Autophagy
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1013 | Bortezomib (PS-341) | <1 mg/mL | 76 mg/mL | <1 mg/mL |
| S6851 | RA-190 | <1 mg/mL | 100 mg/mL | '20 mg/mL |
| S8943 | VLX600 | ˂1 mg/mL | 13 mg/mL | ˂1 mg/mL |
| S6716 | NSC 185058 | <1 mg/mL | 43 mg/mL | 21 mg/mL |
| S7455 | Resatorvid (TAK-242) | <1 mg/mL | 72 mg/mL | '72 mg/mL |
| S1109 | BI 2536 | <1 mg/mL | 21 mg/mL | '100 mg/mL |
| S1105 | LY294002 | <1 mg/mL | 36 mg/mL | 21 mg/mL |
| S1092 | KU-55933 (ATM Kinase Inhibitor) | <1 mg/mL | 33 mg/mL | ''<1 mg/mL |
| S1102 | U0126-EtOH | <1 mg/mL | 85 mg/mL | ''<1 mg/mL |
| S1150 | Paclitaxel | <1 mg/mL | 171 mg/mL | '18 mg/mL |
| S1460 | SP600125 | <1 mg/mL | 44 mg/mL | '<1 mg/mL |
| S1490 | Ponatinib (AP24534) | <1 mg/mL | 30 mg/mL | '<1 mg/mL |
| S1113 | GSK690693 | <1 mg/mL | 39 mg/mL | ''<1 mg/mL |
| S2758 | Wortmannin | <1 mg/mL | 85 mg/mL | '<1 mg/mL |
| S2704 | LY2109761 | <1 mg/mL | 2 mg/mL | '<1 mg/mL |
| S2767 | 3-Methyladenine (3-MA) | 10 mg/mL | 3 mg/mL | '4 mg/mL |
| S2243 | Degrasyn (WP1130) | <1 mg/mL | 77 mg/mL | '18 mg/mL |
| S1786 | Verteporfin | <1 mg/mL | 100 mg/mL | ''<1 mg/mL |
| S7046 | Brefeldin A | <1 mg/mL | 4 mg/mL | '<1 mg/mL |
| S8037 | Necrostatin-1 | <1 mg/mL | 51 mg/mL | ''<1 mg/mL |
| S2775 | Nocodazole | <1 mg/mL | 7 mg/mL | <1 mg/mL |
| S3042 | Purmorphamine | <1 mg/mL | 4 mg/mL | '<1 mg/mL |
| S4157 | Chloroquine Phosphate | 100 mg/mL | <1 mg/mL | '''<1 mg/mL |
| S1413 | Bafilomycin A1(Baf-A1) | <1 mg/mL | 6 mg/mL | '<1 mg/mL |
| S1835 | Azithromycin | <1 mg/mL | 100 mg/mL | '100 mg/mL |
| S8808 | DC661 | <1 mg/mL | 62 mg/mL | '49 mg/mL |
| S7289 | PFK15 | <1 mg/mL | 19 mg/mL | 2 mg/mL |
| S7885 | SBI-0206965 | <1 mg/mL | 97 mg/mL | '10 mg/mL |
| S8576 | EAD1 | 100 mg/mL | 100 mg/mL | 100 mg/mL |
| S8764 | IITZ-01 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7888 | Spautin-1 | <1 mg/mL | 54 mg/mL | ''7 mg/mL |
| S8317 | 3BDO | <1 mg/mL | 65 mg/mL | '49 mg/mL |
| S7811 | MHY1485 | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S8596 | Autophinib | <1 mg/mL | 69 mg/mL | <1 mg/mL |
| S7423 | KN-93 Phosphate | 92 mg/mL | 100 mg/mL | '<1 mg/mL |
| S8807 | PFK158 | ˂1 mg/mL | 14 mg/mL | 4 mg/mL |
| S3758 | Cucoline hydrochloride, Kukoline hydrochloride, Sabianine A hydrochloride | -1 mg/mL | 73 mg/mL | -1 mg/mL |
| S8369 | Lys05 | 3 mg/mL | 9 mg/mL | <1 mg/mL |
| S7660 | Obeticholic Acid | <1 mg/mL | 84 mg/mL | '84 mg/mL |
