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conformational change

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31

Inhibitors & Agonists

1

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2

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2

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1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109176
    Giredestrant
    5 Publications Verification

    GDC-9545; RG6171

    		 Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .
    Giredestrant
  • HY-145391
    Triperiden

    		Influenza Virus Infection
    Triperiden is an inhibitor of influenza virus multiplication. Triperiden targets the haemagglutinin of fowl plague virus (FPV) for antiviral activity and acts by inhibiting the conformational change in the haemagglutinin at acid pH. Triperiden is also anticholinergic anti-parkinsonism agent .
    Triperiden
  • HY-123054
    BTSA1
    1 Publications Verification

    		 Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis .
    BTSA1
  • HY-Y0788
    Indoline

    		HIV Infection
    Indoline is a derivative of Indole (HY-W001132). Indoline can used as the basic structure for CD4 mimetic compounds (CD4mcs), which triggers conformational changes of the HIV-1 envelope glycoprotein (Env) in advance, and causes viral inactivation
    Indoline
  • HY-162865
    FGFR2-IN-3

    		FGFR Cancer
    FGFR2-IN-3 is an inhibitor of fibroblast growth factor receptor 2 (FGFR2). FGFR2-IN-3 has good binding properties, forming key interactions and inducing conformational changes in FGFR2. FGFR2-IN-3 can be used for research on tumors .
    FGFR2-IN-3
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate; RG6171 tartrate

    		 Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
    Giredestrant tartrate
  • HY-P9962
    Efungumab

    		Fungal Infection
    Efungumab is a monoclonal antibody with antifungal activity. Efungumab binds to HSP 90, preventing a conformational change needed for fungal viability. Efungumab can be used for research on invasive candidiasis (IC) .
    Efungumab
  • HY-122106
    RS-104966

    		MMP Others
    RS-104966 is a potent collagenase-1 (MMP-1) inhibitor. RS-104966 induces a conformational change in the side chains of the S10 pocket of MMP-1 .
    RS-104966
  • HY-121461
    A25822B

    15-Azasterol

    		 Fungal Infection
    A25822B is an antifungal agent, with a MIC of 1 μM for Ascosphaera apis. A25822B causes conformational changes in mitochondria and disruption of spore membrane structure. A25822B can be used for the research of bee chalk disease .
    A25822B
  • HY-169234
    BChE-IN-35

    		Cholinesterase (ChE) Neurological Disease
    BChE-IN-35 (Azo-9) is a BChE inhibitor. BChE-IN-35 has a dynamic cis/trans conformational change, where the cis isomer preferentially binds to BChE. BChE-IN-35 can be used in Alzheimer's disease (AD) research .
    BChE-IN-35
  • HY-161276
    BFC1108

    		Apoptosis Bcl-2 Family Cancer
    BFC1108 is a small molecule Bcl-2 functional converter. BFC1108 induces a conformational change in Bcl-2, resulting in the exposure of its BH3 domain both in vitro and in vivo. BFC1108 effectively induces apoptosis in Bcl-2 expressing cancers. .
    BFC1108
  • HY-170429
    BJP-07-017-3

    		PIN1 Cancer
    BJP-07-017-3 is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 9 nM. BJP-07-017-3 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation .
    BJP-07-017-3
  • HY-127111
    NDI-091143
    2 Publications Verification

    		 ATP Citrate Lyase Cancer
    NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate .
    NDI-091143
  • HY-116182
    RO5487624

    		Influenza Virus Infection
    RO5487624, an analogue of RO5464466 (HY-120690), is an orally active hemagglutinin (HA) inhibitor of influenza H1N1 viruses that abolishes influenza virus fusion by blocking HA conformational changes in low pH environments. RO5487624 displays a protective effect on mice that are lethally challenged with influenza H1N1 virus .
    RO5487624
  • HY-101083
    BDA-366

    		Bcl-2 Family Cancer
    BDA-366 is a potent Bcl2 antagonist (Ki = 3.3 nM), binding Bcl2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
    BDA-366
  • HY-150784
    XR8-89

    		SARS-CoV Infection
    XR8-89 is a potent papain-like protease (PL pro) inhibitor with an IC50 value of 0.1 μM. XR8-89 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. XR8-89 can be used for SARS-CoV-2 research .
    XR8-89
  • HY-150786
    PLP_Snyder530

