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N-terminal domain

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

1

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5

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6

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5

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3

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-123875A

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .
    Ralaniten triacetate
  • HY-P10152

    Biochemical Assay Reagents Infection
    INF7 is a derivative of the N-terminal domain of the HA2 protein and is sensitive to pH. INF7 disrupts the stability of endosomal membranes through a mechanism independent of membrane fusion. INF7 can be used to enhance the endosome escape of complex or liposome-encapsulated proteins. Co-encapsulation of INF7 and molecular imaging probes in liposomes can enhance intracellular signaling and probe retention .
    INF7
  • HY-103076
    EZ-482
    1 Publications Verification

    Apolipoprotein Neurological Disease
    EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas .
    EZ-482
  • HY-150102

    Androgen Receptor Cancer
    EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
    EPI-7170
  • HY-P99777
    Ontorpacept
    1 Publications Verification

    TTI-621

    CD47 Cancer
    Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blocking checkpoint inhibitor with antitumor activity .
    Ontorpacept
  • HY-109070

    EPI-002

    Androgen Receptor Cancer
    Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
    Ralaniten
  • HY-16663
    ITX3
    2 Publications Verification

    ROCK Others
    ITX3 is a specific and nontoxic inhibitor of TrioN (N-terminal GEF domain of the multidomain Trio protein) with an IC50 value of 76 μM. ITX3 can be used for the research of agent .
    ITX3
  • HY-106723A
    AMP-PCP disodium
    1 Publications Verification

    HSP Cancer
    AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90 .
    AMP-PCP disodium
  • HY-152078

    Influenza Virus Infection
    Influenza virus-IN-6 (Compound 35) is a potent influenza N-terminal domain of the polymerase acidic protein subunit (PAN) endonuclease inhibitor with an IC50 of 0.20 μM .
    Influenza virus-IN-6
  • HY-106723

    HSP Cancer
    AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90 .
    AMP-PCP
  • HY-139831

    Galectin Cancer
    Galectin-8-IN-1 is a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a Kd of 48 μM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins.
    Galectin-8-IN-1
  • HY-P2490

    Thrombin Metabolic Disease
    Acetyl-Hirudin (54-65) (sulfated) is a acetyl-fragment of Hirudin which binds directly to thrombin-rHCII(L444R) and disrupts interactions between the N-terminal acidic domain of rHCII and anion-binding exosite I of thrombin that serves to stabilize the complex .
    Acetyl-Hirudin (54-65) sulfated
  • HY-138779
    ICCB-19 hydrochloride
    1 Publications Verification

    Autophagy RIP kinase Apoptosis Inflammation/Immunology
    ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds with N-terminal domain of TRADD (TRADD-N), disrupting its binding to both TRADD-C and TRAF2. ICCB-19 hydrochloride is indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and the degradation of long-lived proteins .
    ICCB-19 hydrochloride
  • HY-138155

    DNA/RNA Synthesis Cancer
    NSC15520 is a small molecular inhibitor of Replication Protein A (RPA). NSC15520 specifically recognizes the RPA N-terminal DNA binding domain (DBD), and blocks the interaction of RPA with p53 or RAD9. NSC15520 also inhibtis helix destabilization of a duplex DNA (dsDNA) oligonucleotide, involves in DNA replication, DNA repair, DNA recombination, and DNA damage response signaling .
    NSC15520
  • HY-155478

    Androgen Receptor Cancer
    Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
    Androgen receptor-IN-6
  • HY-P991158

    TGF-β Receptor Neurological Disease
    Rinvatercept, a fusion protein, is a glycyl (1)-chimeric N-terminal (1-108)-peptide (2-109) combined from the sequences of the extracellular domains of the human ACVR2A/B, and is fused via a G3 peptide linker (110-112) to an immunoglobulin G1 (IgG1) Fc fragment. Rinvatercept can be used for research of neuromuscular disease .
    Rinvatercept
  • HY-114855
    BT2
    Maximum Cited Publications
    8 Publications Verification

    Bcl-2 Family Metabolic Disease
    BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC) . BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM .
    BT2
  • HY-103078

    HIV Infection
    I-XW-053 is an inhibitor of HIV-1 capsid protein that can suppress the replication of HIV-189BZ167 with an IC50 value of 164.2 μM. I-XW-053 exhibits antiviral activity and can block the interface between capsid protein (CA) N-terminal domains (NTD-NTD interface) with micromolar affinity .
    I-XW-053
  • HY-103078A