| S4430 | Hydroxychloroquine Sulfate | 67 mg/mL | <1 mg/mL | '<1 mg/mL |
| S7949 | MRT68921 HCl | <1 mg/mL | <1 mg/mL | '<1 mg/mL |
| S8744 | PHY34 | <1 mg/mL | 100 mg/mL | 42 mg/mL |
| S5920 | CA-5f | <1 mg/mL | 78 mg/mL | <1 mg/mL |
| S7683 | PIK-III | <1 mg/mL | 63 mg/mL | 63 mg/mL |
| S8793 | ULK-101 | <1 mg/mL | 92 mg/mL | '''<1 mg/mL |
| S8527 | ROC-325 | <1 mg/mL | 4 mg/mL | 4 mg/mL |
| S9424 | Liensinine diperchlorate | -1 mg/mL | 50 mg/mL | -1 mg/mL |
| S6471 | Lucanthone | <1 mg/mL | 33 mg/mL | 68 mg/mL |
| S9150 | Daurisoline | -1 mg/mL | 64 mg/mL | -1 mg/mL |
| S1078 | MK-2206 2HCl | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S1060 | Olaparib (AZD2281) | 0.002 mg/mL | 86 mg/mL | <1 mg/mL |
| S1267 | Vemurafenib (PLX4032) | <1 mg/mL | 97 mg/mL | <1 mg/mL |
| S1047 | Vorinostat (SAHA) | <1 mg/mL | 52 mg/mL | '3 mg/mL |
| S6797 | QX77 | <1 mg/mL | 60 mg/mL | <1 mg/mL |
| S6650 | EN6 | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S1002 | ABT-737 | <1 mg/mL | 100 mg/mL | '<1 mg/mL |
| S1049 | Y-27632 2HCl | 14 mg/mL | 64 mg/mL | '<1 mg/mL |
| S2619 | MG-132 | <1 mg/mL | 90 mg/mL | 25 mg/mL |
| S1009 | Dactolisib (BEZ235) | <1 mg/mL | 0.01 mg/mL | '<1 mg/mL |
| S1040 | Sorafenib Tosylate | 0.01 mg/mL | 127 mg/mL | '''<1 mg/mL |
| S1021 | Dasatinib | <1 mg/mL | 98 mg/mL | <1 mg/mL |
| S1039 | Rapamycin (Sirolimus) | <1 mg/mL | 20 mg/mL | '<1 mg/mL |
| S1068 | Crizotinib (PF-02341066) | <1 mg/mL | 9 mg/mL | '<1 mg/mL |
| S1023 | Erlotinib HCl (OSI-744) | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S1120 | Everolimus (RAD001) | <1 mg/mL | 100 mg/mL | 7 mg/mL |
| S1025 | Gefitinib (ZD1839) | <1 mg/mL | 89 mg/mL | 4 mg/mL |
| S1004 | Veliparib (ABT-888) | <1 mg/mL | 17 mg/mL | ''<1 mg/mL |
| S1053 | Entinostat (MS-275) | <1 mg/mL | 75 mg/mL | '<1 mg/mL |
| S1065 | Pictilisib (GDC-0941) | <1 mg/mL | 44 mg/mL | '<1 mg/mL |
| S1378 | Ruxolitinib (INCB018424) | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S1030 | Panobinostat (LBH589) | <1 mg/mL | 69 mg/mL | '<1 mg/mL |
| S1026 | Imatinib Mesylate (STI571) | 118 mg/mL | 118 mg/mL | ''<1 mg/mL |
| S1250 | Enzalutamide (MDV3100) | <1 mg/mL | 92 mg/mL | '<1 mg/mL |
| S1133 | Alisertib (MLN8237) | <1 mg/mL | 27 mg/mL | <1 mg/mL |
| S1011 | Afatinib (BIBW2992) | <1 mg/mL | 97 mg/mL | 15 mg/mL |
| S2226 | Idelalisib (CAL-101, GS-1101) | <1 mg/mL | 83 mg/mL | '23 mg/mL |
| S1048 | Tozasertib (VX-680, MK-0457) | <1 mg/mL | 93 mg/mL | '<1 mg/mL |
