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Atf4 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

1

Natural
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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-158202
    ATF4-IN-2

    		Epigenetic Reader Domain Neurological Disease
    ATF4-IN-2 (Compound 29) is a ATF4 inhibitor with a IC50 value of 47.71 nM. ATF4-IN-2 can be used in the study of neurodegenerative diseases .
    ATF4-IN-2
  • HY-158201
    ATF4-IN-1

    		Eukaryotic Initiation Factor (eIF) Neurological Disease
    ATF4-IN-1 (Compound 21) is an ATF4 inhibitor and also an eIF2B activator. ATF4-IN-1 can be used in research on neurodegenerative diseases .
    ATF4-IN-1
  • HY-158196
    PERK/eIF2α activator 1

    		PERK Apoptosis Cancer
    PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM .
    PERK/eIF2α activator 1
  • HY-100355
    C18-Ceramide

    		Endogenous Metabolite Neurological Disease Cancer
    C18-Ceramide is a bioactive molecule with multiple functions in cells, can cross the blood-brain barrier, not a traditional agonist or inhibitor targeting a single site. It can act on multiple cellular targets, such as proteins related to endoplasmic reticulum stress (e.g., ATF-4, XBP-1, CHOP), proteins in the PI3K/AKT signaling pathway, and SNARE complex proteins. It exerts activities like inducing cell death, promoting autophagy, and regulating exocytosis through mechanisms such as activating endoplasmic reticulum stress, inhibiting the PI3K/AKT signaling pathway, and affecting lipid raft - related functions. It can be used in research on the mechanism of neuronal injury in the field of neuroscience and in the treatment research of cancers such as glioma in the field of oncology .
    C18-Ceramide
  • HY-117938
    T-3861174

    		Aminoacyl-tRNA Synthetase Cancer
    T-3861174 is an inhibitor of prolyl-tRNA synthetase (PRS, Aminoacyl-tRNA Synthetase) without completely inhibiting its translation process. T-3861174 activates the GCN2-ATF4 pathway and induces death in multiple tumor cell lines, including SK-MEL-2. T-3861174 demonstrated significant antitumor activity in multiple xenograft models without significantly affecting body weight .
    T-3861174
  • HY-112903A
    YW3-56 hydrochloride

    		Protein Arginine Deiminase MDM-2/p53 PERK mTOR Autophagy Cancer
    YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer .
    YW3-56 hydrochloride
  • HY-158204
    CNB-001

    		Lipoxygenase Neurological Disease
    CNB-001 is a potent 5-lipoxygenase (5-LOX) inhibitor, decreases 5-LOX expression, and increases proteasome activity. CNB-001 also increases eIF2α phosphorylation and HSP90 and ATF4 levels in Alzheimer's disease transgenic mice, and limits the accumulation of soluble Aβ and ubiquitinated aggregated proteins. CNB-001 maintains the expression of synapse-associated proteins and improves memory. CNB-001 can be used for the research of Alzheimer's disease .
    CNB-001
  • HY-172784
    Anticancer agent 273

    		PI3K Akt Apoptosis Cancer
    Anticancer agent 273 (Compound 9q) is a potent anticancer agent found in matrine. Anticancer agent 273 inhibits the proliferation of cancer cells (e.g., HeLa cells with an IC50 value of 4.48 μM). Anticancer agent 273 exerts anticancer effects by modulating the expression of PI3K/AKT and activating transcription factor 4 (ATF4), which promotes endoplasmic reticulum stress and induces apoptosis. Anticancer agent 273 is promising for research of cancers, such as cervical cancer .
    Anticancer agent 273
  • HY-112654A
    GCN2iB acetate

    		Endogenous Metabolite Cancer
    GCN2iB acetate is a GCN2 inhibitor that enhances Gcn2 activity and Atf4 expression. GCN2iB can activate Gcn2 mutants lacking functional regulatory regions or certain kinase domain substitution mutants. GCN2iB increases eIF2 phosphorylation by Gcn2 at low concentrations, thereby enhancing the cellular response to nutritional stress. GCN2iB may have potential benefits for the inhibition of cancer cells expressing low basal levels of aspartate synthetase, enhancing their sensitivity to the anti-leukemic compound L-aspartase .
    GCN2iB acetate
  • HY-138844
    3-AP-Me

    		Eukaryotic Initiation Factor (eIF) p38 MAPK JNK Apoptosis Cancer
    3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research .
    3-AP-Me
  • HY-170872
    PT-129

    		PROTACs DNA/RNA Synthesis Cancer
    PT-129 is an RPOTAC degrader targeting the NTF2 domain (protein-RNA interaction site) of G3BP1/2, which mediates the disassembly of intracellular stress granules. PT-129 can inhibit the formation of stress granules in stressed cells and disassemble existing stress granules, and can disrupt the transmission of ATF4, thereby inhibiting the proliferation of cancer cells. Stress granules (SGs) are membrane-less cytoplasmic compartments formed under stress stimuli. SGs promote the transmission of ATF4 from fibroblasts to tumor cells through a migratory effect, mediating fibroblast-related tumor growth. And G3BP1/2 is a central protein of the SGs network, and the inhibition of G3BP1/2 may reduce the stress resistance of cancer cells in the tumor microenvironment. PT-129 is composed of a target protein ligand (red part) G3BP1/2-Targeting ligand-1 (HY-170873), an E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a PROTAC linker (black part) Amino-PEG3-C2-acid (HY-W040165); among them, the E3 ligase ligand + linker form a complex Thalidomide-NH-PEG3-propionic acid (HY-136166) .
    PT-129
  • HY-158205
    HPO-DAEE

    4-Hydroperoxy-2-decenoic acid ethyl ester

    		 Reactive Oxygen Species HDAC SOD Inflammation/Immunology Cancer
    HPO-DAEE (4-Hydroperoxy-2-decenoic acid ethyl ester) elicits nuclear accumulation of Nrf2 and activated antioxidant response element (ARE). HPO-DAEE induces antioxidant genes upregulation (eg: HO-1) through Nrf2-ARE signaling. HPO-DAEE induces reactive oxygen species generation. HPO-DAEE also inhibits histone deacetylase and upregulate expression of extracellular superoxide dismutase via histone acetylation. HPO-DAEE protects against 6-hydroxydopamine-induced cell death via activation of Nrf2-ARE and eIF2α-ATF4 pathways .
    HPO-DAEE
  • HY-13559
    Atiprimod

    Azaspirane

    		 Apoptosis Cancer
    Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
    Atiprimod
  • HY-112056
    DIM-C-pPhCO2Me
    1 Publications Verification

    		 Nuclear Hormone Receptor 4A/NR4A Apoptosis DAPK Isocitrate Dehydrogenase (IDH) PERK Cancer
    DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research .
    DIM-C-pPhCO2Me

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