 (## Represents P < 0.01) vs. H2O2-only-treated cells. & Represents P > 0.05 vs. H2O2-only-treated cells. N, not significant, P > 0.05. δ Represents P < 0.05 (δδ Represents P < 0.01) vs. Z-VAD-FMK-treated cells.
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| S7046 |
Brefeldin ABrefeldin A 作用于HCT 116细胞，抑制内酯抗生素和ATPase，作用于protein transport（蛋白转运），IC50为0.2 μM，诱导癌细胞分化和凋亡。它还能提高同源重组修复效率，是CRISPR-mediated HDR的增强剂。Brefeldin A 也是自噬和线粒体自噬的抑制剂。 |
Cells were treated with brefeldin A or manumycin A, and the resulting supernatant was collected after 48 h for exosomal preparation (lanes 1 and 2), or exosomes obtained from C81 cells were trypsin-treated or freeze/thawed (F/T) and then trypsin-treated (lanes 3 and 4). Lanes 5 and 6, input exosome controls from C81 or CEM cells, respectively. Resulting exosomes were assayed for the presence of Tax by Western blotting. |
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| S1759 |
Pitavastatin CalciumPitavastatin Calcium，一种新型的Statins类药物，是pitavastatin的钙盐形式。Pitavastatin是高效的HMG-CoA reductase抑制剂。Pitavastatin Calcium 可通过抑制 ROS 的生成而减弱AGEs诱导的线粒体自噬。Pitavastatin Calcium 可诱导自噬和凋亡。 |
Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.
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| S7162 |
Mdivi-1Mdivi-1 是一个具有选择性和细胞穿膜性的线粒体分裂抑制剂，抑制了DRP1（发动蛋白相关GTP酶）和Dynamin I (Dnm1)的IC50为1-10 μM。Mdivi-1 可减少线粒体自噬而增加细胞凋亡。 |
a Representative TUNEL/DAPI photomicrographs of ipsilateral cortex in different groups (scale bar = 100 μm). |
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| S9424 |
Liensinine diperchlorateLiensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor. |
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| S1060 |
Olaparib (AZD2281)Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。在BRCA突变的细胞中，Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。 |
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. A) Cells were pre-treated +/- 1 uM olaparib (2h) then sequentially +/- 150nM PTX (24h) then +/- GMX 12nM (48h). Cells were harvested for (left) NAD+ quantification by LC-MS/MS (mean +/-SD of quadruplicates) or (right) viability by CellTiter-Glo (mean +/-SD of duplicates) B) PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A) by western blotting.
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| S1002 |
ABT-737ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-w，无细胞试验中EC50分别为78.7 nM，30.3 nM和197.8 nM；但对Mcl-1， Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。 |
Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown. |
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| S1378 |
Ruxolitinib (INCB018424)Ruxolitinib (INCB018424)是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.
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| S1042 |
Sunitinib MalateSunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，在无细胞试验中IC50分别为80 nM 和2 nM，也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 |
Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading. |
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| S1076 |
SB203580SB203580 是一种p38 MAPK抑制剂，在THP-1细胞中IC50为0.3-0.5 μM，对SAPK3(106T)和SAPK4(106T)选择性低10倍，且阻断PKB磷酸化，IC50为3-5 μM。SB203580 可诱导线粒体自噬和细胞自噬。 |
A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
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| S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin) HCl是一种抗生素类试剂，可抑制DNA topoisomerase II，并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗，但是在免疫治疗中有将HBV重活化的风险。 |
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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| S1141 |
Tanespimycin (17-AAG)Tanespimycin (17-AAG)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 2。 |
SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
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| S1225 |
EtoposideEtoposide是一种鬼臼毒素的半合成衍生物，通过抑制topoisomerase II 活性而抑制DNA合成。Etoposide可诱导自噬、线粒体自噬和细胞凋亡。 |
Cellular biomarker responses in HT29 cells exposed to various cytotoxic chemotherapeutic agents in combination with the Chk1 inhibitor V158411. HT29 cells were exposed to the combination GI80 of gemcitabine (0.2 uM), camptothecin (0.44 uM), cisplatin (68 uM), oxaliplatin (131 uM), doxorubicin (1.2 uM) or etoposide (59 uM) for 18 hours followed by DMSO (-) or 400 nM V158411 (+) for a further 24 hours. Protein expression was characterized by immunoblotting.
