Search Result
Results for "
Autophagy Inhibitor
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
46
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-163136
-
|
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Autophagy
REV-ERB
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Cancer
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Autophagy/REV-ERB-IN-1 (compound 24) is a dual inhibitor of autophagy and REV-ERB. Autophagy/REV-ERB-IN-1 has anti-tumor activity with a CC50 value of 2.3 μM on BTB-474 cells.
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-
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- HY-162100
-
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ULK
Autophagy
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Cancer
|
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MR-2088 is a selective ULK1/ULK2 inhibitor with pEC50 values of 8.3 and 8.7, respectively. MR-2088 selectively inhibits autophagy through ULK1/2 mediated inhibition .
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- HY-Y1269H
-
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Salmiac, meets analytical specification of Ph. Eur. BP USP FCC
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Autophagy
Biochemical Assay Reagents
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Others
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Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC (Salmiac, meets analytical specification of Ph. Eur. BP USP FCC) can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
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-
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- HY-116071
-
|
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Autophagy
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Cancer
|
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Autophagy-IN-3 (Compound 6k) is an autophagy inhibitor. Autophagy-IN-3 promotes metabolic stress in the tumor microenvironment and enhances the effects of cytostatics in combined treatments .
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-
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- HY-163136A
-
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Autophagy
REV-ERB
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Cancer
|
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Autophagy/REV-ERB-IN-1
hydrochloride (Compound 24) is a dual autophagy and REV-ERB inhibitor with
anticancer activity. Autophagy/REV-ERB-IN-1 (hydrochloride) has improved
potency in blocking autophagy, enhanced toxicity against cancer cells.
Autophagy/REV-ERB-IN-1 (hydrochloride) can be used for the research for
melanoma .
|
-
-
- HY-150636
-
|
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Autophagy
Apoptosis
|
Cancer
|
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Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
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-
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- HY-101920
-
|
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Autophagy
PI3K
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Neurological Disease
Cancer
|
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Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34 .
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-
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- HY-131344
-
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mTOR
Autophagy
|
Cancer
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mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells .
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-
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- HY-124132
-
|
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Autophagy
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Cancer
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Autophagy-IN-4 (Compound 34) is an autophagy inhibitor, with an EC50 of 0.5 μM and a LD50 of 27 μM for U2OS cells .
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-
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- HY-124726
-
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Autophagy
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Neurological Disease
Cancer
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Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively .
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-
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- HY-150757
-
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Autophagy
Apoptosis
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Cancer
|
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Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research .
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-
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- HY-144637
-
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Apoptosis
Autophagy
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Cancer
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Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
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- HY-123058
-
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PI3K
Autophagy
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Cancer
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Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components .
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-
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- HY-U00434
-
-
-
- HY-163193
-
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Atg4
Autophagy
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Cancer
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MJO445 (Compound 7) is a ATG4B inhibitor, which inhibits the autophagy of glioblastoma .
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-
-
- HY-N8530
-
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Others
|
Inflammation/Immunology
|
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Conodurine is a monoterpenoid indole alkaloid.
Conodurine can inhibit lysosomal acidification. Conodurineis isolated from the natural
Tabernaemontana corymbosa .
|
-
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- HY-110228
-
|
1,1-Dimethylbiguanide-d6 hydrochloride
|
AMPK
Autophagy
Mitophagy
|
Cardiovascular Disease
Metabolic Disease
|
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Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
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- HY-B0146
-
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CL 318952
|
YAP
Apoptosis
Autophagy
|
Cancer
|
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Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation .
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- HY-15531S
-
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ABT-199-d8; GDC-0199-d8; RG7601-d8
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Bcl-2 Family
Autophagy
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Cancer
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Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
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- HY-117357
-
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SGK
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Cancer
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SI-113 is a SGK1 inhibitor, with an IC50 of 600 nM. SI113 induces autophagy .
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- HY-112698
-
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p62
Atg8/LC3
Autophagy
Apoptosis
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Cancer
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CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity .
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- HY-110019
-
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Lu 19-005
|
Serotonin Transporter
Dopamine Transporter
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Neurological Disease
|
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Indatraline hydrochloride (Lu 19-005) is a non-selective monoamine transporter inhibitor that blocks the reuptake of neurotransmitters (dopamine, serotonin, and norepinephrine). Indatraline hydrochloride can be used for the research of antidepressive. Indatraline hydrochloride induces autophagy while simultaneously inhibiting cell proliferation. Indatraline hydrochloride may also serve to direct the development of new agents for autophagy-related diseases such as atherosclerosis or restenosis .
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- HY-124582
-
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Autophagy
mTOR
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Cancer
|
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NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .
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-
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- HY-112914
-
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mTOR
Autophagy
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Cancer
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mTOR inhibitor-1 (Compound C-4) is an ATP-Competitive mTOR inhibitor which can suppress cells proliferation and inducing autophagy .
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-
-
- HY-147520
-
-
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- HY-N1244
-
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Sarmentosine; Sarmentosine (glycoside)
|
Keap1-Nrf2
mTOR
Apoptosis
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Cancer
|
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Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells .
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-
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- HY-B0146R
-
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CL 318952 (Standard)
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YAP
Apoptosis
Autophagy
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Cancer
|
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Verteporfin (Standard) is the analytical standard of Verteporfin. This product is intended for research and analytical applications. Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation .
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-
-
- HY-111621
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DC661
4 Publications Verification
|
Autophagy
Apoptosis
|
Cancer
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DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity .
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-
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- HY-107720
-
|
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NO Synthase
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Cancer
|
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ARL-17477 is a dual inhibitor of NOS1and the autophagy-lysosomal system with anticancer activity and can inhibit tumor growth in KRAS-mutated cancers .
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-
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- HY-12057S
-
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Isotope-Labeled Compounds
Raf
Autophagy
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Cancer
|
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Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
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- HY-12057S1
-
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PLX4032-d7; RG7204-d7; RO5185426-d7
|
Isotope-Labeled Compounds
Raf
Autophagy
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Cancer
|
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Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
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- HY-13629S1
-
-
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- HY-50910
-
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CCI-779
|
mTOR
Autophagy
Apoptosis
Bacterial
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Cancer
|
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Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model .
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-
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- HY-15184
-
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Azalomycin B; Gopalamicin; Efomycin E
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Autophagy
Antibiotic
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Cancer
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Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells .
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- HY-123056
-
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Autophagy
Apoptosis
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Cancer
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EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis .
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- HY-B1417
-
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Desmethylamitriptyline hydrochloride; Desitriptilina hydrochloride
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Autophagy
Drug Metabolite
Apoptosis
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Neurological Disease
Cancer
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Nortriptyline (Desmethylamitriptyline) hydrochloride, the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline hydrochloride is a potent autophagy inhibitor and has anticancer effects .
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- HY-118620
-
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Desmethylamitriptyline; Desitriptilina
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Autophagy
Drug Metabolite
Apoptosis
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Neurological Disease
Cancer
|
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Nortriptyline (Desmethylamitriptyline), the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline is a potent autophagy inhibitor and has anticancer effects .
N
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-
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- HY-148507
-
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MEK
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Cancer
|
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GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis .
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-
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- HY-117924
-
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Autophagy enhancer-67
|
Autophagy
|
Neurological Disease
|
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AUTEN-67 (Autophagy enhancer-67) is an orally active autophagy enhancer and MTMR14 inhibitor. AUTEN-67 has anti-aging and neuroprotective effects. AUTEN-67 protects neurons from stress-induced cell death. AUTEN-67 also restores nesting behavior in a mice model of Alzheimer disease .
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- HY-13417A
-
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Acadesine phosphate; AICA Riboside phosphate
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AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
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Cancer
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AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
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- HY-13417
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Acadesine; AICA Riboside
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AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
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Cancer
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AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
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- HY-12990
-
-
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- HY-129111
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EACC
3 Publications Verification
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Autophagy
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Infection
Neurological Disease
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EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion .
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- HY-112897
-
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Autophagy
PI3K
Apoptosis
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Cancer
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IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
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-
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- HY-15206S
-
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Isotope-Labeled Compounds
Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
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Metabolic Disease
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Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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-
-
- HY-15206S1
-
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Glyburide-d3
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Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
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Metabolic Disease
|
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Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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- HY-N2117
-
-
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- HY-B0795
-
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mTOR
Autophagy
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Cancer
|
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MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes .
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-
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- HY-135811
-
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Parasite
Toll-like Receptor (TLR)
Autophagy
|
Infection
|
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Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity .
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-
-
- HY-121532
-
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Ras
Apoptosis
Autophagy
|
Cancer
|
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(-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line) .
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- HY-13003
-
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mTOR
Autophagy
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Cancer
|
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Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.
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- HY-112818
-
-
- HY-149343
-
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Apoptosis
Autophagy
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Cancer
|
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Anticancer agent 132 (compound Rh1) is an inducer of apoptosis and autophagy with antitumor and antimetastasis activity. Anticancer agent 132 arrests cell cycle and inhibits cell proliferation .
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- HY-155657
-
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Src
|
Inflammation/Immunology
|
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BT424 is a specific HCK inhibitor. BT424 can regulate macrophage activation and autophagy in vitro. BT424 ameliorates inflammation and kidney fibrosis in UUO model .
|
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- HY-10999
-
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GSK1120212; JTP-74057
|
MEK
Autophagy
Apoptosis
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Cancer
|
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Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
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- HY-12031A
-
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MEK
Autophagy
Mitophagy
Influenza Virus
|
Cancer
|
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U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
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- HY-146130
-
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Atg7
Autophagy
|
Cancer
|
|
ATG7-IN-2 (compound 1) is a potent ATG7 inhibitor, with an IC50 of 0.089 μM. ATG7-IN-2 inhibits autophagy marker LC3B .
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- HY-163001
-
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Autophagy
p62
Atg8/LC3
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Cancer
|
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Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
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- HY-13251
-
-
- HY-135811A
-
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Parasite
Toll-like Receptor (TLR)
Autophagy
|
Infection
|
|
Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity .
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- HY-162365
-
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HSP
Apoptosis
Autophagy
|
Cancer
|
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JD-02 is a novel Hsp90 inhibitor. JD-02 can induce autophagy and apoptosis. JD-02 increses the level of reactive oxygen species .
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- HY-N12277
-
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Apoptosis
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Neurological Disease
|
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Celosin K (compound 8) can be isolated from the seeds of Semen Celosiae. Celosin K is a potent inhibitor of neuron injury elicited by t-BHP. Celosin K inhibits oxidative stress and apoptosis, and acts of autophagy .
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-
- HY-149577
-
|
|
EBV
|
Cancer
|
|
Epstein-Barr virus (EBV) lytic cycle inducer-1 Dp44mT (compound C7) is an iron-chelatoe-like compound. Dp44mT cooperates with HDAC inhibitor Romidespin (HY-15149) and SAHA to induce EBV lytic cycle. Dp44mT reactivates EBV lytic cycle by activating the ERK1/2-autophagy axis in epithelial cancers .
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- HY-17471A
-
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1,1-Dimethylbiguanide hydrochloride
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AMPK
Autophagy
Mitophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy .
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- HY-100599
-
-
- HY-19312
-
-
- HY-138939
-
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Lipoxygenase
|
Cancer
|
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5-LOX-IN-2, an inhibitor of 5-lipoxygenase (5-LOX) with an IC50 of 0.33 μM, inhibits 5-LOX in a dose-dependent manner . 5-LOX-IN-2, reduces the cell viability of renal cancer cells and induces apoptosis, can be used for cancer research .
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- HY-N2593
-
|
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Autophagy
|
Inflammation/Immunology
Cancer
|
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Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation .
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- HY-Y1269
-
|
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|
|
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Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor .
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- HY-155954
-
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Apoptosis
Autophagy
|
Cancer
|
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UCM-1336 is a potent ICMT inhibitor, with an IC50 of 2 μM. UCM-1336 induces mislocalization of endogenous Ras, decreases Ras activation and induces cell death by autophagy and apoptosis .
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- HY-10219
-
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Sirolimus; AY-22989
|
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
Bacterial
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Cancer
|
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Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
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-
- HY-141882
-
|
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Atg8/LC3
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
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DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC50 of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination researchs in cancer through inhibiting autophagy .
|
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- HY-15531
-
|
ABT-199; GDC-0199; RG7601
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
|
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- HY-16966
-
|
|
ULK
Autophagy
Apoptosis
|
Cancer
|
|
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2 .
|
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- HY-128339
-
|
|
Autophagy
|
Cancer
|
|
Autogramin-1 potently inhibits autophagy induced by either starvation (IC50=0.17 μM) or mTORC1 inhibition (Rapamycin; IC50=0.44 μM) .
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- HY-128340
-
|
|
Autophagy
|
Cancer
|
|
Autogramin-2 potently inhibits autophagy induced by either starvation (IC50=0.27 μM) or mTORC1 inhibition (Rapamycin; IC50=0.14 μM) .
|
-
- HY-110067
-
-
- HY-103438
-
|
|
Apoptosis
Akt
mTOR
|
Cancer
|
|
BIBU1361 induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6 .
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- HY-12048
-
-
- HY-12031
-
|
|
MEK
Autophagy
Mitophagy
Influenza Virus
|
Cancer
|
|
U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
|
-
- HY-15609
-
-
- HY-N0112
-
|
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Infection
Cancer
|
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-162041
-
|
|
Survivin
|
Cancer
|
|
AQIM-I is an inhibitor of survivin via inhibits survivin expression and colony formation. AQIM-I induces ROS production, apoptosis, cell cycle arrest, DNA damage, and autophagy. AQIM-I inhibits nonsmall cell lung cancer cells A549 with an IC50 value of 9 nM .
|
-
- HY-160699
-
|
|
ULK
Ras
|
Cancer
|
|
DCC-3116 is an orally active ULK1/2 inhibitor. DCC-3116 can promote autophagy in lung cancer cells by inhibiting KRAS G12C signaling, thereby inhibiting the proliferation of lung cancer cells and exerting anti-cancer effects .
|
-
- HY-N3913
-
|
|
STAT
Bcl-2 Family
|
Cancer
|
|
Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells .
|
-
- HY-10162
-
|
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-13629
-
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-100596
-
|
|
Autophagy
|
Metabolic Disease
|
|
AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy . AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression .
|
-
- HY-114490
-
ULK-101
3 Publications Verification
|
ULK
|
Cancer
|
|
ULK-101 is a potent and selective ULK1 inhibitor, with IC50 values of 1.6 nM and 30 nM for ULK1 and ULK2, respectively. ULK-101 suppresses autophagy and sensitizes cancer cells to nutrient stress .
|
-
- HY-B0627
-
|
1,1-Dimethylbiguanide
|
AMPK
Autophagy
Mitophagy
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy .
|
-
- HY-10999S
-
|
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
|
-
- HY-122571
-
|
|
Filovirus
Parasite
Autophagy
|
Infection
Cancer
|
|
Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy .
|
-
- HY-155785
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species
JAK
|
Cancer
|
|
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
|
-
- HY-108701
-
|
|
NAMPT
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death .
|
-
- HY-10542A
-
|
|
Atg8/LC3
Raf
|
Neurological Disease
|
|
(Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder .
|
-
- HY-10999A
-
|
GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
|
MEK
Apoptosis
|
Cancer
|
|
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis .
|
-
- HY-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-146131
-
|
|
Atg7
Atg8/LC3
Autophagy
|
Cancer
|
|
ATG7-IN-3 (compound 18) is a potent ATG7 inhibitor, with an IC50 of 0.048 μM. ATG7-IN-3 inhibits autophagy. ATG7-IN-3 inhibits the formation of endogenous LC3B puncta in the neuroglioma cell line H4 .