    		SARS-CoV Infection
    PLP_Snyder530 is a potent papain-like protease (PL pro) inhibitor with an IC50 value of 6.4 μM. PLP_Snyder530 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. PLP_Snyder530 can be used for SARS-CoV-2 research .
    PLP_Snyder530
  • HY-P1740
    RGD peptide (GRGDNP)
    5 Publications Verification

    		 Integrin Apoptosis Caspase Inflammation/Immunology
    RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
    RGD peptide (GRGDNP)
  • HY-150783
    SARS-CoV-2-IN-24

    		SARS-CoV Infection
    SARS-CoV-2-IN-24 (compound 7) is a potent papain-like protease (PL pro) inhibitor. SARS-CoV-2-IN-24 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. SARS-CoV-2-IN-24 can be used for SARS-CoV-2 research .
    SARS-CoV-2-IN-24
  • HY-119682
    Bax agonist 1

    		Bcl-2 Family Apoptosis Cancer
    Bax agonist 1 (compound SMBA2) is a Bax agonist (Ki=57.2 nM). Bax agonist 1 induces Bax conformational changes by blocking S184 phosphorylation, promoting Bax insertion into the mitochondrial membrane and forming Bax oligomers, which induce cytochrome c release and apoptosis in malignant cancer cells expressing Bax. Bax agonist 1 can be used in lung cancer research .
    Bax agonist 1
  • HY-134539
    IMT1
    3 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-144998
    NVP-DKY709

    		Molecular Glues IKZF Family Inflammation/Immunology Cancer
    NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
    NVP-DKY709
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA)
    5 Publications Verification

    		 Integrin Apoptosis Inflammation/Immunology Cancer
    RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
    RGD peptide (GRGDNP) (TFA)
  • HY-144382
    Glutamate-5-kinase-IN-2

    		Bacterial Infection
    Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.2 µM. Glutamate-5-kinase-IN-2 shows G5K inhibition by promotes conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-2
  • HY-156078
    α-Glucosidase-IN-32

    		Glycosidase Metabolic Disease
    α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
    α-Glucosidase-IN-32
  • HY-164895
    PIN1 degrader-1

    		PIN1 Cancer
    PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research .
    PIN1 degrader-1
  • HY-101083A
    (Rac)-BDA-366

    		Bcl-2 Family Cancer
    (Rac)-BDA-366 (example 2) is the despinner of BDA-366 (HY-101083). BDA-366 is a potent Bcl-2 antagonist (Ki=3.3 nM), binding Bcl-2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl-2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
    (Rac)-BDA-366
  • HY-162809
    XMU-MP-9

    		Ras Cancer
    XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used in cancer research .
    XMU-MP-9
  • HY-Y1754
    2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid

    TOAC

    		 Biochemical Assay Reagents
    2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid (TOAC) is a compound with the ability to probe conformational changes, folding processes and interactions of peptides and proteins. 2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid is often used in relevant biological research to gain a deeper understanding of the behavior and function of biomacromolecules. 2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid plays an important role in analyzing the interactions and dynamic responses of biological systems.
    2,2,6,6-Tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid
  • HY-161577
    BFC1103

    		Bcl-2 Family Cancer
    BFC1103 is a small-molecule compound whose primary mechanism of action involves interaction with a specific domain of Bcl-2, particularly its loop domain. This interaction induces a conformational change in Bcl-2, exposing its BH3 (Bcl-2 homology 3) domain, thereby switching Bcl-2's function from anti-apoptotic to pro-apoptotic. The cell death induced by BFC1103 is dependent on the presence of Bax or Bak, both of which are key proteins involved in the intrinsic apoptotic pathway mediated by mitochondria. BFC1103 has successfully inhibited lung metastasis of triple-negative breast cancer in mouse models. It can be utilized in studying the roles of Bcl-2 family proteins in cancer development and how they impact the survival and proliferation of cancer cells .
    BFC1103
  • HY-W017113
    2-Mercaptobenzothiazole

    		Endogenous Metabolite Aryl Hydrocarbon Receptor Metabolic Disease
    2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
    2-Mercaptobenzothiazole

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