| S1555 | zad8555 | <1 mg/mL | 50 mg/mL | '3 mg/mL |
| S1006 | Saracatinib (AZD0530) | <1 mg/mL | 35 mg/mL | '31 mg/mL |
| S1057 | Obatoclax Mesylate (GX15-070) | <1 mg/mL | 83 mg/mL | <1 mg/mL |
| S1141 | Tanespimycin (17-AAG) | <1 mg/mL | 100 mg/mL | '5 mg/mL |
| S1166 | Cisplatin | <1 mg/mL | 60 mg/mL | ''<1 mg/mL |
| S1033 | Nilotinib (AMN-107) | <1 mg/mL | 27 mg/mL | '<1 mg/mL |
| S1044 | Temsirolimus (CCI-779) | <1 mg/mL | 67 mg/mL | '75 mg/mL |
| S1038 | PI-103 | <1 mg/mL | 24 mg/mL | '<1 mg/mL |
| S1069 | Luminespib (NVP-AUY922) | <1 mg/mL | 93 mg/mL | ''31 mg/mL |
| S1149 | Gemcitabine HCl | 19 mg/mL | <1 mg/mL | ''<1 mg/mL |
| S1122 | Mocetinostat (MGCD0103) | <1 mg/mL | 13 mg/mL | '<1 mg/mL |
| S1178 | Regorafenib (BAY 73-4506) | <1 mg/mL | 97 mg/mL | ''<1 mg/mL |
| S1129 | SRT1720 HCl | <1 mg/mL | 38 mg/mL | '<1 mg/mL |
| S1014 | Bosutinib (SKI-606) | <1 mg/mL | 100 mg/mL | ''''2 mg/mL |
| S1077 | SB202190 (FHPI) | <1 mg/mL | 66 mg/mL | '12 mg/mL |
| S2853 | Carfilzomib (PR-171) | <1 mg/mL | 50 mg/mL | ''<1 mg/mL |
| S1191 | Fulvestrant | <1 mg/mL | 100 mg/mL | '100 mg/mL |
| S1075 | SB216763 | <1 mg/mL | 23 mg/mL | ''<1 mg/mL |
| S1135 | Pemetrexed | 94 mg/mL | <1 mg/mL | <1 mg/mL |
| S2218 | Torkinib (PP242) | <1 mg/mL | 61 mg/mL | 18 mg/mL |
| S1225 | Etoposide | <1 mg/mL | 100 mg/mL | '''<1 mg/mL |
| S2248 | Silmitasertib (CX-4945) | <1 mg/mL | 16 mg/mL | '<1 mg/mL |
| S8048 | Venetoclax (ABT-199) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1230 | Flavopiridol (Alvocidib) | <1 mg/mL | 15 mg/mL | 8 mg/mL |
| S2111 | Lapatinib | <1 mg/mL | 100 mg/mL | '<1 mg/mL |
| S1237 | Temozolomide | <1 mg/mL | 38 mg/mL | <1 mg/mL |
| S5003 | Tacrolimus (FK506) | <1 mg/mL | 94 mg/mL | ''83 mg/mL |
| S1950 | Metformin HCl | 33 mg/mL | <1 mg/mL | '<1 mg/mL |
| S1573 | Fasudil (HA-1077) HCl | 65 mg/mL | 5 mg/mL | '<1 mg/mL |
| S1224 | Oxaliplatin | 3 mg/mL | -1 mg/mL | '''0.01 mg/mL |
| S7110 | (+)-JQ1 | <1 mg/mL | 91 mg/mL | 91 mg/mL |
| S2181 | Ixazomib Citrate (MLN9708) | <1 mg/mL | 100 mg/mL | '<1 mg/mL |
| S1972 | Tamoxifen Citrate | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S2827 | Torin 1 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S2658 | Omipalisib (GSK2126458) | <1 mg/mL | 100 mg/mL | '<1 mg/mL |
| S1782 | Azacitidine (5-Azacytidine) | <1 mg/mL | 48 mg/mL | ''<1 mg/mL |
| S2180 | Ixazomib (MLN2238) | <1 mg/mL | 72 mg/mL | ''9 mg/mL |