|
-
- HY-12855A
-
Lys05
2 Publications Verification
Lys01 trihydrochloride
|
Autophagy
|
Cancer
|
|
Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
|
-
- HY-135811S
-
-
- HY-N2959
-
|
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 µM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- HY-135811S1
-
-
- HY-13018
-
|
|
IKK
ULK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells .
|
-
- HY-13018A
-
|
|
IKK
ULK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells .
|
-
- HY-10999S1
-
|
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib- 13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
|
-
- HY-10219S
-
|
Sirolimus-d3; AY-22989-d3
|
mTOR
FKBP
Autophagy
|
Cancer
|
|
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
|
-
- HY-13018B
-
|
|
IKK
ULK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells .
|
-
- HY-12057
-
|
PLX4032; RG7204; RO5185426
|
Raf
Autophagy
|
Cancer
|
|
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-13030
-
-
- HY-103706
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis .
|
-
- HY-N0072
-
|
|
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities .
|
-
- HY-13630
-
|
BMY-40481
|
Topoisomerase
Bacterial
Autophagy
Apoptosis
|
Infection
Neurological Disease
Cancer
|
|
Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-12406
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Autophagy
|
Cancer
|
|
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity .
|
-
- HY-111383
-
-
- HY-148598
-
|
CUR5-8
|
Apoptosis
Autophagy
|
Metabolic Disease
|
|
Curcumin 5-8 (CUR5-8) is a potent and orally active naturally active curcumin (CUR) analog. Curcumin 5-8 inhibits lipid droplet formation. Curcumin 5-8 increases autophagy and inhibits Apoptosis. Curcumin 5-8 improves insulin resistance and insulin sensitivity .
|
-
- HY-163178
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Bisabosqual A, a potent asparagine synthetase (ASNS) inhibitor, with an IC50 of 10.7 μM. Bisabosqual A can covalently modify the K556 site of ASNS protein. Bisabosqual A promotes oxidative stress and apoptosis, while inhibiting autophagy, cell migration and epithelial-mesenchymal transition (EMT), impeding cancer cell development .
|
-
- HY-10587A
-
|
|
Histone Methyltransferase
Apoptosis
Autophagy
|
Cancer
|
|
BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells .
|
-
- HY-N0410
-
|
Eleutheroside A; β-Sitosterol β-D-glucoside
|
Apoptosis
Reactive Oxygen Species
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-B0006A
-
|
BM 14190 phosphate hemihydrate
|
Adrenergic Receptor
Autophagy
Bacterial
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker . Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome .
|
-
- HY-151972
-
|
|
Epigenetic Reader Domain
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
|
-
- HY-12041
-
|
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis .
|
-
- HY-10218
-
|
RAD001; SDZ-RAD
|
mTOR
FKBP
Autophagy
Apoptosis
Bacterial
|
Cancer
|
|
Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities .
|
-
- HY-50895A
-
|
ZD-1839 hydrochloride
|
EGFR
|
Cancer
|
|
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .
|
-
- HY-19992
-
|
Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP
|
Hexokinase
Apoptosis
Autophagy
|
Cancer
|
|
3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities .
|
-
- HY-10999S2
-
|
GSK1120212-13C,d3; JTP-74057-13C,d3
|
Isotope-Labeled Compounds
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
|
-
- HY-N0484
-
|
|
Autophagy
Mitophagy
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc .
|
-
- HY-10162S1
-
|
AZD2281-d8; KU0059436-d8
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-17471AR
-
|
1,1-Dimethylbiguanide hydrochloride (Standard)
|
AMPK
Autophagy
Mitophagy
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin (hydrochloride) (Standard) is the analytical standard of Metformin (hydrochloride). This product is intended for research and analytical applications. Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy .
|
-
- HY-16592
-
|
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus . Brefeldin A is also an autophagy and mitophagy inhibitor . Brefeldin A is a CRISPR/Cas9 activator . Brefeldin A inhibits HSV-1 and has anti-cancer activity .
|
-
- HY-101840A
-
|
L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride
|
TRP Channel
Autophagy
COX
Prostaglandin Receptor
Na+/H+ Exchanger (NHE)
|
Inflammation/Immunology
Cancer
|
|
EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma .
|
-
- HY-135825
-
|
|
Autophagy
|
Neurological Disease
|
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment .
|
-
- HY-139535
-
|
CG-806
|
FLT3
Btk
Apoptosis
|
Cancer
|
|
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .
|
-
- HY-101535
-
|
|
Atg8/LC3
MMP
|
Cancer
|
|
ARP101 is a potent and selective inhibitor matrix metalloproteinase-2 (MMP-2). ARP101 induces autophagy-associated cell death in cancer cells. ARP101 is effective in inducing the formation of autophagosome and conversion of LC3I into LC3II .
|
-
- HY-144782
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
|
-
- HY-144779
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
|
-
- HY-144782A
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC10-IN-2 hydrochloride (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 hydrochloride modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
|
-
- HY-100932
-
ML-9
2 Publications Verification
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity . ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively . ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation .
|
-
- HY-B0006
-
-
- HY-13418A
-
|
Compound C; BML-275
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599) .
|
-
- HY-12481
-
|
|
PI3K
Autophagy
|
Cancer
|
|
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
|
-
- HY-10197
-
|
SL-2052; KY-12420
|
Organoid
PI3K
Polo-like Kinase (PLK)
Autophagy
Antibiotic
|
Cancer
|
|
Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively .
|
-
- HY-117985
-
|
DA-1229
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
Inflammation/Immunology
|
|
Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-161257
-
|
|
Autophagy
|
Cancer
|
|
CDC20-IN-1 (Compound E1) is a specific inhibitor of CDC20 and can be used in triple-negative breast cancer research. CDC20-IN-1 can induce autophagy in cancer cells and inhibit MDA-MB-231 cell proliferation, with an IC50 value of 1.43 μM .
|
-
- HY-101840
-
-
- HY-14266
-
|
TMC120; R147681
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
|
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
|
-
- HY-B0372A
-
|
|
SARS-CoV
Autophagy
HIV
|
Metabolic Disease
|
|
Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions .
|
-
- HY-13630A
-
|
BMY-40481 disodium
|
Topoisomerase
Autophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-10586
-
-
- HY-N0712
-
|
|
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function .
|
-
- HY-N1416
-
|
|
|
|
|
Pogostone is isolated from patchouli oil with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy .
|
-
- HY-10162S3
-
|
AZD2281-d4-1; KU0059436-d4-1
|
Isotope-Labeled Compounds
PARP
Autophagy
Mitophagy
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Cancer
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Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
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- HY-B0116
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- HY-B0116A
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- HY-10218S
-
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RAD001-d4; SDZ-RAD-d4
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mTOR
FKBP
Autophagy
Apoptosis
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Cancer
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Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].
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- HY-103157
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NSC168807
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Autophagy
Ferroptosis
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Cardiovascular Disease
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PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice .
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- HY-W040129
-
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Bacterial
Fungal
Apoptosis
Antibiotic
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Infection
Cancer
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Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor .
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- HY-117985B
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DA-1229 tartrate
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Dipeptidyl Peptidase
Autophagy
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Metabolic Disease
Inflammation/Immunology
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Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
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- HY-131257
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Drug Metabolite
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Others
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Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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- HY-133779
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Drug Metabolite
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Others
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Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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- HY-118160
-
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NSC 73233
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NO Synthase
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Inflammation/Immunology
Cancer
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PPM-18 (NSC 73233), a potent anti-inflammatory agent, inhibits nitric oxide synthase expression. PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter . PPM-18, an analog of Vitamin K, induces autophagy and apoptosis in bladder cancer cells through ROS and AMPK signaling pathways .
