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permeability response

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18

Inhibitors & Agonists

1

Screening Libraries

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-131370B
    Intralipid 20%

    		Others Cancer
    Intralipid 20% is a safe fat emulsion that can be used as a nutritional supplement. Intralipid 20% effectively inhibits the opening of the mitochondrial permeability transition pore, effectively protecting the heart from ischaemia-reperfusion injury and has some potential to modulate the innate immune response .
    Intralipid 20%
  • HY-121134
    Decylubiquinone

    		Reactive Oxygen Species Neurological Disease Cancer
    Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition .
    Decylubiquinone
  • HY-125021
    2BAct
    1 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Neurological Disease
    2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .
    2BAct
  • HY-129079
    TFMB-(R)-2-HG
    1 Publications Verification

    		 Others Cancer
    TFMB-(R)-2-HG, a cell membrane-permeable version of (R)-2-HG, is a carcinogenic factor in Acute myeloid leukemia (AML). TFMB-(R)-2-HG impairs SCF ER-Hoxb8 cells differentiation in response to estrogen withdrawal .
    TFMB-(R)-2-HG
  • HY-149823
    TRPV4 antagonist 4

    		TRP Channel Neurological Disease
    TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury .
    TRPV4 antagonist 4
  • HY-101379A
    8-Bromo-cGMP sodium
    1 Publications Verification

    		 Calcium Channel Cardiovascular Disease Neurological Disease
    8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K + . 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses .
    8-Bromo-cGMP sodium
  • HY-110258
    ML334
    5 Publications Verification

    LH601A

    		 Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    ML334
  • HY-149143
    JNJ-28583113

    		TRP Channel Inflammation/Immunology
    JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
    JNJ-28583113
  • HY-149555
    DNL343

    		Eukaryotic Initiation Factor (eIF) Neurological Disease
    DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity 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 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation .
    DNL343
  • HY-114454
    INH14
    1 Publications Verification

    		 IKK Inflammation/Immunology Cancer
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity .
    INH14
  • HY-131614
    TPC2-A1-N
    2 Publications Verification

    		 Calcium Channel Others
    TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells .
    TPC2-A1-N
  • HY-110258B
    (R,S,R)-ML334

    (R,S,R)-LH601A

    		 Others Cancer
    (R,S,R)-ML334 is the isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    (R,S,R)-ML334
  • HY-149431
    NDNA4

    		HSP Potassium Channel Cancer
    NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
    NDNA4
  • HY-108391
    C8-Ceramide

    N-Octanoyl-D-erythro-sphingosine

    		 Apoptosis PKC Autophagy Inflammation/Immunology Cancer
    C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
    C8-Ceramide
  • HY-149432
    NDNA3

    		HSP Potassium Channel Cancer
    NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC50: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC50: 12.66 μM) and MCF-10A (IC50: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
    NDNA3
  • HY-112291
    SB 220025

    		p38 MAPK Src PKC Inflammation/Immunology
    SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
    SB 220025
  • HY-119312
    C8 Dihydroceramide

    		PKC Cancer
    C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
    C8 Dihydroceramide
  • HY-12379
    NS-2028

    		Guanylate Cyclase Inflammation/Immunology
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity . NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM . NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM . NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM) . NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability .
    NS-2028

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