| S1590 | TWS119 | <1 mg/mL | 64 mg/mL | '<1 mg/mL |
| S1396 | Resveratrol | <1 mg/mL | 45 mg/mL | <1 mg/mL |
| S1322 | Dexamethasone | <1 mg/mL | 79 mg/mL | '''6 mg/mL |
| S1648 | Cytarabine | 48 mg/mL | 1 mg/mL | ''''<1 mg/mL |
| S1792 | Simvastatin | <1 mg/mL | 83 mg/mL | '83 mg/mL |
| S1714 | Gemcitabine | 52 mg/mL | 52 mg/mL | '<1 mg/mL |
| S2163 | PF-4708671 | <1 mg/mL | 30 mg/mL | 8 mg/mL |
| S2817 | Torin 2 | <1 mg/mL | 20 mg/mL | ''''<1 mg/mL |
| S1582 | H 89 2HCl | 6 mg/mL | 104 mg/mL | '<1 mg/mL |
| S2713 | Geldanamycin | <1 mg/mL | 36 mg/mL | <1 mg/mL |
| S2770 | MK-5108 (VX-689) | <1 mg/mL | 92 mg/mL | '<1 mg/mL |
| S2449 | Forskolin | <1 mg/mL | 82 mg/mL | '37 mg/mL |
| S7306 | Dorsomorphin (Compound C) 2HCl | 94 mg/mL | <1 mg/mL | '<1 mg/mL |
| S2505 | Rosiglitazone maleate | <1 mg/mL | 94 mg/mL | '<1 mg/mL |
| S2799 | Daporinad (FK866, APO866) | <1 mg/mL | <1 mg/mL | '78 mg/mL |
| S2929 | Pifithrin-α (PFTα) HBr | <1 mg/mL | 67 mg/mL | '<1 mg/mL |
| S7164 | GSK343 | <1 mg/mL | 1 mg/mL | '4 mg/mL |
| S8059 | Nutlin-3a | <1 mg/mL | 100 mg/mL | '100 mg/mL |
| S7007 | Binimetinib (MEK162) | <1 mg/mL | 88 mg/mL | '<1 mg/mL |
| S2751 | Milciclib (PHA-848125) | <1 mg/mL | 92 mg/mL | '<1 mg/mL |
| S7397 | Sorafenib | <1 mg/mL | 63 mg/mL | '''''<1 mg/mL |
| S2556 | Rosiglitazone | <1 mg/mL | 71 mg/mL | '<1 mg/mL |
| S3030 | Niclosamide | <1 mg/mL | <1 mg/mL | <1 mg/mL |
| S8047 | Dynasore | <1 mg/mL | 64 mg/mL | '<1 mg/mL |
| S1263 | CHIR-99021 (CT99021) | <1 mg/mL | 10 mg/mL | <1 mg/mL |
| S8075 | GANT61 | <1 mg/mL | <1 mg/mL | '12 mg/mL |
| S1389 | Omeprazole | <1 mg/mL | 69 mg/mL | 13 mg/mL |
| S1979 | Amiodarone HCl | <1 mg/mL | 23 mg/mL | 11 mg/mL |
| S2480 | Loperamide HCl | <1 mg/mL | 22 mg/mL | 4 mg/mL |
| S4028 | Dexamethasone Sodium Phosphate | 103 mg/mL | <1 mg/mL | <1 mg/mL |
| S1693 | Carbamazepine | <1 mg/mL | 47 mg/mL | 18 mg/mL |
| S2458 | Clonidine HCl | 53 mg/mL | 53 mg/mL | 53 mg/mL |
| S1837 | Flubendazole | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S1747 | Nimodipine | <1 mg/mL | 84 mg/mL | 84 mg/mL |
| S7067 | Tepotinib (EMD 1214063) | <1 mg/mL | 5 mg/mL | '<1 mg/mL |
| S7177 | PF-543 | <1 mg/mL | 93 mg/mL | ''93 mg/mL |
| S2491 | Nitrendipine | <1 mg/mL | 72 mg/mL | <1 mg/mL |
| S5243 | Ruxolitinib Phosphate | 29 mg/mL | 80 mg/mL | '8 mg/mL |
| S7781 | Sunitinib | <1 mg/mL | 25 mg/mL | ''<1 mg/mL |
| S7786 | Erlotinib | <1 mg/mL | 78 mg/mL | '15 mg/mL |
