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Eif Inhibitors

" in MedChemExpress (MCE) Product Catalog:

100

阻害剤およびアゴニスト

3

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6

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1

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Targets Recommended:
製品番号 製品名 Target 研究分野 構造式
  • HY-12495A
    ISRIB
    25+ Cited Publications

    		 Biochemical Assay Reagents Eukaryotic Initiation Factor (eIF) Neurological Disease
    ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .
    ISRIB
  • HY-12495
    ISRIB (trans-isomer)
    45+ Cited Publications

    		 PERK Autophagy Apoptosis Neurological Disease
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
    ISRIB (trans-isomer)
  • HY-19356
    Rocaglamide
    25+ Cited Publications

    Roc-A

    		 NF-κB HSP Eukaryotic Initiation Factor (eIF) Inflammation/Immunology Cancer
    Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia .
    Rocaglamide
  • HY-112163
    Zotatifin
    5+ Cited Publications

    eFT226

    		 Eukaryotic Initiation Factor (eIF) SARS-CoV Apoptosis Infection Cancer
    Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex . Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM) . Zotatifin induces cell apoptosis .
    Zotatifin
  • HY-15486
    Salubrinal
    35+ Cited Publications

    		 Phosphatase HSV Autophagy Apoptosis Infection Inflammation/Immunology Cancer
    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation . Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis . Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5 .
    Salubrinal
  • HY-19831
    4EGI-1
    15+ Cited Publications

    		 Eukaryotic Initiation Factor (eIF) Autophagy Apoptosis Cancer
    4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
    4EGI-1
  • HY-13251
    Silvestrol
    Maximum Cited Publications
    52 Publications Verification

    (-)-Silvestrol

    		 Eukaryotic Initiation Factor (eIF) Apoptosis Autophagy Cancer
    Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from Agave americana Linn.. Silvestrol induces autophagy and caspase-mediated apoptosis .
    Silvestrol
  • HY-101513
    eIF4A3-IN-1
    4 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Neurological Disease Cancer
    eIF4A3-IN-1 is a selective eIF4A3 inhibitor (IC50: 0.26 μM; Kd: 0.043 μM) with cellular nonsense-mediated RNA decay (NMD) inhibitory activity. eIF4A3-IN-1 can specifically bind to the non-ATP binding site of eIF4A3. eIF4A3-IN-1 has anti-tumor and analgesic activities .
    eIF4A3-IN-1
  • HY-N2397
    9''-Methyl salvianolate B

    MSB

    		 DNA/RNA Synthesis PPAR NF-κB Autophagy Cardiovascular Disease Infection Inflammation/Immunology
    9''-Methyl salvianolate B (MSB) is a blood-brain barrier-permeable inhibitor with high affinity for g5Rp, with a Kd value of 117 nM against African swine fever virus (ASFV) g5Rp. 9''-Methyl salvianolate B also acts as a ZBP1 inhibitor. It exhibits strong binding affinity to key proteins in the PPARγ/NF-κB pathway. 9''-Methyl salvianolate B blocks the interaction between ASFV g5Rp and host proteins eIF5A or RPS15. It restores hypusination modification of eIF5A, promotes autophagy (Autophagy), and inhibits ASFV replication. 9''-Methyl salvianolate B effectively disrupts ZBP1-mediated PANoptosome assembly. It effectively alleviates myocardial ischemia/reperfusion injury. 9''-Methyl salvianolate B can be used in studies related to African swine fever .
    9''-Methyl salvianolate B
  • HY-100022
    Tomivosertib
    10+ Cited Publications

    eFT508

    		 MNK PD-1/PD-L1 Cancer
    Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
    Tomivosertib
  • HY-14427
    4E1RCat
    3 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ～4 μM.
    4E1RCat
  • HY-15969
    Sal003
    4 Publications Verification

    		 Phosphatase Apoptosis Cancer
    Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal .
    Sal003
  • HY-111022
    Icerguastat
    3 Publications Verification

    Sephin1; IFB-088

    		 Phosphatase Infection Inflammation/Immunology
    Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .
    Icerguastat
  • HY-118266
    BTdCPU
    3 Publications Verification

    		 Phosphatase Apoptosis Cancer
    BTdCPU is a potent heme regulated inhibitor kinase (HRI) activator that promotes eIF2α phosphorylation and induces apoptosis in Dexamethasone (HY-14648) (Dex)-resistant cancer cells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma .
    BTdCPU
  • HY-19560
    SBI-0640756
    3 Publications Verification

    SBI-756

    		 Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    SBI-0640756 (SBI-756) is an inhibitor of eIF4G1 and disrupts the eIF4F complex.
    SBI-0640756
  • HY-136453
    CR-1-31-B
    10+ Cited Publications