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| S2730 |
Crenolanib (CP-868596)Crenolanib (CP-868596)是一种有效的，选择性PDGFRα/β抑制剂，在CHO细胞中Kd为2.1 nM/3.2 nM，也能有效抑制FLT3，对D842V突变型敏感对V561D突变型不敏感，作用于PDGFR比作用于c-Kit，VEGFR-2，TIE-2，FGFR-2，EGFR，erbB2，和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。 |
Western blot analysis using 4G10 and anti-FLT3 antibody after immunoprecipitation with anti-FLT3 antibody and Western blot analysis of phospho-ERK (pERK) and ERK performed on whole cell lysates from HB119 and Molm14 cells. Cells were exposed to 100 nM crenolanib for 60 min.
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| S1950 |
Metformin HClMetformin HCl 降低肝细胞中高血糖症，主要通过抑制肝糖原的产生（肝脏糖异生作用)发挥作用。Metformin可促进单核细胞中的线粒体自噬。Metformin可通过激活JNK/p38 MAPK 信号通路和GAD153来诱导肺癌细胞系的凋亡。 |
Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
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| S1802 |
AICAR (Acadesine)AICAR (Acadesine)是AMPK的激活剂，引起ZMP积累，模拟AMP对AMPK和AMPKK的刺激作用。AICAR (Acadesine)可诱导线粒体自噬。Phase 3。 |
Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. *P < 0.05, **P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4). |
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| S1396 |
ResveratrolResveratrol具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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| S1322 |
DexamethasoneDexamethasone 是一种有效的半合成的糖皮质激素类甾体药物，也是一种interleukin receptor调节剂，具有抗炎和免疫抑制作用。Dexamethasone 可诱导自噬和线粒体自噬。Dexamethasone 被用于COVID-19临床病人测试中，并发现对危重症患者有一定效果。 |
Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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| S1792 |
SimvastatinSimvastatin 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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| S1204 |
MelatoninMelatonin 是一种 MT receptor 激动剂激素, 用作膳食补充品。Melatonin 是一种选择性的 ATF-6 的抑制剂并可下调 COX-2。Melatonin 可增强线粒体自噬并调节凋亡和自噬的稳态。 |
TUNEL staining of treated adipocytes and flow cytometry analysis of positive TUNEL cells (n=3). |
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| S3017 |
AspirinAspirin 是水杨酸类不可逆的COX1 and COX2抑制剂，常用作止痛药来缓解轻微疼痛，作为解热药减少发热，并作为一种抗炎药物。Aspirin 可诱导自噬并激发线粒体自噬。 |
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| S5312 |
Urolithin AUrolithin A, a metabolite of ellagitannin, is a first-in-class natural compound that induces mitophagy both in vitro and in vivo following oral consumption. |
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| S5243 |
Ruxolitinib PhosphateRuxolitinib Phosphate是Ruxolitinib的磷酸盐形式。Ruxolitinib 是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
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| S2348 |
Rotenone (Barbasco)Rotenone 是一种植物杀虫剂，是线粒体电子传递mitochondrial electron transport的抑制剂。Rotenone 可抑制 NADH/DB oxidoreductase 和 NADH oxidase，对应的IC50值分别为28.8 nM和5.1 nM。Rotenone 可通过增强线粒体活性氧的产生来诱导凋亡。 |
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| S2396 |
SalidrosideSalidroside 是一种糖苷类化合物，作用于SACC-2细胞增殖，IC50为4.99±0.23 μg/mL。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1102 |
U0126-EtOHU0126-EtOH是一种高度选择性的MEK1/2抑制剂，无细胞试验中IC50为0.07 μM/0.06 μM，作用于ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。U0126可抑制细胞自噬和线粒体自噬并具有抗病毒的活性。 |
Cells were stimulated with TPA (10 nM) for 15 min in the presence of the indicated concentrations of U0126. Samples were collected and analyzed by Western blot to detect phosphorylated p42/p44 MAPK. |
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| S2767 |
3-Methyladenine (3-MA)3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。3-Methyladenine (3-MA)可成功应用于抑制线粒体自噬。现配现用（加热助溶）。 |
granulosa cells (GCs) with 24 h of melatonin (10 μM) treatment were rinsed in PBS, and then exposed to H2O2 (200 μM) for 2 h. The autophagy inhibitor 3-MA (10 mM), or the apoptosis inhibitor Z-VAD-FMK (50 μM) were added 1 h prior to H2O2 incubation. Cell viability was determined using the CCK-8 assay. Data represent mean ± S.E; n = 3 in each group. *P < 0.05 (**P < 0.01) vs. vehicle group at 0 h. # Represents P < 0.05 (## Represents P < 0.01) vs. H2O2-only-treated cells. & Represents P > 0.05 vs. H2O2-only-treated cells. N, not significant, P > 0.05. δ Represents P < 0.05 (δδ Represents P < 0.01) vs. Z-VAD-FMK-treated cells.
