Autophagy
信号通路图
研究领域
抑制剂选择性比较
Autophagy产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6716New |
NSC 185058NSC185058抑制ATG4B和自噬反应，而不影响mTOR或PtdIns3K信号通路。 |
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| S6471New |
LucanthoneLucanthone是新型的自噬抑制剂，也是可用于口服的DNA嵌入剂、DNA修复酶APE1的抑制剂。 |
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| S8793New |
ULK-101ULK-101是一种有效的、选择性的ULK1抑制剂，对ULK1和ULK2的IC50值分别为8.3 nM和30 nM。 |
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| S8807New |
PFK158PFK158是有效的、选择性PFKFB3抑制剂。它具有良好的药代动力学特性，在好几种接种有人源肿瘤的小鼠模型中，能引起约80%的肿瘤抑制作用。 |
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| S8808New |
DC661DC661是能够使溶酶体脱酸，显著抑制自噬（autophagy），比羟化氯喹（HCQ）更有效。 |
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| S8744New |
PHY34PHY34是一种自噬晚期（late-stage autophagy）抑制剂，具有纳摩尔级别的抑制效力，在体内对高级别浆液性卵巢癌（HGSOC）具有抗肿瘤活性。 |
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| S5920New |
CA-5fCA-5f是一种有效的自噬晚期（late-stage autophagy）抑制剂，通过抑制自噬体-溶酶体融合发挥作用。 |
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| S1105 |
LY294002LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。 |
Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
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| S1150 |
PaclitaxelPaclitaxel是一种microtubule聚合物稳定剂，在人内皮细胞中IC50为0.1 pM。 |
Microscope image (406) magnification of U937 cells after exposure to SM-TNs. a) Untreated U937 cells. b) U937 cells treated with 200 nM, and 35 nM ODS empty shells. c) U937 cells treated with microcrystalline (free) Taxol prepared by sonicating Taxol in 20%H3PO4/0.8% SDS solution. d) U937 cells treated with 200 nM SM-TN. A SM-TN is seen in the middle of the picture. e) U937 cells treated with 35 nM SMTN.The nanowires are too small to see at this magnification, but their effect on the cells is clearly visible. Scale bar = 10 mm. |
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| S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。也会抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。 |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
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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。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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| S2775 |
NocodazoleNocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50分别为0.21 μM， 0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率，对增强精确的基因编辑效力具有加成作用。 |
A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively. |
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| S4157 |
Chloroquine diphosphateChloroquine diphosphate是一种4-氨基喹啉的抗疟疾和抗风湿药，也是一种ATM激活剂。 |
NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
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| S1835 |
AzithromycinAzithromycin是一种抑制蛋白合成的抗生素，用于细菌感染的治疗。 |
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| S7289 |
PFK15PFK15 是一种强效的选择性的6-phosphofructo-2-kinase (PFKFB3)抑制剂，其IC50为207 nM。 |
b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays. |
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| S7885 |
SBI-0206965SBI-0206965是一种高度选择性自吞噬激酶ULK1抑制剂，IC50为108 nM，选择性比作用于ULK2高7倍。 |
Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, ** p < 0.01, *** p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05. |
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| S8576 |
EAD1EAD1是一种有效的自噬（autophagy）抑制剂，在BxPC3细胞中IC50为5.8 μM。它在肺癌和胰腺癌细胞中具有抗增殖活性。 |
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| S8764 |
IITZ-01IITZ-01是一种有效的自噬（autophagy）抑制剂，可增强自噬体的积累，但通过破坏溶酶体功能抑制自噬体的退化。 |
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| S7888 |
Spautin-1Spautin-1是一种有效的特异性autophagy抑制剂，抑制USP10 和 USP13的去泛素化活性，IC50为∼0.6-0.7 μM。 |
Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
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| S8317 |
3BDO3BDO是一种丁内酯衍生物，可靶向FKBP1A并激活mTOR信号通路，抑制HUVECs自噬。 |
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| S7811 |
MHY1485MHY1485是一种有效的，细胞渗透性 mTOR 激动剂，也能有效抑制 autophagy。 |
Exosomal miR-124-3p inhibited neuronal inflammation by suppressing the activity of mTOR signaling. A, B) Immunoblot (A) and quantitative (B) data of p-4E-BP1 and p-P70S6K in neurons after scratch injury and exosomal treatment. Their expression was increased after scratch injury and was suppressed by miR-124-3p–up-regulated exosomes, suggesting that miR-124-3p suppresses the activity of mTOR signaling (n = 6/group). ##P < 0.01 vs. control group; **P < 0.01 vs. injury group. C) Expression levels of inflammatory mediators in the culture medium were detected in the 3 groups of neurons: injured neurons (injury group), injured neurons treated with miR-124-3p–up-regulated exosomes (I+Exo-124), and injured neurons treated with miR-124-3p-up-regulated exosomes and the mTOR activator (MHY1485). Compared with the I+Exo-124 group, the MHY1485 group represented an increased expression on proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and a decreased expression of anti-inflammatory cytokines (IL-10), suggesting that MHY1485 blocks the anti-inflammatory effect of miR-124-3p in injured neurons. Thus, the inhibitory effect of exosomal miR-124-3p on neuronal inflammation was exerted by suppressing the activity of mTOR signaling (n = 6/group). #P < 0.05 vs. injury group; *P < 0.05 vs. I+Exo-124 group.
