-
Australia
-
Austria
-
Belgium
-
Brazil
-
Canada
-
China
-
Czech Republic
-
Denmark
-
Finland
-
France
-
Germany
-
Greece
-
Hong Kong
-
Hungary
-
Iceland
-
India
-
Ireland
-
Israel
-
Italy
-
Japan
-
Korea
-
Luxembourg
-
Malaysia
-
Netherlands
-
New Zealand
-
Norway
-
Poland
-
Qatar
-
Romania
-
Saudi Arabia
-
Singapore
-
Spain
-
Sweden
-
Switzerland
-
Taiwan
-
Turkey
-
United Kingdom
-
United States
Autophagy Inhibitors
- Featured Inhibitors
- Inhibitors (68)
- Modulators (16)
- Chemicals (2)
- Agonists (3)
- Activators (209)
- Antagonist (1)
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S6999 | Chloroquine | Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity. |
|
|
| S4157 | Chloroquine diphosphate | Chloroquine 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). |
|
|
| S4430 | HCQ (Hydroxychloroquine) Sulfate | Hydroxychloroquine (HCQ) 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. |
|
|
| S7888 | Spautin-1 | Spautin-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. This compound enhances apoptosis. |
|
|
| S7683 | PIK-III | PIK-III (VPS34-IN2), 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. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively. |
|
|
| S8369 | Lys05 Trihydrochloride | Lys05 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. |
|
|
| S8808 | DC661 | DC661 is a potent palmitoyl protein thioesterase 1 (PPT1) inhibitor. DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than HCQ. DC661 induces apoptosis. |
|
|
| E4824 | Hydroxychloroquine | Hydroxychloroquine (HCQ) is an antimalarial drug that inhibits autophagy and is used to treat systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). It exhibits immunomodulatory, antithrombotic, and antiplatelet properties. It inhibits the release endothelin-1, a potent vasoconstrictor, and restores impaired angiogenesis in TNF-α-treated endothelial cells in vitro. It also reduces the production of inflammatory cytokines such as TNF-α, IFN-γ, and IL-6 from peripheral blood mononuclear cells, upregulates IL-10 and decreases platelet aggregation. |
|
|
| S8596 | Autophinib | Autophinib 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. |
|
|
| S6716 | NSC 185058 | NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways. |
|
|
| S3698 | Nortriptyline hydrochloride | Nortriptyline hydrochloride (Desitriptyline, ELF-101, EN-7048, Desmethylamitriptyline) is the hydrochloride salt form of nortriptyline, a tricyclic antidepressant agent used for short-term treatment of various forms of depression. |
|
|
| S8527 | ROC-325 | ROC-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. |
|
|
| S8576 | EAD1 | EAD1 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. |
|
|
| S5920 | CA-5f | CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. |
|
|
| S9150 | Daurisoline | Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects. |
|
|
| S8764 | IITZ-01 | IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function. |
|
|
| S9424 | Liensinine diperchlorate | Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor. |
|
|
| S6471 | Lucanthone | Lucanthone 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. |
|
|
| E4809 | Piperaquine tetraphosphate tetrahydrate | Piperaquine tetraphosphate tetrahydrate is an inhibitor of autophagy . It is a bisquinoline antimalarial agent effective against Plasmodium falciparum. This compound is useful in antimalarial research. | ||
| E8307New | Chloroquine dihydrochloride | Chloroquine dihydrochloride acts as an inhibitor of autophagy and toll-like receptors (TLRs). Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. | ||
| E6578New | AS1708727 | AS1708727 is an orally bioavailable Foxo1 inhibitor that exhibits EC50 values of 0.33 μM against G6Pase and 0.59 μM against PEPCK. | ||
| S8744 | PHY34 | PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo. | ||
| S1105 | LY294002 | LY294002 (SF 1101, NSC 697286) 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. This compound also inhibits CK2 with IC50 of 98 nM. It is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis. |
|
|
| S1013 | Bortezomib | Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. This compound 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. |
|
|
| S1460 | SP600125 | SP600125 (Nsc75890) 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. This compound 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. It inhibits autophagy and activates apoptosis. |
|
|
| 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. It blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also inhibits autophagosome formation. Solutions are unstable and should be fresh-prepared. |
|
|
| S1102 | U0126-EtOH | U0126-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. |
|
|
| S1413 | Bafilomycin A1 (Baf-A1) | Bafilomycin A1 (Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM, and it is found to inhibit autophagy while inducing apoptosis. |