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| S7046 |
Brefeldin ABrefeldin A 作用于HCT 116细胞，抑制内酯抗生素和ATPase，作用于protein transport（蛋白转运），IC50为0.2 μM，诱导癌细胞分化和凋亡。它还能提高同源重组修复效率，是CRISPR-mediated HDR的增强剂。Brefeldin A 也是自噬和线粒体自噬的抑制剂。 |
Cells were treated with brefeldin A or manumycin A, and the resulting supernatant was collected after 48 h for exosomal preparation (lanes 1 and 2), or exosomes obtained from C81 cells were trypsin-treated or freeze/thawed (F/T) and then trypsin-treated (lanes 3 and 4). Lanes 5 and 6, input exosome controls from C81 or CEM cells, respectively. Resulting exosomes were assayed for the presence of Tax by Western blotting. |
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| S1759 |
Pitavastatin CalciumPitavastatin Calcium，一种新型的Statins类药物，是pitavastatin的钙盐形式。Pitavastatin是高效的HMG-CoA reductase抑制剂。Pitavastatin Calcium 可通过抑制 ROS 的生成而减弱AGEs诱导的线粒体自噬。Pitavastatin Calcium 可诱导自噬和凋亡。 |
Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.
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| S7162 |
Mdivi-1Mdivi-1 是一个具有选择性和细胞穿膜性的线粒体分裂抑制剂，抑制了DRP1（发动蛋白相关GTP酶）和Dynamin I (Dnm1)的IC50为1-10 μM。Mdivi-1 可减少线粒体自噬而增加细胞凋亡。 |
a Representative TUNEL/DAPI photomicrographs of ipsilateral cortex in different groups (scale bar = 100 μm). |
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| S9424 |
Liensinine diperchlorateLiensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1060 |
Olaparib (AZD2281)Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。在BRCA突变的细胞中，Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。 |
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. A) Cells were pre-treated +/- 1 uM olaparib (2h) then sequentially +/- 150nM PTX (24h) then +/- GMX 12nM (48h). Cells were harvested for (left) NAD+ quantification by LC-MS/MS (mean +/-SD of quadruplicates) or (right) viability by CellTiter-Glo (mean +/-SD of duplicates) B) PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A) by western blotting.
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| S1002 |
ABT-737ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-w，无细胞试验中EC50分别为78.7 nM，30.3 nM和197.8 nM；但对Mcl-1， Bcl-B及Bfl-1没有抑制作用。ABT-737可诱导线粒体通路的凋亡和线粒体自噬。Phase 2。 |
Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown. |
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| S1378 |
Ruxolitinib (INCB018424)Ruxolitinib (INCB018424)是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.
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| S1042 |
Sunitinib MalateSunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，在无细胞试验中IC50分别为80 nM 和2 nM，也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 |
Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading. |
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| S1076 |
SB203580SB203580 是一种p38 MAPK抑制剂，在THP-1细胞中IC50为0.3-0.5 μM，对SAPK3(106T)和SAPK4(106T)选择性低10倍，且阻断PKB磷酸化，IC50为3-5 μM。SB203580 可诱导线粒体自噬和细胞自噬。 |
A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
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| S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin) HCl是一种抗生素类试剂，可抑制DNA topoisomerase II，并在肿瘤细胞中诱导DNA损伤、线粒体自噬和凋亡。Doxorubicin 可降低 AMPK的基础磷酸化。Doxorubicin 可应用于HIV感染病人的联合治疗，但是在免疫治疗中有将HBV重活化的风险。 |
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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| S1141 |
Tanespimycin (17-AAG)Tanespimycin (17-AAG)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 2。 |
SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
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| S1225 |
EtoposideEtoposide是一种鬼臼毒素的半合成衍生物，通过抑制topoisomerase II 活性而抑制DNA合成。Etoposide可诱导自噬、线粒体自噬和细胞凋亡。 |
Cellular biomarker responses in HT29 cells exposed to various cytotoxic chemotherapeutic agents in combination with the Chk1 inhibitor V158411. HT29 cells were exposed to the combination GI80 of gemcitabine (0.2 uM), camptothecin (0.44 uM), cisplatin (68 uM), oxaliplatin (131 uM), doxorubicin (1.2 uM) or etoposide (59 uM) for 18 hours followed by DMSO (-) or 400 nM V158411 (+) for a further 24 hours. Protein expression was characterized by immunoblotting.