    		 Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    CR-1-31-B is a synthetic rocaglate and a potent eIF4A inhibitor. CR-1-31-B exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis. CR-1-31-B perturbs association of Plasmodium falciparum eIF4A (PfeIF4A) with RNA. CR-1-31-B induces apoptosis of neuroblastoma and gallbladder cancer cells .
    CR-1-31-B
  • HY-149555
    DNL343

    		Eukaryotic Initiation Factor (eIF) Neurological Disease
    DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
    DNL343
  • HY-19356A
    Didesmethylrocaglamide

    		Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity .
    Didesmethylrocaglamide
  • HY-147831
    HR-19011

    		Eukaryotic Initiation Factor (eIF) Epigenetic Reader Domain Cancer
    HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia) .
    HR-19011
  • 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-148105
    DS12881479
    1 Publications Verification

    		 MNK Eukaryotic Initiation Factor (eIF) Apoptosis FLT3 DYRK Cancer
    DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia .
    DS12881479
  • HY-101997
    BEPP hydrochloride

    		Orthopoxvirus Apoptosis Caspase Bcl-2 Family Akt Infection Cancer
    BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) modulator. BEPP hydrochloride enhances the phosphorylation levels of PKR and eIF2α, activates caspase-3, upregulates the pro-apoptotic protein BAX, and downregulates the anti-apoptotic protein Bcl-2. BEPP hydrochloride inhibits vaccinia virus replication and exhibits selective cytotoxicity in cells expressing PKR. BEPP hydrochloride can be used in research related to cancer and viral infections .
    BEPP hydrochloride
  • HY-153399A
    Fosigotifator THAM sodium

    ABBV-CLS-7262 THAM sodium

    		 Eukaryotic Initiation Factor (eIF) Neurological Disease Cancer
    Fosigotifator (ABBV-CLS-7262) THAM sodium is a brain penetrant, orally active EIF2b (eukaryotic initiation factor) activator. Fosigotifator THAM sodium stabilizes the elF2B complex and boosts the activity, including that of complexes carrying pathogenic vanishing white matter (VWM) mutations. Fosigotifator THAM sodium is an integrated stress response inhibitor (ISRI). Fosigotifator THAM sodium can be used for amyotrophic lateral sclerosis research .
    Fosigotifator THAM sodium
  • HY-16366
    Briciclib

    ON 014185

    		 Eukaryotic Initiation Factor (eIF) CDK c-Myc MDM-2/p53 Caspase Apoptosis Cancer
    Briciclib (ON 014185) is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib can be used for the study of hematological system tumors and solid tumors .
    Briciclib
  • HY-130240
    GCN2-IN-6
    3 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells) . GCN2-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GCN2-IN-6
  • HY-172815
    IDB-001

    		JNK Eukaryotic Initiation Factor (eIF) p38 MAPK Cancer
    IDB-001 is a human ribosomal peptidyl transferase center (PTC) inhibitor that induces conformational changes and blocks translational elongation in specific sequence contexts through complementary interactions with Asp/Glu residues in nascent polypeptides. IDB-001 preferentially stalls ribosomes at positions containing acidic peptide motifs, thereby inhibiting cancer cell proliferation, and activates the integrated stress response via eIF2α phosphorylation at high concentrations. In addition, IDB-001 mildly triggers ribotoxic stress responses through phosphorylation of JNK and p38. IDB-001 has been applied to mechanistic studies of triple-negative breast cancer .
    IDB-001
  • HY-176842
    eIF4A-IN-1

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A-IN-1 (Compound 79) is an eIF4A inhibitor that inhibits protein translation. eIF4A-IN-1 canb be used in gastric cancer research .
    eIF4A-IN-1
  • HY-148447
    eIF4A-IN-3

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A-IN-3, Silvestrol (HY-13251) analogue, is an eIF4A inhibitor. eIF4A-IN-3 blocks protein translation initiation by interfering with eIF4F complex assembly, preferentially inhibiting translation of mRNAs with long, highly structured 5'-untranslated regions. eIF4A-IN-3 inhibits proliferation of human breast cancer cells. eIF4A-IN-3 has moderate apical to basolateral permeability in intestinal cell monolayers and a low efflux ratio .
    eIF4A-IN-3
  • HY-145262
    eIF4E-IN-2

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e) with an IC50 of 13 nM. eIF4E-IN-2 inhibits MDA-MB-361 cells proliferation. eIF4E-IN-2 can be used for the study of breast cancer .
    eIF4E-IN-2
  • HY-100733
    4E2RCat
    5 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Autophagy Virus Protease Neurological Disease
    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
    4E2RCat
  • HY-148450
    eIF4A3-IN-16