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- HY-12855
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Autophagy
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Cancer
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Lys01, a dimeric form of Chloroquine (HY-17589A), is an autophagy inhibitor. Lys01 inhibits cell viability of 1205Lu, c8161, LN229, HT-29 cells with IC50s of 3.6, 3.8, 7.9, 6.0 μM. Lys01 can be used for anticancer research .
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- HY-114569
-
|
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Ras
Cyclin G-associated Kinase (GAK)
Autophagy
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Cancer
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6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase) .
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- HY-N0585
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(Rac)-NCTD
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Endogenous Metabolite
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Cancer
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(Rac)-Norcantharidin ((Rac)-NCTD) is the isoform of Norcantharidin, which is a synthetic and demethylated anticancer agent derived from Cantharidin (HY-N0209). Norcantharidin has lighter side effects and stronger bioactivity than Cantharidin. And Norcantharidin inhibits cell proliferation, migration and metastasis, and causes apoptosis and autophagy .
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- HY-137506
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- HY-154910
-
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mTOR
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Cancer
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CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy ,with an IC50 is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study .
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- HY-128477
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Autophagy enhancer-67 inner salt
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Autophagy
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Neurological Disease
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AUTEN-67 (inner salt), the inner salt form of AUTEN-67 (HY-117924), is an orally active autophagy-enhancing agent and MTMR14 inhibitor with potent antiaging and neuroprotective effects. AUTEN-67 (inner salt) hampers the progression of neurodegenerative symptoms in a drosophila model of Huntington's disease .
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- HY-12794
-
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PI3K
Autophagy
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Neurological Disease
Cancer
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Vps34-PIK-III is an orally active and selective VPS34 inhibitor (IC50=18 nM). Vps34-PIK-III effectively inhibits autophagy and can be used as a molecular tool. vps34-PIK-III is also a PI3K inhibitor that inhibits the expression of genes in liver cancer stem cells (CSCs) .
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- HY-10249
-
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Akt
AMPK
Autophagy
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Cancer
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GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation .
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- HY-12034
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WYE-354
5 Publications Verification
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mTOR
Autophagy
Apoptosis
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Cancer
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WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro .
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- HY-B0968
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Autophagy
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Cardiovascular Disease
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Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
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- HY-100558
-
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BafA1
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Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
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Infection
Cancer
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Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H +-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis .
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- HY-B0968A
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Autophagy
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Cardiovascular Disease
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Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
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- HY-13636
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ICI 182780; ZD 9238; ZM 182780
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Estrogen Receptor/ERR
Autophagy
Apoptosis
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Cancer
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Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
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- HY-19808
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- HY-Y1269D
-
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Salmiac, for molecular biology
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Biochemical Assay Reagents
Autophagy
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Cancer
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Ammonium chloride, for molecular biology (Salmiac, for molecular biology) is ammonium chloride that can be used for molecular biology research. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
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- HY-10181
-
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BMS-354825
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Bcr-Abl
Src
Autophagy
Apoptosis
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Cancer
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Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
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- HY-10181A
-
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BMS-354825 hydrochloride
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Bcr-Abl
Src
Autophagy
Apoptosis
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Cancer
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Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
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- HY-B0736A
-
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FI7056
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Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
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Infection
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Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
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- HY-B1490
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Serotonin Transporter
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
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- HY-126147
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HDAC
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Cancer
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J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1 .
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- HY-122614
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S29434
2 Publications Verification
NMDPEF
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Autophagy
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Neurological Disease
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S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production .
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- HY-137742
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ULK
Autophagy
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Cancer
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SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research .
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- HY-10181B
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BMS-354825 monohydrate
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Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
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- HY-B1490A
-
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Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects .
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- HY-B0736
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- HY-19312S
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PI3K
Autophagy
Mitophagy
Endogenous Metabolite
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Cancer
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3-Methyladenine-d3 is the deuterium labeled 3-Methyladenine[1]. 3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[2].
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- HY-100932A
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Myosin
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Cancer
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ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity . ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively . ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation .
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- HY-135318
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NBDHEX
1 Publications Verification
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Apoptosis
Autophagy
Glutathione S-transferase
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Cancer
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NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor .
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- HY-155182
-
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HDAC
Autophagy
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Neurological Disease
Inflammation/Immunology
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HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain .
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- HY-A0061
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Trifluorothymidine; 5-Trifluorothymidine; TFT
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Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
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Cancer
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Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
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- HY-17589
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- HY-N0567
-
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Safflomin A; HSYA
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Apoptosis
Autophagy
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Cardiovascular Disease
Cancer
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Hydroxysafflor yellow A (Safflomin A) is a natural product of flavonoids isolated from safflower. Hydroxysafflor yellow A can inhibit cell proliferation and promote apoptosis through the autophagy pathway. Hydroxysafflor yellow A has anti-inflammatory, antioxidant and antitumor effects. Hydroxysafflor yellow A can be used in the study of cardiovascular disease .
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- HY-Y0152
-
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(8R,9S)-Cinchonine; LA40221
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Apoptosis
Parasite
Autophagy
Caspase
Calcium Channel
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Others
Inflammation/Immunology
Cancer
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Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
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- HY-12661A
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PERK
Autophagy
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Cancer
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AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy .
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- HY-17589A
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- HY-17589B
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- HY-W011209
-
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Riboprine
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Autophagy
Endogenous Metabolite
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Cancer
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N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity .
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- HY-146684
-
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HDAC
Autophagy
Apoptosis
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Cancer
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HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
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- HY-19551
-
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ApoG2
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Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy . Apogossypolone also has antifungal activity .
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- HY-146390
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Autophagy
Reactive Oxygen Species
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Cancer
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Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer .
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- HY-10224A
-
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LBH589 lactate; NVP-LBH589 lactate
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HDAC
HIV
Autophagy
Apoptosis
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Infection
Cancer
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Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma .
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- HY-151487
-
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Sirtuin
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Neurological Disease
Metabolic Disease
Cancer
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CypD-IN-3 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-3 has CypD affinity with an IC50 value of 0.01 μM. CypD-IN-3 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .
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- HY-151488
-
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Sirtuin
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Neurological Disease
Metabolic Disease
Cancer
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CypD-IN-4 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-4 has CypD affinity with an IC50 value of 0.057 μM. CypD-IN-4 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .
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- HY-149344
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Apoptosis
Autophagy
EGFR
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Cancer
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Anticancer agent 133 (compound Rh2) is an anti-cancer agent with cytotoxic and antimetastatic activities. Anticancer agent 133 induces cell cycle arrest, apoptosis, and autophagy. Anticancer agent 133 also inhibits cell metastasis via suppression of EGFR expression mediated by FAK-regulated integrin β1 .
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- HY-156432
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Anaplastic lymphoma kinase (ALK)
mTOR
PARP
Caspase
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Cancer
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ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies .
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- HY-Y1269C
-
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Salmiac, for cell culture
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Biochemical Assay Reagents
Autophagy
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Others
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Ammonium chloride, for cell culture (Salmiac, for cell culture) is a reagent that can be used in cell culture to provide a source of nitrogen. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
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- HY-11109
-
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TAK-242; CLI-095
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Toll-like Receptor (TLR)
TNF Receptor
Interleukin Related
Autophagy
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Inflammation/Immunology
Cancer
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Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases .
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- HY-15206
-
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Glyburide
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Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
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Metabolic Disease
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Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
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- HY-50895
-
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ZD1839
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EGFR
Autophagy
Apoptosis
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Cancer
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Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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- HY-100663
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EGFR
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Others
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Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
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- HY-138779
-
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Autophagy
RIP kinase
Apoptosis
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Inflammation/Immunology
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ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds with N-terminal domain of TRADD (TRADD-N), disrupting its binding to both TRADD-C and TRAF2. ICCB-19 hydrochloride is indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and the degradation of long-lived proteins .
