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conformational disorder

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14

Inhibitors & Agonists

3

Natural
Products

Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-134539
    IMT1
    Maximum Cited Publications
    10 Publications Verification

    		 Oxidative Phosphorylation Mitochondrial Metabolism DNA/RNA Synthesis Metabolic Disease Cancer
    IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
    IMT1
  • HY-N0735
    Phellodendrine chloride
    2 Publications Verification

    		 Autophagy Apoptosis AMPK mTOR STAT Interleukin Related PKC p38 MAPK NF-κB COX Reactive Oxygen Species (ROS) PI3K Akt MMP Neurological Disease Inflammation/Immunology Cancer
    Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway .
    Phellodendrine chloride
  • HY-157802
    LTGO-33

    		Sodium Channel Neurological Disease
    LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
    LTGO-33
  • HY-N0427
    Phellodendrine

    		Akt NF-κB AMPK mTOR PKC STAT Interleukin Related p38 MAPK COX Reactive Oxygen Species (ROS) Apoptosis Autophagy PI3K MMP Neurological Disease Inflammation/Immunology Cancer
    Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway .
    Phellodendrine
  • HY-160550
    DPM-1003

    		Phosphatase Inflammation/Immunology
    DPM-1003 is a PTP1B conformational inhibitor that targets the non-catalytic, disordered segment at the C-terminus of the PTP1B protein, showing improvement in lung inflammation in mice .
    DPM-1003
  • HY-N0735R
    Phellodendrine chloride (Standard)

    		Reference Standards Autophagy mTOR AMPK Apoptosis STAT Interleukin Related PKC p38 MAPK NF-κB COX Reactive Oxygen Species (ROS) PI3K Akt MMP Neurological Disease Inflammation/Immunology Cancer
    Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
    Phellodendrine chloride (Standard)
  • HY-144327
    Aβ-IN-2

    		Amyloid-β Neurological Disease
    Aβ-IN-2 is a Aβ1-42 aggregation inhibitor. Aβ-IN-2 inhibits Aβ1-42 self-aggregation in vitro by delaying the exponential growth phase or reduces the quantity of fibrils in the steady state. Aβ-IN-2 can be used for the research of conformational disorders .
    Aβ-IN-2
  • HY-144326
    Aβ-IN-1

    		Amyloid-β Neurological Disease
    Aβ-IN-1 is a Aβ1-42 aggregation inhibitor. Aβ-IN-1 inhibits Aβ1-42 self-aggregation in vitro by delaying the exponential growth phase or reduces the quantity of fibrils in the steady state. Aβ-IN-1 can be used for the research of conformational disorders .
    Aβ-IN-1
  • HY-174282
    RDS-04-010

    		Dopamine Transporter Neurological Disease
    RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD) .
    RDS-04-010
  • HY-106964A
    (Rac)-S 16924

    		5-HT Receptor Neurological Disease
    (Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. (Rac)-S 16924 regulates signaling through its interaction with the 5-HT1A receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the 5-HT1A receptor in mental disorders, especially schizophrenia .
    (Rac)-S 16924
  • HY-131642
    L-γ-Carboxyglutamic acid

    H-Gla-OH

    		 mGluR Neurological Disease
    L-γ-Carboxyglutamic acid (H-Gla-OH) is a mGluR2 antagonist with an IC50 of 102 μM. L-γ-Carboxyglutamic acid binds to the mGluR2 receptor site via the overlapping extended amino acid conformation of its amino and carboxyl groups with glutamic acid, and its additional acidic group locates in a restricted region, thereby blocking the full activation of the receptor. L-γ-Carboxyglutamic acid can be used for the research of neurological disorders .
    L-γ-Carboxyglutamic acid
  • HY-180880
    TFAP2β modulator-1

    		Apoptosis Cancer
    TFAP2β modulator-1 (compound A6) is a potent TFAP2β modulator that promotes TFAP2β condensation by inducing conformational changes in the intrinsically disordered region. TFAP2β modulator-1 promotes TFAP2β condensation, induces apoptosis, and exhibits anti-tumor functions in esophageal squamous cell carcinoma (ESCC) cells, mouse models, and organoids. TFAP2β modulator-1 can be used for ESCC research .
    TFAP2β modulator-1
  • HY-181605
    MOR antagonist 2 hydrochloride

    		Opioid Receptor Neurological Disease
    MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder .
    MOR antagonist 2 hydrochloride
  • HY-181888
    GRL-142

    		HIV HIV Protease Infection
    GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC50=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND) .
    GRL-142

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