| S8595 | Tat-beclin 1 (Tat-BECN1) | 100 mg/mL | -1 mg/mL | -1 mg/mL |
| S5715 | atorvastatin | -1 mg/mL | 100 mg/mL | '-1 mg/mL |
| S7655 | CB-839 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S3653 | Spermidine trihydrochloride | 50 mg/mL | 30 mg/mL | <1 mg/mL |
| S9027 | Corynoxine | <1 mg/mL | 77 mg/mL | 77 mg/mL |
| S4081 | Sulfacetamide Sodium | 51 mg/mL | 19 mg/mL | <1 mg/mL |
| S7483 | DMOG | 35 mg/mL | 35 mg/mL | '35 mg/mL |
| S8240 | SMER28 | <1 mg/mL | 52 mg/mL | 52 mg/mL |
| S7104 | AZD1208 | <1 mg/mL | 75 mg/mL | ''<1 mg/mL |
| S4546 | Xylitol | 30 mg/mL | 30 mg/mL | <1 mg/mL |
| S7840 | Dorsomorphin (Compound C, BML-275) | <1 mg/mL | 1 mg/mL | '2 mg/mL |
| S9310 | Isorhychophylline | -1 mg/mL | 77 mg/mL | -1 mg/mL |
| S1238 | Tamoxifen | <1 mg/mL | 74 mg/mL | ''74 mg/mL |
| S8597 | LYN-1604 | 100 mg/mL | 50 mg/mL | '100 mg/mL |
| S2924 | CHIR-99021 (CT99021) HCl | <1 mg/mL | 93 mg/mL | 2 mg/mL |
| S2215 | DAPT (GSI-IX) | <1 mg/mL | 86 mg/mL | 50 mg/mL |
| S1241 | Vincristine sulfate | 60 mg/mL | 100 mg/mL | ''<1 mg/mL |
| S1168 | Valproic acid sodium salt (Sodium valproate) | 33 mg/mL | 33 mg/mL | 33 mg/mL |
| S1041 | STF-62247 | <1 mg/mL | 53 mg/mL | 3 mg/mL |
| S7153 | 10058-F4 | <1 mg/mL | 49 mg/mL | '4 mg/mL |
| S7980 | VPS34-IN1 | <1 mg/mL | 85 mg/mL | ''85 mg/mL |
| S4750 | Sulfacetamide sodium salt hydrate | 50 mg/mL | 50 mg/mL | 2 mg/mL |
Autophagy製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1013 |
Bortezomib (PS-341)Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors. |
Effect of different proteasome inhibitors on dysferlin expression and on membrane resealing in cultured primary myoblasts. Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of bortezomib for 24 hours. Western blots of protein extracts were stained with anti-dysferlin antibodies and with anti–a-tubulin antibody as loading control.
|
|
| S6851新 |
RA-190RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells. |
||
| S8943新 |
VLX600VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity. |
||
| S6716新 |
NSC 185058NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways. |
||
| S7455新 |
Resatorvid (TAK-242)Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid inhibits autophagy. |
||
| S1109 |
BI 2536BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. |
|
|
| S1105 |
LY294002LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis. |
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.
