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conformational change

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43

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1

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1

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3

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8

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1

Inhibitory Antibodies

2

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Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-135024B
    Phenylacetyl CoA tetrasodium

    Phenylacetyl Coenzyme A tetrasodium

    		 Others Metabolic Disease
    Phenylacetyl Coenzyme A (Phenylacetyl Coenzyme A) tetrasodium is an effector molecule of the TetR family transcriptional repressor PaaR. Phenylacetyl Coenzyme A tetrasodium changes the conformation of PaaR, causing it to dissociate from DNA and initiate transcription. Phenylacetyl Coenzyme A tetrasodium is promising for research of microbial metabolism .
    Phenylacetyl CoA tetrasodium
  • 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-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-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-N3103
    p-Coumaric Acid Ethyl Ester

    Ethyl (E)-p-hydroxycinnamate; Ethyl trans-4-hydroxycinnamate

    		 Tyrosinase Inflammation/Immunology
    p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate; Ethyl trans-4-hydroxycinnamate) is a non-competitive, reversible inhibitor of tyrosinase (IC50=4.89 μg/mL, Ki=1.83 μg/mL), which can quench the intrinsic fluorescence of the enzyme. p-Coumaric Acid Ethyl Ester changes the binding affinity of L-tyrosine by inducing conformational changes in the catalytic domain of tyrosinase, and does not bind to the copper ion of the enzyme. p-Coumaric Acid Ethyl Ester is used in the development of medicines, cosmetics and fruit preservation products using pollen .
    p-Coumaric Acid Ethyl Ester
  • 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-P10948
    CS-VIP 8

    		WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .
    CS-VIP 8
  • 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-P10948A
    CS-VIP 8 TFA

    		WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 TFA is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 TFA induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 TFA is promising for research of hematological diseases such as leukemia .
    CS-VIP 8 TFA
  • 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-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-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-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-144998
    NVP-DKY709

    		IKZF Family Molecular Glues 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-134539
    IMT1
    4 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-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-173521
    JNJ-9676

    		SARS-CoV DNA/RNA Synthesis Infection
    JNJ-9676 is an orally active inhibitor of membrane (M) protein. JNJ-9676 has in vitro antiviral activity against SARS-CoV-2, SARS-CoV, and sarbecovirus from bats and pangolins. JNJ-9676 inhibits viral assembly by stabilizing the conformational changes of the M protein dimer, preventing the release of infectious viruses. JNJ-9676 has significant antiviral effects and can be used in research on the prevention and treatment of coronavirus infections .
    JNJ-9676
  • 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-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-144896
    FHT-1015
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    FHT-1015 is a selective SMARCA4 (IC50 = 4 nM) and SMARCA2 (IC50 = 5 nM) (also known as BRG1 and BRM) inhibitor. FH-1015 is an allosteric inhibitor that causes conformation change in the BRG1/BRM protein upon interaction with an allosteric site, inhibiting ATPase activity. FH-1015 interferes with tumor cell growth and migration. FH-1015 can be studied in research for uveal melanoma and hematologic cancer .
    FHT-1015
  • 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-P10941A
    VSLRGDTRG acetate

    		Integrin FAK ERK Inflammation/Immunology Cancer
    VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
    VSLRGDTRG acetate
  • HY-P10941
    VSLRGDTRG

    		Integrin FAK ERK Inflammation/Immunology Cancer
    VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
    VSLRGDTRG
  • HY-19487
    Ribocil

    		Bacterial Infection
    Ribocil is a selective inhibitor targeting the bacterial FMN riboswitch, regulating the bacterial riboflavin riboswitch. Ribocil competitively binds to the FMN binding site, mimicking the natural ligand FMN to induce conformational changes in the riboswitch, inhibiting ribB gene expression, reducing riboflavin synthesis, and thus inhibiting bacterial growth. Ribocil strongly inhibits GFP expression (EC50=0.3 μM). Ribocil exhibits in vivo antibacterial activity in a mouse model and can be used to study antibacterial drugs related to drug-resistant bacterial infections and bacterial riboflavin metabolic pathways[1][2].
    Ribocil
  • 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-D0896
    ANS

    ANSA; 8-Anilino-1-naphthalenesulfonic acid

    		 Bacterial Infection
    ANS (8-Anilino-1-naphthalenesulfonic acid) is a competitive inhibitor targeting thyroxine binding globulin (TBG) (Ki=2.09×10 6 M -1). ANS is used in radioimmunoassay by displacing bound triiodothyronine (T3) to improve detection sensitivity. ANS can block the protein binding site of T3 and release free T3 for antibody recognition. As a fluorescent probe, ANS can specifically bind to the hydrophobic region of proteins (such as membrane proteins) and monitor the dynamics of protein conformation through changes in fluorescent signals. It is widely used in biochemical research and antibacterial material development .
    ANS
  • 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-P1793A
    α-Casein (90-95) TFA

    		Opioid Receptor Biochemical Assay Reagents Neurological Disease Inflammation/Immunology Cancer
    α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) TFA inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) TFA activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer .
    α-Casein (90-95) TFA
  • HY-P1793
    α-Casein (90-95)

    		Opioid Receptor Biochemical Assay Reagents Neurological Disease Inflammation/Immunology Cancer
    α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer .
    α-Casein (90-95)
  • 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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