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- HY-50895S1
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ZD1839-d6
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EGFR
Autophagy
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Cancer
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Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
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- HY-50895B
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ZD 1839 dihydrochloride
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Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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- HY-B0968S
-
|
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Autophagy
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Cardiovascular Disease
|
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Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
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- HY-10969
-
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GX15-070 Mesylate
|
Bcl-2 Family
Autophagy
Parasite
|
Infection
Cancer
|
|
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
|
-
- HY-50856
-
|
INCB18424
|
JAK
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
|
-
- HY-N6939
-
|
|
HBV
Fungal
Apoptosis
Autophagy
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes . Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy .
|
-
- HY-N0047
-
|
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
|
-
- HY-14374
-
GPP78
1 Publications Verification
CAY10618
|
NAMPT
Autophagy
|
Inflammation/Immunology
Cancer
|
|
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects .
|
-
- HY-10969A
-
|
GX15-070
|
Bcl-2 Family
Autophagy
Parasite
|
Infection
Cancer
|
|
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
|
-
- HY-Y1362
-
|
|
|
|
|
Ethyl pyruvate is a simple derivative of the endogenous metabolite pyruvate. Ethyl pyruvate is an HMGB1 release inhibitor. Ethyl pyruvate can induce apoptosis by autophagy. Ethyl pyruvate has anti-inflammatory, antioxidant and anti-tumor activity. Ethyl pyruvate can be used in the study of neurodegenerative diseases such as Alzheimer's and Parkinson's disease .
|
-
- HY-19934A
-
|
TAS-117 hydrochloride
|
Akt
Apoptosis
Autophagy
|
Cancer
|
|
Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
|
-
- HY-19934
-
|
TAS-117
|
Akt
Apoptosis
Autophagy
|
Cancer
|
|
Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
|
-
- HY-105037
-
|
IPP-201101
|
Autophagy
|
Inflammation/Immunology
|
|
Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
|
-
- HY-149829
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Antitumor agent-97 (compound 42) is an anticancer agent. Antitumor agent-97 can effectively inhibit the proliferation and autophagy of MGC 803 cells, and induce apoptosis. Antitumor agent-97 also enhances ROS accumulation in MGC 803 cells. Antitumor agent-97 can be used in cancer research .
|
-
- HY-118032
-
|
|
Apoptosis
Autophagy
JNK
ERK
|
Cancer
|
|
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice .
|
-
- HY-155747
-
|
|
Autophagy
|
Cancer
|
|
FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research .
|
-
- HY-161125
-
|
|
Others
|
Others
|
|
(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .
|
-
- HY-118630
-
|
|
PIKfyve
Autophagy
|
Cancer
|
|
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca 2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells .
|
-
- HY-115570
-
|
GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
|
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
|
-
- HY-B0223
-
-
- HY-12248
-
|
CB-839
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
|
-
- HY-12248A
-
|
CB-839 hydrochloride
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
|
-
- HY-156278
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cell cycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells .
|
-
- HY-162344
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Ir-CA is an antitumor agent. Ir-CA can accumulate in mitochondria and induces mitochondria dysfunction. Ir-CA induces apoptosis and autophagy. Ir-CA initiates mitophagy and cell cycle arrest to kill Cisplatin (HY-17394)-resistant A549R cells. Ir-CA can effectively inhibit metastasis by inhibiting MMP-2/MMP-9 .
|
-
- HY-10218R
-
|
RAD001 (Standard); SDZ-RAD (Standard)
|
mTOR
FKBP
Autophagy
Apoptosis
Bacterial
|
Cancer
|
|
Everolimus (Standard) is the analytical standard of Everolimus. This product is intended for research and analytical applications. Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities .
|
-
- HY-16160
-
|
|
Autophagy
ICMT
|
Cancer
|
|
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research .
|
-
- HY-15433
-
|
JNJ-26481585
|
HDAC
Apoptosis
Autophagy
|
Cancer
|
|
Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity . Quisinostat can induce autophagy in neuroblastoma cells .
|
-
- HY-14266S
-
|
TMC120-d11; R147681-d11
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
|
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
|
-
- HY-10971A
-
|
MLN 8237 sodium
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
|
-
- HY-B0372AS
-
|
|
Isotope-Labeled Compounds
SARS-CoV
Autophagy
HIV
|
Metabolic Disease
|
|
Bromhexine-d3 (hydrochloride) is deuterium labeled Bromhexine (hydrochloride). Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions[1][2][3][4].
|
-
- HY-151489
-
|
|
Sirtuin
|
Neurological Disease
Metabolic Disease
Cancer
|
|
CypD-IN-1 is a potent and subtype-selective cyclophilin E (CypE) inhibitor. CypD-IN-1 has CypE affinity with IC50 and Ki values of 0.013 μM and 0.072 μM, respectively. CypD-IN-1 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .
|
-
- HY-13027
-
|
GSI-IX
|
Organoid
γ-secretase
Amyloid-β
Autophagy
Notch
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment .
|
-
- HY-B0006S
-
|
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
|
-
- HY-B0006S1
-
|
BM 14190-d4
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
|
-
- HY-B0116S
-
-
- HY-B0006S2
-
-
- HY-13417S
-
|
Acadesine-13C2,15N; AICA Riboside-13C2,15N
|
Isotope-Labeled Compounds
|
Others
|
|
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N)is the 13C and 15N labeledAICAR(HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
|
-
- HY-157320
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
|
-
- HY-B0006R
-
|
BM 14190 (Standard)
|
Adrenergic Receptor
Autophagy
Bacterial
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol (Standard) is the analytical standard of Carvedilol. This product is intended for research and analytical applications. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
|
-
- HY-10971
-
|
MLN 8237
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
|
-
- HY-15142
-
|
Hydroxydaunorubicin hydrochloride
|
Topoisomerase
ADC Cytotoxin
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
|
-
- HY-12203
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria .
|
-
- HY-N2500
-
|
|
Microtubule/Tubulin
Apoptosis
Autophagy
|
Infection
Cardiovascular Disease
|
|
Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from Anthriscus sylvestris. Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis . Deoxypodophyllotoxin induces cell autophagy and apoptosis . Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons .
|
-
- HY-125927
-
|
8-NH2-Ado
|
DNA/RNA Synthesis
Akt
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity .
|
-
- HY-13636S
-
|
ICI 182780-d3; ZD 9238-d3; ZM 182780-d3
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
|
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
|
-
- HY-10295A
-
|
|
Organoid
p38 MAPK
Autophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity . SB202190 hydrochloride induces autophagy .
|
-
- HY-147942
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
|
-
- HY-105037A
-
|
IPP-201101 TFA
|
Autophagy
|
Inflammation/Immunology
|
|
Forigerimod TFA (IPP-201101 TFA) is a CD4 T-cell modulator. Forigerimod TFA is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod TFA can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
|
-
- HY-152228
-
|
|
Histone Methyltransferase
Autophagy
|
Cancer
|
|
SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer .
|
-
- HY-Y1269I
-
|
Salmiac (Pharmaceutical primary standard, USP)
|
Biochemical Assay Reagents
Autophagy
|
Others
|
|
Ammonium chloride United States Pharmacopeia (USP) Reference Standard (Salmiac, Pharmaceutical primary standard, USP) is a reagent that can be used in cell culture to provide a source of nitrogen. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
|
-
- HY-132242
-
|
SFN-NAC
|
HDAC
Apoptosis
|
Cancer
|
|
DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC) is an orally active HDAC inhibitor and metabolite of sulforaphane (HY-13755) with longer half-life and better blood-brain barrier permeability. DL-Sulforaphane N-acetyl-L-cysteine activates autophagy-mediated downregulation of α-tubulin expression through the ERK pathway and can be used in cancer research .
|
-
- HY-10201A
-
|
Bay 43-9006 Tosylate
|
Raf
VEGFR
FLT3
Autophagy
Ferroptosis
Apoptosis
|
Cancer
|
|
Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator .
