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Results for "

PERK-IN-2

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

1

Peptides

4

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0168A
    Milnacipran hydrochloride
    2 Publications Verification

    		 Serotonin Transporter PERK Neurological Disease
    Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) [2] .
    Milnacipran hydrochloride
  • HY-135220
    PERK-IN-2
    1 Publications Verification

    		 PERK Cancer
    PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM .
    PERK-IN-2
  • HY-153740
    PF-07284892

    ARRY-558

    		 SHP2 Cancer
    PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC50 value of 21 nM. PF-07284892 decreases the expression of pERK .
    PF-07284892
  • HY-W010451
    1,2,4-Trihydroxybenzene

    HydroxyhydroquINone

    		 PERK Eukaryotic Initiation Factor (eIF) Potassium Channel Apoptosis Cardiovascular Disease Cancer
    1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm [2] .
    1,2,4-Trihydroxybenzene
  • 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 [2] .
    DIM-C-pPhCO2Me
  • HY-101991
    ML291

    		PERK Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden .
    ML291
  • 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-B0168
    Milnacipran
    2 Publications Verification

    		 Serotonin Transporter PERK Neurological Disease
    Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) [2] .
    Milnacipran
  • 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-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) [2] .
    Atiprimod
  • HY-N3480
    Isogosferol

    (+)-Isogospherol; Isogospherol

    		 Others Inflammation/Immunology
    Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2 .
    Isogosferol
  • HY-114978
    VU0424465

    		mGluR PERK Neurological Disease
    VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons [2].
    VU0424465
  • HY-B0168S
    Milnacipran-d10 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter PERK Neurological Disease
    Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) [2] .
    Milnacipran-d10 hydrochloride
  • HY-13559A
    Atiprimod dimaleate

    Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate

    		 STAT Apoptosis Caspase Interleukin Related Autophagy Reactive Oxygen Species (ROS) Atg8/LC3 p62 JAK Cardiovascular Disease Inflammation/Immunology Cancer
    Atiprimod (Azaspirane) (dimaleate) 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) [2] .
    Atiprimod dimaleate
  • HY-110102
    Atiprimod hydrochloride

    Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615

    		 JAK STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Atg8/LC3 p62 Cardiovascular Disease Inflammation/Immunology Cancer
    Atiprimod (Azaspirane) hydrochloride 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) [2] .
    Atiprimod hydrochloride
  • HY-155098
    CNBCA

    		SHP2 Cancer
    CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .
    CNBCA
  • HY-173188
    EGFR-IN-154

    		EGFR Akt PERK JNK p38 MAPK Cancer
    EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC50 values of 0.16 μM, 21.73 μM and 41.56 μM against EGFR Del19, EGFR WT and EGFR L858R, respectively. EGFR-IN-154 shows anticancer activity on various cance cell lines. EGFR-IN-154 induces mitochondrial apoptosis, and decreases pERK1/2 and pAkt levels, but increases pJNK and pp38 levels .
    EGFR-IN-154
  • HY-144693
    MEK/PI3K-IN-2

    		MEK PI3K PERK Cancer
    MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
    MEK/PI3K-IN-2
  • HY-144692
    MEK/PI3K-IN-1

    		MEK PI3K PERK Cancer
    MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
    MEK/PI3K-IN-1
  • HY-B0168AS
    Milnacipran-d5 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter PERK Neurological Disease
    Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) [2] .
    Milnacipran-d5 hydrochloride
  • HY-B0168AR
    Milnacipran hydrochloride (Standard)

    		Reference Standards Serotonin Transporter PERK Neurological Disease
    Milnacipran (hydrochloride) (Standard) is the analytical standard of Milnacipran hydrochloride (HY-B0168A). This product is intended for research and analytical applications. Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) [2] .
    Milnacipran hydrochloride (Standard)
  • HY-W010451R
    1,2,4-Trihydroxybenzene (Standard)

    HydroxyhydroquINone (Standard)

    		 Reference Standards PERK Potassium Channel Apoptosis Eukaryotic Initiation Factor (eIF) Cardiovascular Disease Cancer
    1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm [2] .
    1,2,4-Trihydroxybenzene (Standard)
  • HY-P11011A
    Peptide R54 acetate

    Pep R54 acetate; CXCR4 antagonist peptide 19 acetate

    		 CXCR ERK Akt Cancer
    Peptide R54 acetate (Pep R54 acetate) is a CXCR4 antagonist. Peptide R54 acetate inhibits CXCL12-dependent activation of pERK1/2 and pAKT. The combination of Peptide R54 acetate and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer [2].
    Peptide R54 acetate
  • HY-101991R
    ML291 (Standard)

    		Reference Standards PERK Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    ML291 (Standard) is the analytical standard of ML291 (HY-101991). This product is intended for research and analytical applications. ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden .
    ML291 (Standard)
  • HY-181087
    Anticancer agent 296

    		PERK Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Bcl-2 Family Cancer
    Anticancer agent 296 is a potent anticancer agent that activates the PERK-eIF2α-CHOP signaling pathway to induce endoplasmic reticulum stress, thereby regulating caspase and Bcl-2 family proteins, ultimately leading to apoptosis. Anticancer agent 296 increases intracellular levels of reactive oxygen species (ROS), reduces mitochondrial membrane potential, and promotes Ca 2+ release. Anticancer agent 296 suppresses cell colony formation and S-phase cell proliferation, and induces autophagy. Anticancer agent 296 is applicable for research on non-small cell lung cancer (NSCLC) .
    Anticancer agent 296
  • HY-182360
    Cytisine-platinum(IV) prodrug-1

    		PERK Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Reactive Oxygen Species (ROS) STING DNA/RNA Synthesis PD-1/PD-L1 Cancer
    Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer .
    Cytisine-platinum(IV) prodrug-1
  • HY-W097625R
    6-Methoxyflavone (Standard)

    		Toll-like Receptor (TLR) MyD88 p38 MAPK NF-κB Heme Oxygenase (HO) Reference Standards PERK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    6-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases [2] .
    6-Methoxyflavone (Standard)

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