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4A3-IN-16 (compound 60) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-16 inhibits MBA-MB-231cell growth with an EC50 value of 1 nM. eIF4A3-IN-16 interferes the assembling of eIF4F translation complex with a myc-LUC EC50 value of 1 nM and a tub-LUC EC50 value of 30 nM. eIF4A3-IN-16 can be used for triple negative breast cancer (TNBC) research .
    eIF4A3-IN-16
  • HY-112163A
    rel-Zotatifin

    rel-eFT226

    		 Eukaryotic Initiation Factor (eIF) SARS-CoV Apoptosis Infection Cancer
    rel-Zotatifin is the racemic isomer of Zotatifin, acts as an eIF4A inhibitor with activity less than Zotatifin. Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex .
    rel-Zotatifin
  • HY-101785
    eIF4A3-IN-2
    1 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM .
    eIF4A3-IN-2
  • HY-153074
    ISR-IN-1

    		Eukaryotic Initiation Factor (eIF) Infection
    ISR-IN-1 is an integrated stress response inhibitor targeting eIF2B. ISR-IN-1 enhances eIF2B guanine nucleotide exchange factor activity, stabilizes eIF2B heteropentamer dimers via symmetrical protein-protein interface binding, and releases global protein synthesis inhibition from phosphorylated eIF2α α. ISR-IN-1 can be used for the research of prion disease .
    ISR-IN-1
  • HY-19831A
    (Z)-4EGI-1

    		Eukaryotic Initiation Factor (eIF) Cancer
    (Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity .
    (Z)-4EGI-1
  • HY-148422
    Rohinitib
    1 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .
    Rohinitib
  • HY-119271
    CMLD010509

    SDS-1-021

    		 c-Myc Apoptosis Cancer
    CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism .
    CMLD010509
  • HY-176844
    eIF4A-IN-1 intermediate

    		ADC Payload Drug Intermediate Cancer
    eIF4A-IN-1 intermediate (Compound 71E) is an intermediate of Eukaryotic translation initiation factor 4A (eIF4A) inhibitor. eIF4A-IN-1 intermediate can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs) .
    eIF4A-IN-1 intermediate
  • HY-146805
    EB1

    		MNK Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation .
    EB1
  • HY-148062
    RSS0680

    		PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK Others
    RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC with protein kinase degradation activity (Pink: FLT3-IN-17 (HY-148070); Black: Linker (HY-W041970); Blue: E3 ligase Ligand (HY-112078)). RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
    RSS0680
  • HY-145309
    eIF4E-IN-3

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4E-IN-3 (Example 485) is a eIF4E inhibitor with an IC50 of 0.00859 μM. eIF4E-IN-3 inhibits the activity of eIF4E. eIF4E-IN-3 is used in cancer research .
    eIF4E-IN-3
  • HY-15359
    Episilvestrol
    1 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    Episilvestrol is a derivative of silvestrol, isolated from the fruits and twigs of Aglaia perviridis, and is a specific eIF4A-targeting translation inhibitor, with antitumor activity.
    Episilvestrol
  • 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-114267
    Cbz-B3A

    		mTOR Others
    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
    Cbz-B3A
  • HY-139098
    7-Methyl-diguanosine triphosphate

    m7Gp3G

    		 DNA/RNA Synthesis Others
    7-Methyl-diguanosine triphosphate (m7Gp3G) is an mRNA cap structure analog that inhibits in vitro protein synthesis by binding to the translation initiation complex. 7-Methyl-diguanosine triphosphate binds to eIF4E, promotes cap-dependent translation initiation, stabilizes mRNA, and acts as a translation enhancer. 7-Methyl-diguanosine triphosphate can be used to prepare synthetic capped RNA transcripts for studies related to mRNA translation, splicing, turnover, and intracellular transport .
    7-Methyl-diguanosine triphosphate
  • HY-145835
    PERK-IN-5

    		PERK Cancer
    PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
    PERK-IN-5
  • 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-111522
    RK-9123016

    		Sirtuin c-Myc Cancer
    RK-9123016 is a potent inhibitor of SIRT2. RK-9123016 inhibits the enzymatic activity of SIRT2 with an IC50 value of 0.18 µM but not other human sirtuin members including SIRT1 and SIRT3 at 100 µM. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression .
    RK-9123016
  • HY-13559
    Atiprimod

    Azaspirane ; SKF 106615-12; SKF 106615A12

    		 STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Bcl-2 Family p62 Atg8/LC3 PARP NF-κB PERK JAK Cardiovascular Disease Inflammation/Immunology Cancer
    Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and 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. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
    Atiprimod
  • HY-179109
    EIF2B-IN-1

    		Eukaryotic Initiation Factor (eIF) Others
    EIF2B-IN-1 (Compound A) is an eIF2B inhibitor. EIF2B-IN-1 binds eIF2B. EIF2B-IN-1 stabilises the eIF2B decamer and favours inhibitory eIF2B:eIF2(αP) complex formation. EIF2B-IN-1 exhibits weak displacement of ISRIB. EIF2B-IN-1 can be used in the research of integrated stress responses .
    EIF2B-IN-1

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