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| S8596 |
AutophinibAutophinib是有效的自噬 (autophagy)抑制剂，在饥饿诱导的自噬试验和rapamycin诱导的自噬试验中，其IC50分别为90 nM和40 nM。它还是Vps34的抑制剂，IC50为19 nM。 |
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| S3758 |
Sinomenine hydrochlorideSinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent. |
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| S8369 |
Lys05Lys05是一种新型的溶酶体自噬抑制剂，可有效地在细胞和肿瘤中的溶酶体中积累并降低溶酶体的酸度，从而导致发挥对自噬和肿瘤生长的持续抑制作用。 |
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| S4430 |
Hydroxychloroquine SulfateHydroxychloroquine Sulfate是一种抗疟疾药，用于治疗系统性红斑狼疮，类风湿关节炎等自身免疫病，炎症以及皮肤病。它也是autophagy和toll-like receptor (TLR) 7/9的抑制剂。 |
C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
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| S7949 |
MRT68921 HClMRT68921是一个高效的双重的自噬激酶ULK1/2抑制剂，其IC50分别为2.9 nM和1.1 nM。 |
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| S7683 |
PIK-IIIPIK-III, 一种选择性VPS34酶活性的抑制剂，抑制细胞自噬以及LC3的重新脂化，稳定自噬底物。其对VPS34和 PI(3)Kδ的IC50值分别为0.018 μM和1.2 μM。 |
LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm |
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| S8527 |
ROC-325ROC-325是具有口服活性的溶酶体介导的自噬抑制剂，可减少AML细胞的细胞活性，IC50范围为0.7-2.2 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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| S9150 |
DaurisolineDaurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects. |
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| S1047 |
Vorinostat (SAHA, MK0683)Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。 |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
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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。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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| S1049 |
Y-27632 2HClY-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂，无细胞试验中Ki为140 nM，比对其他激酶包括PKC，cAMP依赖性蛋白激酶，MLCK和PAK的作用强200多倍。 |
The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
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| S1039 |
Rapamycin (Sirolimus)Rapamycin (Sirolimus)是一种特定的 mTOR 抑制剂，在 HEK293细胞中，IC50 为 ~0.1 nM。 |
H4-LC3-GFP cells were treated with 1 nM IFNA2 for the indicated periods in the presence of 200 nM rapamycin. Images of the cells were collected using an ArrayScan HCS 4.0 Reader. Representative cells are shown. The average spot intensity in 500 cells from each indicated sample was determined. Data are displayed as means ?SD of the spot intensity per cell (below). RLU, relative leight unit.