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| S2730 |
Crenolanib (CP-868596)Crenolanib (CP-868596)是一种有效的，选择性PDGFRα/β抑制剂，在CHO细胞中Kd为2.1 nM/3.2 nM，也能有效抑制FLT3，对D842V突变型敏感对V561D突变型不敏感，作用于PDGFR比作用于c-Kit，VEGFR-2，TIE-2，FGFR-2，EGFR，erbB2，和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。 |
Western blot analysis using 4G10 and anti-FLT3 antibody after immunoprecipitation with anti-FLT3 antibody and Western blot analysis of phospho-ERK (pERK) and ERK performed on whole cell lysates from HB119 and Molm14 cells. Cells were exposed to 100 nM crenolanib for 60 min.
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| S1950 |
Metformin HClMetformin HCl 降低肝细胞中高血糖症，主要通过抑制肝糖原的产生（肝脏糖异生作用)发挥作用。Metformin可促进单核细胞中的线粒体自噬。Metformin可通过激活JNK/p38 MAPK 信号通路和GAD153来诱导肺癌细胞系的凋亡。 |
Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
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| S1802 |
AICAR (Acadesine)AICAR (Acadesine)是AMPK的激活剂，引起ZMP积累，模拟AMP对AMPK和AMPKK的刺激作用。AICAR (Acadesine)可诱导线粒体自噬。Phase 3。 |
Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. *P < 0.05, **P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4). |
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| S1396 |
ResveratrolResveratrol具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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| S1322 |
DexamethasoneDexamethasone 是一种有效的半合成的糖皮质激素类甾体药物，也是一种interleukin receptor调节剂，具有抗炎和免疫抑制作用。Dexamethasone 可诱导自噬和线粒体自噬。Dexamethasone 被用于COVID-19临床病人测试中，并发现对危重症患者有一定效果。 |
Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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| S1792 |
SimvastatinSimvastatin 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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| S1204 |
MelatoninMelatonin 是一种 MT receptor 激动剂激素, 用作膳食补充品。Melatonin 是一种选择性的 ATF-6 的抑制剂并可下调 COX-2。Melatonin 可增强线粒体自噬并调节凋亡和自噬的稳态。 |
TUNEL staining of treated adipocytes and flow cytometry analysis of positive TUNEL cells (n=3). |
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| S3017 |
AspirinAspirin 是水杨酸类不可逆的COX1 and COX2抑制剂，常用作止痛药来缓解轻微疼痛，作为解热药减少发热，并作为一种抗炎药物。Aspirin 可诱导自噬并激发线粒体自噬。 |
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| S5312 |
Urolithin AUrolithin A, a metabolite of ellagitannin, is a first-in-class natural compound that induces mitophagy both in vitro and in vivo following oral consumption. |
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| S5243 |
Ruxolitinib PhosphateRuxolitinib Phosphate是Ruxolitinib的磷酸盐形式。Ruxolitinib 是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
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| S2348 |
Rotenone (Barbasco)Rotenone 是一种植物杀虫剂，是线粒体电子传递mitochondrial electron transport的抑制剂。Rotenone 可抑制 NADH/DB oxidoreductase 和 NADH oxidase，对应的IC50值分别为28.8 nM和5.1 nM。Rotenone 可通过增强线粒体活性氧的产生来诱导凋亡。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2396 |
SalidrosideSalidroside 是一种糖苷类化合物，作用于SACC-2细胞增殖，IC50为4.99±0.23 μg/mL。 |
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