|
|
| S1092 |
KU-55933 (ATM Kinase Inhibitor)KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy. |
Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated. |
|
| S1102 |
U0126-EtOHU0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity. |
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. |
|
| S1150 |
PaclitaxelPaclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. |
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. |
|
| S1460 |
SP600125SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
Loss of DUSP4 function upregulates IL-6 and IL-8 and enhances mammosphere growth. Immunoblot analysis of MDA-231 cells after treatment of 24 hours with 1 umol/L selumetinib (MEKi) or 10 umol/L SP600125 (JNKi). I, MDA-231 mammosphere formation quantitated by GelCount software 7 days after siRNA transfection. Where indicated, selumetinib (MEKi) or SP600125 (JNK1) or the combination was added to the mammosphere cultures.
|
|
| S1490 |
Ponatinib (AP24534)Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy. |
RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
|
|
| S1113 |
GSK690693GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
|
|
| S2758 |
WortmanninWortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
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. |
|
| S2704 |
LY2109761LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis. |
The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.
|
|
| S2767 |
3-Methyladenine (3-MA)3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating. |
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.
|
|
| S2243 |
Degrasyn (WP1130)Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy. |
Protein expression by western blot analysis of cell lysates from MCF-7, TAMR-4 and 164R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
|
|
| S1786 |
VerteporfinVerteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis. |
Verteporfin treatment inhibits proliferation and induces apoptosis of Tsc1-null cells in vivo. Mice were administered i.p. with vehicle or verteporfin at a dose of 100 mg/kg every other day for 10 d before sacrifice. Mice were sacrificed at 6 wk of age. Three independent experiments were performed and mice in different treatments were pooled for analysis. Percentage of Ki67 and αSMA double-positive cells in α-SMA+ mesenchymal lesions in the indicated kidneys. Immunofluorescence staining and counting were performed on three sagittal sections from different kidney regions for each mouse.
|
|
| S7046 |
Brefeldin ABrefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy. |
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. |
|
| S8037 |
Necrostatin-1Necrostatin-1 is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis. |
Cytosolic extracts or nuclear extracts were examined by Western blot analysis using Abs against p105/p50, p100/p52 and phospho-p65. Solid arrowhead indicates a non-specific band. A nuclear marker, PARP, and cytosolic marker, b-tubulin, were used to assess the purity of each fraction.
|
|
| S2775 |
NocodazoleNocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. |
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. |
|
| S3042 |
PurmorphaminePurmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy. |
a-d) LoVo cells were separately or simultaneously treated with 1 μM purmorphamine and 1 μM thiostrepton for the indicated time. a The Gli1, FoxM1, and CCNB1 protein expression levels were examined by immunoblotting after drug treatment for 48 h. b Cell viability was detected after 6 days using an MTT assay. c LoVo cells treated with indicated drugs were cultured for 2 weeks, and outgrowth colonies were stained with crystal violet. d The matched colony count of (c). Error bars represent the mean and S.D. of three independent experiments. **, p < 0.01.
|
|
| S4157 |
Chloroquine PhosphateChloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
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. |
|
| S1413 |
Bafilomycin A1(Baf-A1)Bafilomycin A1 is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis. |
Mitochondrial depolarization mediated relocation of mitochondrial RC-TPP into lysosomes and the ensuing lysosomal acidity triggered rhodamine fluorescence. RC-TPP-loaded Tom20-GFP+ HeLa cells were treated without or with CCCP (20 μM) in the presence or absence of BFA (200 nM). Colocalization of Tom20-GFP (in green) and mitochondrial RC-TPP (in blue) is shown in cyan. Scale bar: 10 μm.
|
|
| S1835 |
AzithromycinAzithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
||
| S8808 |
DC661DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis. |
||
| S7289 |
PFK15PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM. |
b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays. |
|
| S7885 |
SBI-0206965SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. |
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. |
|
| S8576 |
EAD1EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells. |
||
| S8764 |
IITZ-01IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function. |
||
| S7888 |
Spautin-1Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis. |
Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
|
|
| S8317 |
3BDO3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. |
||
| S7811 |
MHY1485MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits 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.