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| S1023 |
Erlotinib HCl (OSI-744)Erlotinib HCl (OSI-744)是一种EGFR抑制剂，在无细胞试验中IC50为2 nM，对EGFR的选择性比对人c-Src或v-Abl高1000多倍。 |
Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone. |
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| S6650New |
EN6EN6是一种新型共价自噬激活剂，靶向溶酶体v-ATPase的ATP6V1A亚基中的半胱氨酸277，对重组人ATP6V1A蛋白的IC50为1.7μM。 |
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| S1057 |
Obatoclax Mesylate (GX15-070)Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，无细胞试验中Ki为0.22 μM，可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。 |
In vivo antitumor efficacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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| S1038 |
PI-103PI-103是一种多靶点 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50为 2 nM/3 nM/3 nM/15 nM，对 mTOR/DNA-PK的作用较小，IC50为30 nM/23 nM。 |
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
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| S1149 |
Gemcitabine HClGemcitabine HCl是一种DNA synthesis抑制剂，作用于PANC1，MIAPaCa2，BxPC3和Capan2细胞，IC50分别为50 nM， 40 nM， 18 nM和12 nM。 |
RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um. |
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| S2218 |
Torkinib (PP242)Torkinib (PP242)是一种选择性的mTOR抑制剂，在无细胞试验中IC50为8 nM；靶向作用于mTOR复合体，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。 |
Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs+24/44/ESA viability. CSCs+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.
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| S1237 |
TemozolomideTemozolomide(TMZ)是一种单功能的SN-1烷化剂，修饰DNA环上的氮原子以及环外氧基团。在生理pH值下，TMZ转化为活性产物MTIC、降解为methyldiazonium cation，后者再将甲基转移到DNA, 阻碍DNA复制启动，诱使细胞凋亡，是一种DNA损伤诱导剂。 |
C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).
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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。 |
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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| S1573 |
Fasudil (HA-1077) HClFasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。 |
The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
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| S1972 |
Tamoxifen CitrateTamoxifen Citrate是一种雌激素受体拮抗剂，通过竞争性抑制雌激素结合发挥作用。 |
Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells. |
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| S2827 |
Torin 1Torin 1是一种有效的mTORC1/2抑制剂，在无细胞试验中IC50为2 nM/10 nM；作用于mTOR比作用于PI3K选择性高1000倍。 |
Huh-7.5 cells were treated with increasing concentration of Torin 1, a known autophagy inducer, and the autophagy response was assessed by measuring LC3II and p62 levels.
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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。 |
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 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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| S1714 |
GemcitabineGemcitabine是核酸合成抑制剂，是有效、特异的脱氧胞苷类似物，用于化疗。 |
RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um. |
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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。 |
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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| S2713 |
GeldanamycinGeldanamycin是一种天然的HSP90抑制剂，Kd为1.2 μM，特异性干扰糖皮质激素受体（GR）/HSP联合。 |
Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
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| S2929 |
Pifithrin-α (PFTα) HBrPifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。 |
A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments. |
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| S3030 |
NiclosamideNiclosamide能够抑制DNA复制，并抑制STAT3，无细胞试验中IC50为0.7 μM。 Niclosamide 选择性地抑制STAT3的磷酸化，对其他同系物如STAT1和STAT5的激活没有明显抑制作用。 |
Effects of some confirmed hits on IRF7 transcription level in response to IFN-α2a treatment (1 h) in SH-SY5Y cells. Data represent mean expression fold±SEM relative to GAPDH, measured from three independent experiments, each in triplicates. *P<0.05, **P<0.01, and ***P<0.001 compared to IFN-α2a treated cells.
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| S1389 |
OmeprazoleOmeprazole 是一种质子泵抑制剂，用于治疗消化不良，消化性溃疡，胃食管逆流，咽喉逆流。 |
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| S1979 |
Amiodarone HClAmiodarone HCl是一种sodium/potassium-ATPase抑制剂同时也是自噬的激活剂，用于治疗各种心律失常。 |
Drugs across therapeutic indications induce lipid formation in hiPS-CM. Lipid accumulation was detected in cardiac cells using the LipidTox plate-based fluorescent assay on the Thermo Scientific CellInsight High Content platform. A) Ten drugs increased lipid levels in hiPS-CM following 48 h treatment. The lowest drug dose that induced a N1.5-fold increase in lipid formation is shown. B) Representative images (20×) from the assay are shown to the right. All drugs had >55% cell viability at 48 h at these tested concentrations. C) Of these 10 drugs, 8 significantly increased lipid accumulation following only 24 h treatment (images not shown). All drugs had >80% cell viability at 24 h at these drug doses. The graphs represent the mean fold-change of the lowest concentration of drug that significantly induced lipid formation >1.5-fold more than vehicle control. *P<0.05, **P<0.01, and ***P<0.0001.
