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conformational change

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82

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2

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4

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4

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13

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1

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3

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1

Oligonucleotides

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-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-P1740
    RGD peptide (GRGDNP)
    5+ Cited Publications

    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-D0896
    ANS
    1 Publications Verification

    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-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-144998
    NVP-DKY709
    1 Publications Verification

    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-156815

    Orphan GPCR Neurological Disease Inflammation/Immunology
    YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain .
    YL-365
  • HY-W017113
    2-Mercaptobenzothiazole
    1 Publications Verification

    Environmental Pollutants Endogenous Metabolite 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
  • 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-P10856

    P-glycoprotein Cancer
    CPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance .
    CPI1
  • HY-D0947

    DNA Stain Others
    Azure A chloride is a phenothiazine dye. Azure A chloride is an alternative DNA dye used for the separation of DNA and protein fragments in agarose gel electrophoresis and PAGE. Azure A chloride can be chemisorbed on the surface of mild steel according to the Langmuir adsorption isotherm to form a protective film. Azure A chloride binds to double-stranded DNA in a non-cooperative manner via weak intercalation, triggering molecular conformational disturbance, restricted rotational motion, and changes in optical activity .
    Azure A chloride
  • HY-144896
    FHT-1015
    2 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-19487

    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-176811

    Ras PI3K Akt Cancer
    VVD-442 is an inhibitor targeting PI3Kα. VVD-442 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, induces conformational changes, and disrupts the interaction between PI3K p110α and RAS proteins. VVD-442 also blocks RAS-mediated PI3K activation. VVD-442 can be used in research related to RAS-mutant cancers and HER2-overexpressing cancers .
    VVD-442
  • HY-162865

    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-138053

    Ristomycin III

    Antibiotic Cardiovascular Disease Infection
    Ristocetin A sulfate (Ristomycin III) is a glycopeptide antibiotic that binds to von Willebrand factor (VWF) and bacterial cell wall components. Ristocetin A sulfate interferes with the biosynthesis of bacterial peptidoglycan by inhibiting transpeptidation. As an inducer of platelet adhesion and aggregation, Ristocetin A sulfate drives conformational changes by binding to the A1 domain of VWF, thereby activating downstream signaling pathways and promoting cytoskeletal rearrangement. Ristocetin A sulfate not only enhances platelet adhesion and spreading on immobilized VWF, but also induces the formation of asymmetric dimers with anticooperativity between platelets and plasma VWF. Ristocetin A sulfate is widely used in studies related to thromboembolic diseases and bacterial infections .
    Ristocetin A sulfate
  • HY-172815

    JNK Eukaryotic Initiation Factor (eIF) p38 MAPK Cancer
    IDB-001 is a human ribosomal peptidyl transferase center (PTC) inhibitor that induces conformational changes and blocks translational elongation in specific sequence contexts through complementary interactions with Asp/Glu residues in nascent polypeptides. IDB-001 preferentially stalls ribosomes at positions containing acidic peptide motifs, thereby inhibiting cancer cell proliferation, and activates the integrated stress response via eIF2α phosphorylation at high concentrations. In addition, IDB-001 mildly triggers ribotoxic stress responses through phosphorylation of JNK and p38. IDB-001 has been applied to mechanistic studies of triple-negative breast cancer .
    IDB-001
  • HY-173189A

    2′,5′-ApApA pentasodium; 2′,5′-trioligoadenylate pentasodium; 5'-O-Triphosphoryladenylyl-(2'→5')-adenylyl-(2'→5')-adenosine pentasodium

    RSV DNA/RNA Synthesis Infection Cancer
    2-5A (2′,5′-ApApA) pentasodium solution 100 mM is a high-affinity (Ka=0.04 nM) RNase L binder. 2-5A pentasodium solution 100 mM activates the nuclease activity of latent RNase L to cleave single-stranded RNA by inducing conformational changes and dimerization of latent RNase L, thereby mediating critical antiviral responses and enhancing interferon effects. 2-5A pentasodium solution 100 mM not only effectively inhibits Rauscher murine leukemia virus replication, reduces viremia and splenomegaly, but also enhances antileukemic efficacy when combined with amphotericin B and exhibits favorable high-dose tolerance. 2-5A pentasodium solution 100 mM is an important tool molecule for investigating the pathological mechanisms of viral infection, hereditary prostate cancer and leukemia .
    2-5A pentasodium solution (100 mM)
  • HY-N3103

