Atg8/LC3

Autophagy-related 8;

Autophagy-related 8 proteins (Atg8s) are one of the 62 highly conserved eukaryote-specific protein families. Whereas yeast and other fungal species have a single Atg8 gene, multicellular animals, green plants and some protists have several. Animal Atg8 proteins comprise three subfamilies: microtubule-associated protein 1 light chain 3 (MAP1LC3, hereafter referred to as LC3), γ-aminobutyric acid receptor-associated protein (GABARAP) and Golgi-associated ATPase enhancer of 16 kDa (GATE-16).

Atg8 family members are expressed in various tissues, where they participate in multiple cellular processes, such as intracellular membrane trafficking and autophagy. Their role in autophagy has been intensively studied. Atg8 proteins undergo a unique ubiquitin-like conjugation to phosphatidylethanolamine on the autophagic membrane, a process essential for autophagosome formation.

Atg8/LC3 Related Products (71):

By Effects:	Inhibitors (7) Ligand (1) Activators (21) Modulators (2) Inducers (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-175204

SHP2 protein degrader-3	Activator
SHP2 protein degrader-3 is a SHP2 AUTAC degrader. SHP2 protein degrader-3 shows dose-dependent SHP2 degradation ability (DC₅₀ = 3.22 μM) and anti-tumor activity (IC₅₀ = 5.59 μM) in HeLa cells. SHP2 protein degrader-3 induces degradation through the LC3-mediated autophagy pathway, which can be inhibited by lysosome inhibitors. SHP2 protein degrader-3 induces apoptosis in various cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells) (SHP2 Ligand : (HY-100388); LC3 Ligand: (HY-10542); Linker : (HY-128834)).

HY-132972

TrxR-IN-2	Activator
TrxR-IN-2 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 increases reactive oxidative species (ROS) levels and decreases mitochondrial transmembrane potential levels. TrxR-IN-2 triggers DNA damage via H2AX regulation, and induces autophagy via LC3, beclin-1, and p62 regulation. TrxR-IN-2 can be used for the research of drug-resistant hepatocellular carcinoma^[1].

HY-125535

OSU-53
OSU-53 is an orally active AMPK activator (EC₅₀: 0.3 μM) and a direct mTOR inhibitor. OSU-53 induces autophagy and increases conversion of LC3 I to LC3 II. OSU-53 also modulates energy homeostasis by suppressing fatty acid biosynthesis and shifting the metabolism to oxidation by up-regulating the expression of PGC1α and NRF-1. OSU-53 has antitumor activity in various tumor models, such as breast cancer and thyroid cancer.

HY-B0113AR

Omeprazole sodium (Standard)
Omeprazole (sodium) (Standard) is the analytical standard of Omeprazole (sodium). This product is intended for research and analytical applications. Omeprazole sodium (H 16868) is an orally active H⁺,K⁺-ATPase inhibitor and a proton pump inhibitor. Omeprazole sodium competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole sodium inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole sodium inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole sodium alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole sodium aslo has neuroprotective and antibacterial effects.

HY-W768347

Xylitol-¹³C₅
Xylitol-¹³C₅ (Xylite-¹³C₅) is the ¹³C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model.

HY-179049

EGFR/tubulin-IN-1	Activator
EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer.

HY-168891

LC3B recruiter 1
LC3B recruiter 1 (compound 33R) is an LC3B recruiter fragment. LC3B recruiter 1 directly interacts with LC3B with a K_D value of 2.87 µM.

HY-121546

ALLO-1
ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif.

HY-168347

TH152	Ligand
TH152 is a reversible, pan ligand for LC3/GABARAP with a K_D of 2 µM. LC3/GABARAP is an autophagy associated protein.

HY-176749

HUP-46	Inducer
HUP-46 is a BBB-penatrable modulator of αSyn dimerization and autophagy. HUP-46 reduces the ratio of pPP2A/PP2A, increases the autophagy marker LC3BII levels, and decreases αSyn dimerization. HUP-46 can be used for research of neurodegenerative diseases.

HY-B0113S1

Omeprazole-d₃-1
Omeprazole-d₃-1 is the deuterium labeled Omeprazole. Omeprazole-1 (H 16868) is an orally active H⁺,K⁺-ATPase inhibitor and a proton pump inhibitor. Omeprazole-1 competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole-1 inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole-1 inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole-1 alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole-1 aslo has neuroprotective and antibacterial effects.

HY-W142432S

Perfluoroundecanoic acid-¹³C₇
Perfluoroundecanoic acid-¹³C₇ is the ¹³C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation.

HY-170992

Autophagy agonist-1	Inducer
Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC₅₀s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells.

HY-183870

NCO-90	Activator
NCO-90 is a selective SIRT2 inhibitor with an IC₅₀ of 1.0 μM. NCO-90 induces Apoptosis via Caspase activation and mitochondrial superoxide anion production, and also induces Autophagic cell death by increasing LC3-II levels and autophagosome accumulation. NCO-90 exhibits anticancer activity against leukemia. NCO-90 can be used in research related to acute lymphoblastic leukemia and acute myeloid leukemia.

HY-P3148

Astin B
Astin B is a orally active and potent cyclic pentapeptide, that can be isolated from Aster tataricus. Astin B has hepatotoxic effects in vitro and in vivo and that hepatic injury was primarily mediated by apoptosis in a mitochondria/caspase-dependent manner. Astin B induces autophagy in L-02 cells, increases LC3-II and decreases p62 expression.

HY-157548

Antitumor agent-133
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-165539

SMER10
SMER10 is a small-molecule enhancer that can induce autophagy. SMER10 can increase the number of EGFP-LC3 positive autophagosoms in COS-7 and HeLa cells, promoting the conversion of LC3-I to autophagosome-associated LC3-II. SMER10 can efficiently promote the degradation of autophagy substrates, including the mutant huntingtin protein (EGFP-HDQ74) associated with Huntington's disease and the A53T α-synuclein protein associated with Parkinson's disease. SMER10 exerts neuroprotective effect.

HY-112774A

ICSN3250 hydrochloride	Activator
ICSN3250 hydrochloride is a halitulin analogue and a mTORC1 inhibitor. ICSN3250 hydrochloride directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 hydrochloride shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 hydrochloride specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 hydrochloride can be used for the study of cancer .

HY-W010201S1

Citronellol-d₃
Citronellol-d₃ ( (±)-Citronelloll-d₃) is the deuterium labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.

HY-162147

Nur77 modulator 3	Activator	99.01%
Nur77 modulator 3 is a Nur77 modulator. Nur77 modulator 3 induces Nur77 expression, inhibits hepatic stellate cells (HSCs) activation, and reduces extracellular matrix (ECM) deposition. Nur77 modulator 3 enhances Nur77-denpendent autophagic flux and significantly inhibits the mTORC1 signaling pathway. Nur77 modulator 3 ameliorates HSCs activation, inflammation and hepatic fibrosis in vivo.

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