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| S2480 |
Loperamide HClLoperamide HCl是一种阿片受体激动剂，ED50为0.15 mg/kg。 |
Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given. |
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| S4028 |
Dexamethasone Sodium PhosphateDexamethasone Sodium Phosphate是一种白介素受体抑制剂，抑制COX-2。 |
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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| S1693 |
CarbamazepineCarbamazepine 是一种钠离子通道抑制剂，作用于大鼠脑突触体时， IC50为131 μM。 |
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| S2458 |
Clonidine HClClonidine HCl 是一种直接起作用的α2肾上腺素能受体激动剂，ED50为0.02±0.01 mg/kg。 |
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| S1837 |
FlubendazoleFlubendazole 是一种驱虫剂，作用于MDAY-D2 细胞，IC50为3 nM。 |
Inhibitory curves and IC50 values for the reference compound flubendazole (B) against VEGFR2.
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| S1747 |
NimodipineNimodipine是一种二氢吡啶衍生物，是钙离子通道抑制剂Nifedipine的类似物，具有降压活性。Nimodipine能减少细胞内游离Ca2+，Beclin-1及细胞自噬。 |
Assessment of the role of Ca2+ channels during RSV replication. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with calcium channel blockers nifedipine, nimodipine, and tetrandrine (A), at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. NS, no differences at a significance level of 0.05. |
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| S3124 |
Dexamethasone AcetateDexamethasone 是一种有效的糖皮质激素类合成物，属于类固醇药物。Dexamethasone用于很多炎症和自身免疫病的治疗，例如风湿性关节炎和支气管痉挛。接受化疗的癌症病人服用dexamethasone去抵消部分化疗带来的副作用。Dexamethasone 也用在诊断方面，利用它能抑制垂体一肾上腺轴特性。 |
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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| S2491 |
NitrendipineNitrendipine是一种二氢吡啶类钙离子通道抑制剂，IC50为95 nM。 |
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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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| S8595 |
Tat-beclin 1 (Tat-BECN1)Tat-beclin 1 (Tat-BECN1)能够通过动员内源性Beclin 1刺激自噬，改善临床疗效。 |
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| S3653 |
Spermidine trihydrochlorideSpermidine是一种从腐胺和dcSAM中，通过亚精胺合成酶合成的天然聚胺。它是新型的自噬诱导剂，负向调控N-methyl-d-aspartate (NMDA)。 |
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| S9027 |
CorynoxineCorynoxine, a natural oxindole alkaloid, is a new autophagy enhancer. |
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| S4081 |
Sulfacetamide SodiumSulfacetamide Sodium是一种抗生素。 |
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| S8240 |
SMER28SMER28是一种细胞自噬的增强剂，可独立于雷帕霉素、在哺乳动物细胞中诱导细胞自噬。 |
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| S9310 |
IsorhychophyllineIsorhynchophylline is a major tetracyclic oxindole alkaloid isolated from the Chinese herbal medicine Uncaria rhynchophylla (Miq.)Jacks (Gouteng in Chinese). It acts as a neuronal autophagy inducer with therapeutic potential for cardiovascular and central nervous system diseases. |
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| S1238 |
TamoxifenTamoxifen作用于乳腺组织，是一种雌激素受体拮抗剂。 |
E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01. |
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| S8597 |
LYN-1604LYN-1604是一种潜在的ULK1激动剂，在MDA-MB-231细胞中IC50为1.66 μM。它能与野生型ULK1结合，Kd=291.4 nM。与突变型ULK1蛋白ULK1(Y89A)的结合亲和力急剧减小，其Kd值比ULK1、ULK1 (K50A)和ULK1 (L53A)大。 |
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| S1241 |
Vincristine sulfateVincristine sulfate通过与微管蛋白结合而抑制微管聚合，IC50为32 μM。 |
for HXO-RB44 cells, IC50 values for VCR were changed in the different SG600 treatment groups. The results are representative of three independent experiments and of f our replicates in each experiment. |
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| S1168 |
Valproic acid sodium salt (Sodium valproate)Valproic acid sodium salt (Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。 |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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| S1041 |
STF-62247STF-62247是一种靶向具有VHL缺陷的肾细胞癌的小分子化合物，诱导自噬。STF-62247对缺乏VHL的肾细胞具有选择毒性和抑制细胞生长作用;作用于VHL缺陷的细胞比作用于野生型(VHL+)选择性高25倍。 |