|
|
| S8596 |
AutophinibAutophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro. |
||
| S7423 |
KN-93 PhosphateKN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy. |
Paeoniflorin (PF) protects the heart against MI-induced injury in DM mice. Heart function was analyzed by measuring fractional shortening {FS = [LV end diastolic diameter (LVEDD)-LVend systolic diameter (LVESD)]×100/LVEDD} and LV ejection fraction [LVEF = (LVEDD2−LVESD2)/LVEDD2].
|
|
| S8807 |
PFK158PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors. |
||
| S3758 |
Cucoline hydrochloride, Kukoline hydrochloride, Sabianine A hydrochlorideSinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent. |
||
| S8369 |
Lys05Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth. |
||
| S7660 |
Obeticholic AcidObeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3. |
(c) Functional bile canaliculi or lack thereof in PHHs within MPTCs (12 d of drug treatment) as visualized by transport of fluorescent (green) dye into the canaliculi between PHHs. DMSO-treated MPCC control image is shown to the far right. (d) Neutral lipid (Nile red, green) staining of PHHs within MPTCs (12 d of drug treatment). DMSO-treated MPCC control image is shown to the far right. (e) NR1I2 (PXR) gene expression in drug-treated MPTCs relative to DMSOtreated MPTC controls (12 d of treatment). (f) ABCC2 (MRP2) gene expression in drug-treated MPTCs relative to DMSO-treated MPTC controls (12 d of treatment). (g) IL-6 levels in drug-treated MPTC supernatants (6 d of treatment). In all panels, statistical significance is displayed relative to DMSO-treated MPTCs. *p r 0.05, **p r 0.01, ***p r 0.001, and ****p r 0.0001. Scale bars on images represent 80 mm. |
|
| S4430 |
Hydroxychloroquine SulfateHydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9. |
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).
|
|
| S7949 |
MRT68921 HClMRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively. |
|
|
| S8744 |
PHY34PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo. |
||
| S5920 |
CA-5fCA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. |
||
| S7683 |
PIK-IIIPIK-III, which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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 |
|
| S8793 |
ULK-101ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively. |
||
| S8527 |
ROC-325ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM. |
||
| S9424 |
Liensinine diperchlorateLiensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor. |
||
| S6471 |
LucanthoneLucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1. |
||
| S9150 |
DaurisolineDaurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects. |
||
| S1078 |
MK-2206 2HClMK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2. |
VE-cadherin-induced Akt activation mediates YAP phosphorylation and translocation in ECs. HUVECs were starved for 1h and treated with thrombin (1U) for 1h. Total cell lysates were probed with anti-pAkt, Akt or b-actin antibody. The representative blots of three independent experiments are depicted, and the normalized values for p-Akt are shown. HUVECs were cultured and starved as described as in d and incubated for 8h in complete medium with the Akt inhibitor, MK-2206 (1 uM). pAkt, Akt, pYAP and YAP were detected by western blotting using specific antibodies.
|
|
| S1060 |
Olaparib (AZD2281)Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. |
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.
|
|
| S1267 |
Vemurafenib (PLX4032)Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy. |
The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).
|
|
| S1047 |
Vorinostat (SAHA)Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification. |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
|
| S6797新 |
QX77QX77 is a novel activator of chaperone-mediated autophagy (CMA). QX77 induces the up-regulation of Rab11 expression and up-regulates LAMP2A expression. |
||
| S6650新 |
EN6EN6 is a novel covalent autophagy activator and targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase with an IC50 of 1.7 μM for recombinant human ATP6V1A protein. |
||
| S1002 |
ABT-737ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. 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. |
|
| S1049 |
Y-27632 2HClY-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. |
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.
|
|
| S2619 |
MG-132MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells. |
MDA-MB-231 cells were treated with 10 uM MG132 and incubated under normoxia or hypoxia for 4 h. Endogenous interaction between LATS2 and SIAH2 was analysed by immunoprecipitation.
|
|
| S1009 |
Dactolisib (BEZ235)Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. |
Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments. |
|
| S1040 |
Sorafenib TosylateSorafenib Tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
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. |
|
| S1021 |
DasatinibDasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity. |