|
-
- HY-10201
-
|
Bay 43-9006
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
|
-
- HY-50895S2
-
|
|
Isotope-Labeled Compounds
EGFR
Autophagy
|
Cancer
|
|
Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
|
-
- HY-B1490AS
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
|
-
- HY-B1490S
-
|
|
Serotonin Transporter
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
|
-
- HY-W016409
-
|
Ethyl protocatechuate
|
HIF/HIF Prolyl-Hydroxylase
Reactive Oxygen Species
NO Synthase
Autophagy
Apoptosis
|
Metabolic Disease
Cancer
|
|
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect .
|
-
- HY-117025A
-
|
Keramamine A hydrochloride
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1 .
|
-
- HY-B1490AS1
-
|
|
Serotonin Transporter
Isotope-Labeled Compounds
Apoptosis
Autophagy
|
Others
|
|
Imipramine-d4 is deuterium labeled Imipramine. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
|
-
- HY-B1490S1
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Imipramine-d3 (hydrochloride) is deuterium labeled Imipramine (hydrochloride). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
|
-
- HY-117025
-
|
Keramamine A
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1 .
|
-
- HY-152100
-
|
|
Autophagy
|
Cancer
|
|
CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo .
|
-
- HY-157165
-
|
|
Microtubule/Tubulin
PARP
|
Cancer
|
|
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase .
|
-
- HY-B1232
-
|
Su-4885
|
Endogenous Metabolite
Cytochrome P450
Autophagy
|
Neurological Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
|
-
- HY-15425
-
|
Sphingosine Kinase 1 Inhibitor II
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy .
|
-
- HY-15425B
-
|
Sphingosine Kinase 1 Inhibitor II hydrochloride
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy .
|
-
- HY-B0968R
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine (dihydrochloride) (Standard) is the analytical standard of Trimetazidine (dihydrochloride). This product is intended for research and analytical applications. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
|
-
- HY-10029
-
|
Rebemadlin
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
|
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas .
|
-
- HY-10514
-
|
|
PDK-1
IKK
Autophagy
|
Cancer
|
|
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
|
-
- HY-10115
-
|
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
|
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy .
|
-
- HY-10115A
-
|
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
|
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy .
|
-
- HY-15893
-
|
Dimethyloxallyl Glycine
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Cancer
|
|
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .
|
-
- HY-12286
-
|
|
Proteasome
Apoptosis
Autophagy
Caspase
Bcl-2 Family
NF-κB
PARP
|
Cancer
|
|
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α .
|
-
- HY-N1372A
-
|
|
HIV
FAK
Apoptosis
Autophagy
|
Infection
Cancer
|
|
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
|
-
- HY-15142A
-
|
Hydroxydaunorubicin
|
ADC Cytotoxin
Antibiotic
Bacterial
Topoisomerase
AMPK
HIV
Autophagy
Mitophagy
Apoptosis
HBV
|
Infection
Cancer
|
|
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy . Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM .
|
-
- HY-10029A
-
|
(Rac)-Rebemadlin
|
MDM-2/p53
Autophagy
Apoptosis
E1/E2/E3 Enzyme
|
Cancer
|
|
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas .
|
-
- HY-N2199
-
|
|
|
|
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .
|
-
- HY-156348
-
|
|
Monoamine Oxidase
Autophagy
Apoptosis
Cholinesterase (ChE)
|
Neurological Disease
|
|
MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease .
|
-
- HY-161083
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-50895R
-
|
ZD1839 (Standard)
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-B1490R
-
|
|
Serotonin Transporter
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Imipramine (hydrochloride) (Standard) is the analytical standard of Imipramine (hydrochloride). This product is intended for research and analytical applications. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects .
|
-
- HY-10295
-
|
|
Organoid
p38 MAPK
Autophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits . SB202190 induces autophagy .
|
-
- HY-13259
-
MG-132
Maximum Cited Publications
872 Publications Verification
Z-Leu-Leu-Leu-al; MG132
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
|
MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis .
|
-
- HY-14598
-
|
Stilbestrol
|
Estrogen Receptor/ERR
Apoptosis
Autophagy
|
Endocrinology
Cancer
|
|
Diethylstilbestrol (Stilbestrol) is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor. .
|
-
- HY-N2359
-
|
|
Beta-lactamase
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy .
|
-
- HY-N6979
-
|
20-Hydroxyecdysone
|
Caspase
Autophagy
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Serratula coronata which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP . Crustecdysone exhibits regulatory or protective roles in the cardiovascular system . Crustecdysone is an active metabolite of Ecdysone (HY-N0179) .
|
-
- HY-N0107
-
|
|
Apoptosis
Autophagy
mTOR
Akt
|
Cardiovascular Disease
|
|
Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR . Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis . Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction .
|
-
- HY-N0485
-
|
|
Autophagy
Mitophagy
|
Cardiovascular Disease
|
|
Liensinine Diperchlorate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlorate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlorate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc .
|
-
- HY-17589AS
-
-
- HY-103238
-
|
|
AMPK
STAT
Autophagy
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity .
|
-
- HY-17589S1
-
-
- HY-147941
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
|
-
- HY-124896
-
|
6-Geranylnaringenin; Mimulone
|
Phosphatase
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
- HY-13636R
-
|
ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
|
Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-157548
-
|
|
p62
Atg8/LC3
Autophagy
|
Cancer
|
|
Antitumor agent-133 (compound 4d) is a bis-isatin derivative, with activities against Huh1 (IC50=17.13 μM) and Huh7 (IC50=8.27 μM). Antitumor agent-133 induces cell autophagy and inhibits tumor growth through regulation of LC3BII, ATG5 and p62 proteins .
|
-
- HY-15425A
-
|
Sphingosine Kinase 1 Inhibitor II Citrate
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy .
|
-
- HY-B1232A
-
|
Su-4885 Tartrate
|
Endogenous Metabolite
Cytochrome P450
Autophagy
mTOR
|
Neurological Disease
Endocrinology
|
|
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression .
|
-
- HY-17589S
-
-
- HY-144449
-
|
|
mTOR
HDAC
Apoptosis
Autophagy
|
Cancer
|
|
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC) .
|
-
- HY-17589R
-
|
|
Parasite
Autophagy
SARS-CoV
Toll-like Receptor (TLR)
HIV
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Chloroquine (phosphate) (Standard) is the analytical standard of Chloroquine (phosphate). This product is intended for research and analytical applications. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM) .
|
-
- HY-12033
-
|
2-ME2; NSC-659853
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
- HY-122214
-
AC-73
3 Publications Verification
|
Autophagy
|
Cancer
|
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells . AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells .
|
-
- HY-10219S1
-
|
Sirolimus-13C,d3; AY-22989-13C,d3
|
Isotope-Labeled Compounds
|
Others
|
|
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) . Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
|
-
- HY-162460
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1/2 inhibitor (IC50: 0.11/0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .
|
-
- HY-13518
-
|
Astringenin; trans-Piceatannol
|
Syk
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Piceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI) . Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties . Piceatannol induces apoptosis in DLBCL cell lines . Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells .
|
-
- HY-143466
-
|
|
FAK
ULK
AMPK
Apoptosis
Autophagy
|
Cancer
|
|
ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer) .
|
-
- HY-147941A
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
|
-
- HY-12028
-
|
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
|
PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy .
|
-
- HY-B1077
-
|
R-16341
|
Calcium Channel
Dopamine Receptor
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca 2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml .
|
-
- HY-10224
-
|
LBH589; NVP-LBH589
|
HDAC
Autophagy
HIV
Apoptosis
|
Cancer
|
|
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities . Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells . Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma .
|
-
- HY-100490
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-100490B
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-10256A
-
|
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator .
|
-
- HY-151443
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-155520
-
|
|
Parasite
|
Infection
|
|
Antileishmanial agent-19 (Compound F27) is an antileishmanial agent, with a IC50 of 3.39 μM for L. donovani promastigotes. Antileishmanial agent-19 inhibits Leishmania prolyl-tRNA synthetase. Antileishmanial agent-19 inhibits host PI3K/Akt/CREB axis-mediated IL-10 secretion. Antileishmanial agent-19 induces autophagy-mediated apoptosis in L. donovani promastigotes. Antileishmanial agent-19 reduces parasite burden in L.d-infected animals .