    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-150784

    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-P1740A
    RGD peptide (GRGDNP) TFA
    5+ Cited Publications

    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-160528
    IBG3
    1 Publications Verification

    Epigenetic Reader Domain Molecular Glues Cancer
    IBG3 is a Molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia .
    IBG3
  • HY-162809

    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 for the study of colon, lung and pancreatic cancer .
    XMU-MP-9
  • HY-101083

    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-100662

    Bisdesethylchloroquine

    Drug Metabolite Cardiovascular Disease Infection
    Didesethyl chloroquine (Bisdesethylchloroquine) is the major metabolite of the antimalarial agent Chloroquine (HY-17589A). Didesethyl chloroquine is a potent myocardial inhibitor. Didesethyl chloroquine reduces calcium binding and accumulation in cardiac mitochondria, induces mitochondrial swelling, rupture and membrane conformational changes. Didesethyl chloroquine inhibits the growth of Plasmodium falciparum strains. Didesethyl chloroquine can be used in research related to malaria, chikungunya virus infection, and cardiovascular and cerebrovascular diseases .
    Didesethyl chloroquine
  • HY-Y0788

    HIV Infection
    Indoline is a derivative of Indole (HY-W001132). Indoline can use 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 binds to gp120. Indoline CD4mcs can inhibit HIV-1AD8 with an IC50 in the micromolar range .
    Indoline
  • HY-D0193A

    Acid Red 18 (85%); New Coccine (85%)

    Environmental Pollutants Drug Derivative Neurological Disease Inflammation/Immunology
    Ponceau 4R (85%) (Acid Red 18 (85%); New Coccine (85%)) is an orally active synthetic food colorant and a HSA-binding aggregator. Ponceau 4R (85%) binds to HSA, inducing its partial unfolding, conformational changes and aggregation. Ponceau 4R (85%) serves as a food colorant and can be used in research on diseases including type Ⅱ diabetes, Parkinson's disease, Huntington's disease and spongiform encephalopathy .
    Ponceau 4R (85%)
  • HY-P1793

    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-122106

    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-B0956A

    Aminosidine

    Bacterial Parasite Endogenous Metabolite Infection
    Paromomycin (Aminosidine) is an orally active broad-spectrum aminoglycoside aminocyclitol. Paromomycin is produced by Streptomyces riomosus var. Paromomycinus. Paromomycin binding induces local conformational changes in the 16S rRNA A-site. Paromomycin exhibits inhibitory activity against C. parvum. Paromomycin can be used in research related to leishmaniasis, amoebiasis and cryptosporidiosis .
    Paromomycin
  • HY-P10948A

    WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 hydrochloride 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 hydrochloride is promising for research of hematological diseases such as leukemia .
    CS-VIP 8 hydrochloride
  • HY-107401

    SCH-351125

    HIV CCR Calcium Channel Infection
    Ancriviroc (SCH-351125) is an orally active CCR5 antagonist with an IC50 value of 13 nM against hCCR5. Ancriviroc specifically binds to hCCR5, blocks ligand-induced signal transduction, calcium influx, GTPγS binding, chemotaxis, ligand binding, and HIV-1 entry, induces conformational changes in CCR5, and inhibits infection and replication of R5-tropic HIV-1 .
    Ancriviroc
  • HY-P10941A

    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-P11107

    Apoptosis TNF Receptor Inflammation/Immunology Cancer
    RP-832c is a synthetic analogue of host defense peptides (HDP), targeting the mannose receptor CD206 on the surface of M2 polarized macrophages (Kd = 3.5 μM). RP-832c binding to CD206 induces a significant conformational change in the receptor, activating signaling pathways that lead to rapid apoptosis and repolarization of CD206-positive M2 macrophages to an M1 phenotype. RP-832c treatment significantly reduces CD206 gene expression in M2 macrophages while transiently increasing expression of TNF-α, a marker for M1 macrophages. RP-832c is used for the studies of T-cell lymphoma (CTCL) and idiopathic pulmonary fibrosis (IPF) .
    RP-832c
  • HY-P11430