|
|
| S1150 | Paclitaxel | Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy. |
|
|
| S1092 | KU-55933 | KU-55933 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. |
|
|
| S2758 | Wortmannin (SL-2052) | Wortmannin 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. |
|
|
| S8037 | Necrostatin-1 (Nec-1) | Necrostatin-1 (Nec-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. |
|
|
| S1109 | BI 2536 | BI-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. |
|
|
| S1490 | Ponatinib (AP24534) | Ponatinib 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. |
|
|
| S1786 | Verteporfin | Verteporfin 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. |
|
|
| S2704 | LY2109761 | LY2109761 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. This compound blocks autophagy and induces apoptosis. |
|
|
| S2775 | Nocodazole | Nocodazole 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. Nocodazole induces apoptosis. |
|
|
| S1113 | GSK690693 | GSK690693 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. |
|
|
| S7811 | MHY1485 | MHY1485 is a potent, and cell-permeable mTOR activator, and this compound also potently inhibits autophagy. |
|
|
| S7046 | Brefeldin A (BFA chemical) | Brefeldin A (BFA) 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. |
|
|
| S7455 | Resatorvid (TAK-242) | Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. This compound downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF, and it also inhibits autophagy. |
|
|
| S3042 | Purmorphamine | Purmorphamine (Shh Signaling Antagonist VI), 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. |
|
|
| S7146 | DMH1 | DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. This compound inhibits autophagy. |
|
|
| S7751 | VER-155008 | VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins. |
|
|
| S7423 | KN-93 Phosphate | KN-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.This product is not soluble in saline. Please do not dissolve it in saline for administration. |
|
|
| S7033 | GSK2656157 | GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. This compound decreases apoptosis and inhibits excessive autophagy. |
|
|
| 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). This compound induces apoptosis and blocks autophagy. |
|
|
| S7949 | MRT68921 Hydrochloride | MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively. |
|
|
| S8222 | AS1842856 | AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy. |
|
|
| S7682 | SAR405 | SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells. |
|
|
| S7885 | SBI-0206965 | SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells. |
|
|
| S7381 | Pepstatin A | Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases. |
|
|
| S1346 | Heparin Sodium | Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy. |
|
|
| S7289 | PFK-015 | PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM. |
|
|
| S1835 | Azithromycin | Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
|
|
| S2930 | Pifithrin-μ | Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and this compound also inhibits HSP70 function and autophagy. |
|
|
| S8274 | STO-609 | STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. This compound inhibits AMPKK activity and inhibits autophagy. |
|
|
| S7660 | Obeticholic Acid (INT-747) | Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM, and it inhibits autophagy. This compound is in Phase 3. |
|
|
| S7948 | MRT67307 HCl | MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy. |
|
|
| S8793 | ULK-101 | ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively. |
|
|
| S8317 | 3BDO | 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. This compound inhibits oxLDL-induced apoptosis. |
|
|
| S8807 | PFK158 | PFK158 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. |
|
|
| S1733 | Methylprednisolone | Methylprednisolone is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. This compound activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. It markedly reduces autophagy and apoptosis. |
|
|
| S6912 | Vacuolin-1 | Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. This compound is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. |
|
|
| S3758 | Sinomenine hydrochloride | Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent. |
|
|
| S5973 | Methylprednisolone Acetate | Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis. |
|
|
| S4643 | KB-R7943 mesylate | KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. This compound promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux. | ||
| E1232 | Concanavalin A | Concanavalin A is a potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis for cancer therapeutics. |
Products are for research use only. Not for human use. We do not sell to patients.
©Copyright 2013 Selleck Chemicals. All Rights Reserved.