|
-
- HY-156237
-
|
|
Autophagy
|
Others
|
|
Beclin1-ATG14L interaction inhibitor 1 (com 19) is a selective Beclin1-ATG14L interaction inhibitor. This protein interaction mechanism specifically targets complex I of the lipid kinase VPS34 without affecting complex II. Because the integrity of VPS34 complex II depends on the Beclin 1-UVRAG interaction. Beclin1-ATG14L interaction inhibitor 1 can disrupt the formation of VPS34 complex I and inhibit autophagy, but does not affect complex II-related vesicle transport .
|
-
- HY-50907
-
|
|
Bcl-2 Family
Apoptosis
Autophagy
Mitophagy
|
Cancer
|
|
ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
- HY-101180
-
|
Ceramide 2
|
|
|
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation, autophagy and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss .
|
-
- HY-100490A
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-119016
-
SK1-I
1 Publications Verification
BML-258
|
SphK
|
Cancer
|
|
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .
|
-
- HY-119016A
-
|
BML-258 hydrochloride
|
SphK
|
Cancer
|
|
SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity .
|
-
- HY-135887
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
Autophagy
|
Cancer
|
|
ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect .
|
-
- HY-108462
-
ML-SA1
2 Publications Verification
|
Dengue virus
TRP Channel
Flavivirus
|
Infection
|
|
ML-SA1, as a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral .
|
-
- HY-144636
-
|
|
Atg4
Cathepsin
Phospholipase
Autophagy
|
Cancer
|
|
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
|
-
- HY-147039
-
|
NKP-1339 free base; IT-139 free base; KP-1339 free base
|
HSP
Autophagy
|
Cancer
|
|
BOLD-100 (NKP-1339; IT-139) free base is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution .
|
-
- HY-134050
-
|
Apt-1
|
RIP kinase
Autophagy
Apoptosis
Beclin1
Necroptosis
|
Inflammation/Immunology
|
|
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin .
|
-
- HY-B1324A
-
|
Ro 13-8996 free base
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-139426A
-
|
trans-ML-SI3
|
TRP Channel
Autophagy
|
Cancer
|
|
(rel)-ML-SI3 is the isomer of ML-SI3 (HY-139426). ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy .
|
-
- HY-P1098B
-
|
|
IKK
|
Inflammation/Immunology
|
|
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-155731
-
|
|
Influenza Virus
|
Infection
|
|
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM .
|
-
- HY-10256
-
|
SB 203580; RWJ 64809
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-18980
-
|
Mallotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
HIV
RABV
|
Infection
Cancer
|
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
|
-
- HY-10201S2
-
|
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
|
-
- HY-N6002
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 µM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer .
|
-
- HY-111373
-
|
|
mTOR
Autophagy
|
Cancer
|
|
RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
|
-
- HY-10182
-
|
CHIR-99021; CT99021
|
Organoid
GSK-3
Wnt
β-catenin
Autophagy
|
Metabolic Disease
Cancer
|
|
Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy .
|
-
- HY-10182B
-
|
CHIR-99021 trihydrochloride; CT99021 trihydrochloride
|
Organoid
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy .
|
-
- HY-B1324
-
|
Ro 13-8996
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-100490S
-
|
|
Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
|
-
- HY-113914
-
|
Elraglusib
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
|
9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents .
|
-
- HY-146349
-
|
|
PROTACs
EGFR
Autophagy
|
Cancer
|
|
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .
|
-
- HY-108016
-
|
Encordin
|
Src
PI3K
JNK
STAT
EGFR
Apoptosis
Autophagy
|
Cancer
|
|
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
|
-
- HY-18676
-
|
|
Integrin
Autophagy
Apoptosis
|
Cancer
|
|
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain) . OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner . OSU-T315 causes cell death through apoptosis and autophagy .
|
-
- HY-12795
-
|
|
PI3K
Autophagy
|
Cancer
|
|
Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns(3)P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy .
|
-
- HY-145931
-
|
|
mTOR
Autophagy
|
Cancer
|
|
CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo .
|
-
- HY-12033S2
-
|
2-ME2-d5; NSC-659853-d5
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
|
|
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
|
-
- HY-N0568
-
|
Asiaticoside A
|
Endogenous Metabolite
Apoptosis
Autophagy
Keap1-Nrf2
p38 MAPK
Caspase
|
Cardiovascular Disease
Others
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB [5][6], exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity . Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
|
-
- HY-10182A
-
|
CHIR-99021 monohydrochloride; CT99021 monohydrochloride
|
Organoid
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy .
|
-
- HY-N2181
-
|
|
|
|
|
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD) .
|
-
- HY-136351
-
|
|
Autophagy
|
Cancer
|
|
THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines .
|
-
- HY-10224S
-
|
LBH589-d4; NVP-LBH589-d4
|
HDAC
Autophagy
HIV
Apoptosis
|
Cancer
|
|
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
|
-
- HY-13260A
-
|
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity .
|
-
- HY-10224S1
-
|
LBH589-d4 hydrochloride; NVP-LBH589-d4 hydrochloride
|
Isotope-Labeled Compounds
HDAC
Autophagy
HIV
Apoptosis
|
Cancer
|
|
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
|
-
- HY-N3248
-
|
Momordicacoside G
|
Endogenous Metabolite
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Momordicoside G (Momordicacoside G) is an orally active cucurbitane-type triterpene glycoside. Momordicoside G selectively induces apoptosis of M1-like macrophages, without affecting M2-like macrophages. Momordicoside G reduces intracellular ROS levels and promotes autophagy. Momordicoside G also has anticancer activity, inhibiting the growth of cancer cell lines. Momordicoside G stimulates M2-associated lung injury repair and prevents inflammatory lung cancer injury .
|
-
- HY-149262
-
|
|
CDK
DYRK
Autophagy
|
Cancer
|
|
CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research .
|
-
- HY-10587
-
|
|
Histone Methyltransferase
Autophagy
|
Cancer
|
|
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells .
|
-
- HY-12033S
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
|
-
- HY-108239
-
|
|
Histone Methyltransferase
Autophagy
|
Cancer
|
|
BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells .
|
-
- HY-12033S1
-
|
2-ME2-13C6; NSC-659853-13C6
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
|
-
- HY-100008
-
|
NIK333
|
RAR/RXR
SphK
Autophagy
HCV
|
Infection
Cancer
|
|
Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1 . Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression . Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM .
|
-
- HY-50907S
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
- HY-N0103
-
|
|
Autophagy
Apoptosis
PI3K
Akt
Influenza Virus
|
Infection
Inflammation/Immunology
Cancer
|
|
Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer .
|
-
- HY-N0103A
-
|
|
Autophagy
Apoptosis
PI3K
Akt
Influenza Virus
|
Infection
Inflammation/Immunology
Cancer
|
|
Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer .
|
-
- HY-N0281
-
|
7,8-Dihydroxycoumarin
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Inflammation/Immunology
Cancer
|
|
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
|
-
- HY-N3387
-
|
|
Apoptosis
NF-κB
Akt
MMP
|
Inflammation/Immunology
Cancer
|
|
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .
|
-
- HY-13270
-
|
E7010
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-13757A
-
|
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-139426
-
|
ML-SI3 (cis/trans mix)
|
Parasite
TRP Channel
|
Cardiovascular Disease
Neurological Disease
|
|
ML-SI3 is a mixture of cis/trans ML-SI3. ML-SI3 is a TRPML channel modulator. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 µM and 1.7 µM, respectively. ML-SI3 is also able to activate TRPML2 and TRPML3 with EC50s of 3.3-9.4 μM and 29 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy.