Columns depict relative densitometric values that were obtained by comparing with (β-actin. Presenilin 1, Nicastrin, and Pen-2 were increased with the 3-MA treatment (*P<0.001) while the other component of the γ-secretase complex (APH-1 and Presenilin 2) has no difference, compared with the STF-62247 treatment. Moreover, Bace1 and ADAM17 respectively had no difference between 3-MA and STF-62247 treatments. Both autophagy inhibitor and inducer activated α-, β-, and γ-secretases (*P<0.005). Abbreviations: Aβ, beta-amyloid; ADAM17, a disintegrin and metalloprotease 17; APH-1, anterior pharynx-defective 1; APP, amyloid protein precursor; Bace1, beta-site APP cleavage enzyme; 3-MA, 3-methyladenine; Con, control, LC3, microtubule-associated protein 1A/1B-light chain 3. |
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| S4750 |
Sulfacetamide sodium salt hydrateSulfacetamide是一种磺胺类抗生素，通过抑制dihydropteroate synthase(DHPS)阻滞二氢叶酸的合成。Sulfacetamide是细菌para-aminobenzoic acid (PABA)的竞争性抑制剂，PABA是细菌合成叶酸所必需的。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6716New |
NSC 185058NSC185058抑制ATG4B和自噬反应，而不影响mTOR或PtdIns3K信号通路。 |
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| S6471New |
LucanthoneLucanthone是新型的自噬抑制剂，也是可用于口服的DNA嵌入剂、DNA修复酶APE1的抑制剂。 |
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| S8793New |
ULK-101ULK-101是一种有效的、选择性的ULK1抑制剂，对ULK1和ULK2的IC50值分别为8.3 nM和30 nM。 |
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| S8807New |
PFK158PFK158是有效的、选择性PFKFB3抑制剂。它具有良好的药代动力学特性，在好几种接种有人源肿瘤的小鼠模型中，能引起约80%的肿瘤抑制作用。 |
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| S8808New |
DC661DC661是能够使溶酶体脱酸，显著抑制自噬（autophagy），比羟化氯喹（HCQ）更有效。 |
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| S8744New |
PHY34PHY34是一种自噬晚期（late-stage autophagy）抑制剂，具有纳摩尔级别的抑制效力，在体内对高级别浆液性卵巢癌（HGSOC）具有抗肿瘤活性。 |
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| S5920New |
CA-5fCA-5f是一种有效的自噬晚期（late-stage autophagy）抑制剂，通过抑制自噬体-溶酶体融合发挥作用。 |
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| S1105 |
LY294002LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。 |
Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
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| S1150 |
PaclitaxelPaclitaxel是一种microtubule聚合物稳定剂，在人内皮细胞中IC50为0.1 pM。 |
Microscope image (406) magnification of U937 cells after exposure to SM-TNs. a) Untreated U937 cells. b) U937 cells treated with 200 nM, and 35 nM ODS empty shells. c) U937 cells treated with microcrystalline (free) Taxol prepared by sonicating Taxol in 20%H3PO4/0.8% SDS solution. d) U937 cells treated with 200 nM SM-TN. A SM-TN is seen in the middle of the picture. e) U937 cells treated with 35 nM SMTN.The nanowires are too small to see at this magnification, but their effect on the cells is clearly visible. Scale bar = 10 mm. |
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| S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。也会抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。 |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
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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。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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| S2775 |
NocodazoleNocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50分别为0.21 μM， 0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率，对增强精确的基因编辑效力具有加成作用。 |
A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively. |
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| S4157 |
Chloroquine diphosphateChloroquine diphosphate是一种4-氨基喹啉的抗疟疾和抗风湿药，也是一种ATM激活剂。 |
NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
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| S1835 |
AzithromycinAzithromycin是一种抑制蛋白合成的抗生素，用于细菌感染的治疗。 |
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| S7289 |
PFK15PFK15 是一种强效的选择性的6-phosphofructo-2-kinase (PFKFB3)抑制剂，其IC50为207 nM。 |
b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays. |
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| S7885 |
SBI-0206965SBI-0206965是一种高度选择性自吞噬激酶ULK1抑制剂，IC50为108 nM，选择性比作用于ULK2高7倍。 |
Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, ** p < 0.01, *** p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05. |