    Biochemical Assay Reagents Infection
    UBI (31-38) is a Ubiquicidin-derived octapeptide and anti-bacterial agent. UBI (31-38) selectively interacts with anionic phospholipid membranes and restricts lipid lateral motion. UBI (31-38) induces anionic vesicle aggregation via electrostatic repulsion screening, and undergoes conformational changes in membrane-mimicking environments. UBI (31-38) can be used for the research of infection imaging probes .
    UBI (31-38)
  • HY-P10941

    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-150184

    DNA/RNA Synthesis Cancer
    And1-IN-1 is a potent And1 inhibitor with an IC50 of 2.08 μM. And1-IN-1 binds to the N-terminus of And-1 and induces a conformational change in And-1, which promotes the interaction of And-1 with E3 ligase CUL4B for ubiquitin-mediated degradation. And1-IN-1 suppresses the growth of a broad range of cancers and resensitizes platinum-resistant ovarian cancer cells to platinum agents. And1-IN-1 can be used for the studies of ovarian cancer and breast cancer .
    And1-IN-1
  • HY-P10948

    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-164895

    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-P2516

    Tau Protein Neurological Disease
    Tau Peptide (275-305) (Repeat 2 domain) is the Alzheimer's Tau fragment R2, corresponding to the second repeat unit of the microtubule-binding domain, which is believed to be pivotal to the biochemical properties of full tau protein. Tau Peptide (275-305) specifically coordinates with group IIB metal ions (Zn²⁺, Cd²⁺, Hg²⁺), which can induce their conformational changes and significantly promote their pathological accumulation. Tau Peptide (275-305) can be used to study the role of heavy metals in neurodegenerative diseases .
    Tau Peptide (275-305) (Repeat 2 domain)
  • HY-177906

    Fluorescent Dye Amyloid-β Neurological Disease
    h-FTAA is a luminescent conjugated oligothiophene (LCO) probe. h-FTAA can selectively bind to amyloid protein aggregates (such as plaques) and distinguish different conformations of the protein aggregates through changes in fluorescence signals. h-FTAA significantly reduces the neurotoxicity of Aβ1-42 and the Arctic mutant Aβ (AβArc), thereby protecting SH-SY5Y neuroblastoma cells. h-FTAA can be used to dynamically track the formation and maturation process of Aβ plaques .
    h-FTAA
  • HY-121817

    Aldehyde Dehydrogenase (ALDH) Drug Intermediate Amyloid-β Infection Neurological Disease
    Sulfiram is a very weak aldehyde dehydrogenase (ALDH) inhibitor, with an IC50 value of 413 μM against Saccharomyces cerevisiae ALDH. As a photochemical precursor, Sulfiram undergoes photoconversion to form Disulfiram (HY-B0240), a potent ALDH inhibitor. Sulfiram inhibits the dimerization of the extracellular domain fragment (amino acid residues 230-624) of amyloid precursor protein (APP), alters the monomer-dimer equilibrium, induces conformational changes in the fragment, and enhances the production of sAPPα via α-cleavage of APP. Sulfiram can be used in research related to scabies and Alzheimer's disease .
    Sulfiram
  • HY-175838

    P-glycoprotein Cancer
    P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .
    P-gp-IN-32
  • HY-135903

    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-145391

    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-Y0788R

    Reference Standards 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 (Standard)
  • HY-161276
    BFC1108
    1 Publications Verification

    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

    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-E70763

    PDGFR Cancer
    PDGFRalpha is a receptor tyrosine kinases that stimulate cell survival, proliferation and motility. Upon PDGF binding, the receptor dimerizes and undergoes a conformational change, which activates the kinase domain. PDGFRalpha T674I is a mutant of PDGFRalpha. PDGFRalpha T674I Recombinant Human Active Protein Kinase is a recombinant PDGFRalpha T674I protein that can be used to study PDGFRalpha T674I-related functions .
    PDGFRalpha T674I Recombinant Human Active Protein Kinase
  • HY-169846

    Sirtuin Metabolic Disease
    CL5D is an activator of protein deacetylase SIRT6. CL5D can significantly enhance the deacetylation activity of SIRT6 and improve its catalytic efficiency. CL5D regulates SIRT6 activity by promoting conformational changes, especially dependent on the role of Arg-65 residue. CL5D can be used to study the activation mechanism of SIRT6 and its function in metabolism, DNA repair and aging .
    CL5D

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