|
-
- HY-148409
-
|
|
Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
|
-
- HY-13757
-
|
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-151137
-
|
|
mTOR
HSP
Apoptosis
Autophagy
|
Cancer
|
|
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer .
|
-
- HY-13757AS1
-
|
ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
|
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
|
Cancer
|
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
|
-
- HY-13757AR
-
|
ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (Standard) is the analytical standard of Tamoxifen. This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-13757S
-
|
ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride
|
Apoptosis
Estrogen Receptor/ERR
Autophagy
HSP
Isotope-Labeled Compounds
|
Cancer
|
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-134807
-
|
|
P2X Receptor
5-HT Receptor
Autophagy
|
Cancer
|
|
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-Y1269C
-
|
Salmiac, for cell culture
|
Biochemical Assay Reagents
|
|
Ammonium chloride, for cell culture (Salmiac, for cell culture) is a reagent that can be used in cell culture to provide a source of nitrogen. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
|
-
- HY-Y1269H
-
|
Salmiac, meets analytical specification of Ph. Eur. BP USP FCC
|
Buffer Reagents
|
|
Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC (Salmiac, meets analytical specification of Ph. Eur. BP USP FCC) can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
|
-
- HY-Y1269D
-
|
Salmiac, for molecular biology
|
Buffer Reagents
|
|
Ammonium chloride, for molecular biology (Salmiac, for molecular biology) is ammonium chloride that can be used for molecular biology research. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
|
-
- HY-Y1269I
-
|
Salmiac (Pharmaceutical primary standard, USP)
|
Biochemical Assay Reagents
|
|
Ammonium chloride United States Pharmacopeia (USP) Reference Standard (Salmiac, Pharmaceutical primary standard, USP) is a reagent that can be used in cell culture to provide a source of nitrogen. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-105037A
-
|
IPP-201101 TFA
|
Autophagy
|
Inflammation/Immunology
|
|
Forigerimod TFA (IPP-201101 TFA) is a CD4 T-cell modulator. Forigerimod TFA is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod TFA can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
|
-
- HY-P1098B
-
|
|
IKK
|
Inflammation/Immunology
|
|
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-105037
-
|
IPP-201101
|
Autophagy
|
Inflammation/Immunology
|
|
Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-152228
-
|
|
Histone Methyltransferase
Autophagy
|
Cancer
|
|
SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-118620
-
-
-
- HY-13417A
-
-
-
- HY-13417
-
-
-
- HY-N8530
-
-
-
- HY-N1244
-
-
-
- HY-N2117
-
-
-
- HY-121532
-
-
-
- HY-163001
-
|
|
Microorganisms
Source classification
|
Autophagy
p62
Atg8/LC3
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
-
- HY-13251
-
-
-
- HY-N12277
-
-
-
- HY-100599
-
-
-
- HY-19312
-
-
-
- HY-N2593
-
-
-
- HY-10219
-
-
-
- HY-12048
-
-
-
- HY-N0112
-
-
-
- HY-N3913
-
-
-
- HY-13629
-
-
-
- HY-N2959
-
-
-
- HY-N0072
-
-
-
- HY-163178
-
-
-
- HY-N0410
-
-
-
- HY-N0484
-
-
-
- HY-16592
-
-
-
- HY-N0712
-
-
-
- HY-N0585
-
-
-
- HY-100558
-
-
-
- HY-N0567
-
-
-
- HY-Y0152
-
-
-
- HY-W011209
-
-
-
- HY-N6939
-
-
-
- HY-N0047
-
-
-
- HY-15142
-
-
-
- HY-N2500
-
-
-
- HY-125927
-
-
-
- HY-W016409
-
-
-
- HY-117025A
-
-
-
- HY-117025
-
-
-
- HY-B1232
-
-
-
- HY-N1372A
-
-
-
- HY-15142A
-
-
-
- HY-N2359
-
-
-
- HY-N6979
-
-
-
- HY-N0107
-
-
-
- HY-N0485
-
-
-
- HY-124896
-
|
6-Geranylnaringenin; Mimulone
|
Paulownia tomentosa (Thunb.) Steud.
Scrophulariaceae
Plants
|
Phosphatase
Apoptosis
Autophagy
|
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
-
- HY-B1232A
-
-
-
- HY-12033
-
-
-
- HY-13518
-
-
-
- HY-18980
-
|
Mallotoxin; NSC 56346; NSC 94525
|
Structural Classification
Chalcones
Flavonoids
Classification of Application Fields
Source classification
Phenols
Polyphenols
Euphorbiaceae
Plants
Disease Research Fields
Mallotus philippensis
Cancer
|
PKC
Autophagy
Apoptosis
HIV
RABV
|
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
|
-
- HY-N6002
-
-
- HY-108016
-
-
- HY-N0568
-
-
- HY-N3248
-
-
- HY-N0103
-
-
- HY-N0103A
-
-
- HY-N0281
-
|
7,8-Dihydroxycoumarin
|
Classification of Application Fields
Daphne
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
Disease Research Fields
Cancer
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
|
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
|
-
- HY-N3387
-
|
|
Natural Products
Classification of Application Fields
Leguminosae
Source classification
Phenols
Polyphenols
Plants
Inflammation/Immunology
Disease Research Fields
Glycyrrhiza uralensis Fisch.
|
Apoptosis
NF-κB
Akt
MMP
|
|
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-110228
-
|
|
|
Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
|
-
-
- HY-15531S
-
|
|
|
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
|
-
-
- HY-12057S
-
|
|
|
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
|
-
-
- HY-12057S1
-
|
|
|
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
|
-
-
- HY-13629S1
-
|
|
|
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
|
-
-
- HY-15206S
-
|
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Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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- HY-15206S1
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Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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- HY-10999S
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Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-135811S
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Desethyl chloroquine-d4 is the deuterium labeled Desethyl chloroquine. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity[1][2].
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- HY-135811S1
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Desethyl chloroquine-d5 is deuterium labeled Desethyl chloroquine. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity[1][2].
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- HY-10999S1
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Trametinib- 13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-10219S
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Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
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- HY-10999S2
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Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-10162S1
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Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
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- HY-10162S3
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Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
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- HY-10218S
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Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].
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- HY-19312S
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3-Methyladenine-d3 is the deuterium labeled 3-Methyladenine[1]. 3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[2].
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- HY-50895S1
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Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
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- HY-B0968S
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Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
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- HY-14266S
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Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
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- HY-B0372AS
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Bromhexine-d3 (hydrochloride) is deuterium labeled Bromhexine (hydrochloride). Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions[1][2][3][4].
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- HY-B0006S
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Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
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- HY-B0006S1
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Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
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- HY-B0116S
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Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis[1][2][3][4].
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- HY-B0006S2
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Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
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- HY-13417S
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AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N)is the 13C and 15N labeledAICAR(HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
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- HY-13636S
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Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
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- HY-50895S2
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Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
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- HY-B1490AS
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Imipramine-d6 is the deuterium labeled Imipramine hydrochloride. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
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- HY-B1490S
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Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
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- HY-B1490AS1
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Imipramine-d4 is deuterium labeled Imipramine. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
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- HY-B1490S1
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Imipramine-d3 (hydrochloride) is deuterium labeled Imipramine (hydrochloride). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
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- HY-17589AS
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1 Publications Verification
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Chloroquine-d5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
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- HY-17589S1
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Chloroquine-d4 (phosphate) is the deuterium labeled Chloroquine phosphate. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
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- HY-17589S
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Chloroquine-d5 (diphosphate) is the deuterium labeled Chloroquine (phosphate). Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
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- HY-10219S1
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Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) . Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
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- HY-10201S2
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1 Publications Verification
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Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
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- HY-100490S
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Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
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- HY-12033S2
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2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
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- HY-10224S
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Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
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- HY-10224S1
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Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
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- HY-12033S
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2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
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- HY-12033S1
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2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
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- HY-50907S
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ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
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- HY-13757AS1
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Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
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- HY-13757S
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Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
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