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| S8576 |
EAD1EAD1是一种有效的自噬（autophagy）抑制剂，在BxPC3细胞中IC50为5.8 μM。它在肺癌和胰腺癌细胞中具有抗增殖活性。 |
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| S8764 |
IITZ-01IITZ-01是一种有效的自噬（autophagy）抑制剂，可增强自噬体的积累，但通过破坏溶酶体功能抑制自噬体的退化。 |
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| S7888 |
Spautin-1Spautin-1是一种有效的特异性autophagy抑制剂，抑制USP10 和 USP13的去泛素化活性，IC50为∼0.6-0.7 μM。 |
Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
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| S8317 |
3BDO3BDO是一种丁内酯衍生物，可靶向FKBP1A并激活mTOR信号通路，抑制HUVECs自噬。 |
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| S7811 |
MHY1485MHY1485是一种有效的，细胞渗透性 mTOR 激动剂，也能有效抑制 autophagy。 |
Exosomal miR-124-3p inhibited neuronal inflammation by suppressing the activity of mTOR signaling. A, B) Immunoblot (A) and quantitative (B) data of p-4E-BP1 and p-P70S6K in neurons after scratch injury and exosomal treatment. Their expression was increased after scratch injury and was suppressed by miR-124-3p–up-regulated exosomes, suggesting that miR-124-3p suppresses the activity of mTOR signaling (n = 6/group). ##P < 0.01 vs. control group; **P < 0.01 vs. injury group. C) Expression levels of inflammatory mediators in the culture medium were detected in the 3 groups of neurons: injured neurons (injury group), injured neurons treated with miR-124-3p–up-regulated exosomes (I+Exo-124), and injured neurons treated with miR-124-3p-up-regulated exosomes and the mTOR activator (MHY1485). Compared with the I+Exo-124 group, the MHY1485 group represented an increased expression on proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and a decreased expression of anti-inflammatory cytokines (IL-10), suggesting that MHY1485 blocks the anti-inflammatory effect of miR-124-3p in injured neurons. Thus, the inhibitory effect of exosomal miR-124-3p on neuronal inflammation was exerted by suppressing the activity of mTOR signaling (n = 6/group). #P < 0.05 vs. injury group; *P < 0.05 vs. I+Exo-124 group.
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| S8596 |
AutophinibAutophinib是有效的自噬 (autophagy)抑制剂，在饥饿诱导的自噬试验和rapamycin诱导的自噬试验中，其IC50分别为90 nM和40 nM。它还是Vps34的抑制剂，IC50为19 nM。 |
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| S3758 |
Sinomenine hydrochlorideSinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent. |
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| S8369 |
Lys05Lys05是一种新型的溶酶体自噬抑制剂，可有效地在细胞和肿瘤中的溶酶体中积累并降低溶酶体的酸度，从而导致发挥对自噬和肿瘤生长的持续抑制作用。 |
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| S4430 |
Hydroxychloroquine SulfateHydroxychloroquine Sulfate是一种抗疟疾药，用于治疗系统性红斑狼疮，类风湿关节炎等自身免疫病，炎症以及皮肤病。它也是autophagy和toll-like receptor (TLR) 7/9的抑制剂。 |
C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
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| S7949 |
MRT68921 HClMRT68921是一个高效的双重的自噬激酶ULK1/2抑制剂，其IC50分别为2.9 nM和1.1 nM。 |
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| S7683 |
PIK-IIIPIK-III, 一种选择性VPS34酶活性的抑制剂，抑制细胞自噬以及LC3的重新脂化，稳定自噬底物。其对VPS34和 PI(3)Kδ的IC50值分别为0.018 μM和1.2 μM。 |
LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm |
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| S8527 |
ROC-325ROC-325是具有口服活性的溶酶体介导的自噬抑制剂，可减少AML细胞的细胞活性，IC50范围为0.7-2.2 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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| S9150 |
DaurisolineDaurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects. |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1047 |
Vorinostat (SAHA, MK0683)Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。 |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
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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。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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| S1049 |
Y-27632 2HClY-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂，无细胞试验中Ki为140 nM，比对其他激酶包括PKC，cAMP依赖性蛋白激酶，MLCK和PAK的作用强200多倍。 |
The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
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| S1039 |
Rapamycin (Sirolimus)Rapamycin (Sirolimus)是一种特定的 mTOR 抑制剂，在 HEK293细胞中，IC50 为 ~0.1 nM。 |