    HIV Infection
    I-XW-053 is an inhibitor of HIV-1 capsid protein that can suppress the replication of HIV-189BZ167 with an IC50 value of 164.2 μM. I-XW-053 exhibits antiviral activity and can block the interface between capsid protein (CA) N-terminal domains (NTD-NTD interface) with micromolar affinity .
    I-XW-053 sodium
  • HY-E70691

    CDK Cancer
    CLK1 is one of the dual specificity kinases and is the founding member of the 'LAMMER' family of kinases. CLK1 activity is positively regulated by phosphorylation on either tyrosine residues or serine/threonine residues, and is negatively regulated by steric constraints mediated by the N-terminal domain, as well as, by phosphorylation on a subset of serine/threonine residues within the catalytic domain. CLK1 Recombinant Human Active Protein Kinase is a recombinant CLK1 protein that can be used to study CLK1-related functions .
    CLK1 Recombinant Human Active Protein Kinase
  • HY-W286614

    Ribosomal S6 Kinase (RSK) Inflammation/Immunology Cancer
    RSK2-IN-4 (Compound 10) is a RSK2 inhibitor, with an inhibition rate of 13.73% on RSK2 activity at 10 μM. RSK2-IN-4 binds to the ATP-binding site of RSK2 in the NTKD (N-terminal kinase domain), with the electron-donating group at the 4-position of the phenyl ring being the key determinant for its inhibitory activity .
    RSK2-IN-4
  • HY-P5320

    Apoptosis Others
    TAT-BH4 (Bcl-xL) localized mainly at the mitochondria, prevents apoptotic cell death. TAT-BH4 (Bcl-xL) is a fusion peptide that combines the N-terminal cysteine conjugated protein transduction domain of HIV TAT protein (amino acids 49 to 57) with the Bcl-xL BH4 peptide. TAT-BH4 can be used for research of diseases caused by accelerated apoptosis .
    TAT-BH4 (Bcl-xL)
  • HY-P990986

    Interleukin Related Inflammation/Immunology Cancer
    Efdelikofusp alfa is a bispecific Fc fusion protein. Efdelikofusp alfa is formed by fusing the N-terminal extracellular domain of human CD80 (B7.1) with the Fc fragment of human immunoglobulin G4 (IgG4), and is linked to an interleukin-2 variant (IL-2v) as the C-terminal part. Efdelikofusp alfa exhibits potential immunostimulatory, immune checkpoint inhibitory, and antitumor activities.
    Efdelikofusp alfa
  • HY-P990992

    Interleukin Related Inflammation/Immunology Cancer
    Efzilonkofusp alfa is a bispecific Fc fusion protein. Efzilonkofusp alfa is formed by fusing the N-terminal extracellular domain of human CD80 (B7.1) with the Fc fragment of human immunoglobulin G4 (IgG4), and is linked to an interleukin-2 variant (IL-2v) as the C-terminal part. Efzilonkofusp alfa exhibits potential immunostimulatory, immune checkpoint inhibitory, and antitumor activities.
    Efzilonkofusp alfa
  • HY-P5320A

    Apoptosis Others
    TAT-BH4 (Bcl-xL) TFA is localized mainly at the mitochondria, prevents apoptotic cell death. TAT-BH4 (Bcl-xL) is a fusion peptide that combines the N-terminal cysteine conjugated protein transduction domain of HIV TAT protein (amino acids 49 to 57) with the Bcl-xL BH4 peptide. TAT-BH4 TFA can be used for research of diseases caused by accelerated apoptosis .
    TAT-BH4 (Bcl-xL) TFA
  • HY-119906

    FW-04-806

    HSP Apoptosis Cancer
    Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo .
    Conglobatin
  • HY-P991611

    iGluR Inflammation/Immunology
    ART5803 is a humanized IgG1 monoclonal antibody inhibitor targeting NMDAR. ART5803 binds to the N-terminal domain (NTD) of the NMDAR GluN1 subunit (GluN1-NTD) with a high affinity. ART5803 blocks NMDAR internalization induced by pathogenic autoantibodies and restores cell-surface NMDAR expression and functions. ART5803 reverses behavioral abnormalities and NMDAR expression in marmoset disease models. ABT-147 can be used to study anti-NMDAR encephalitis .
    ART5803
  • HY-N15327

    HIV HIV Integrase Infection
    Hyrtiosal, found in the marine sponge Hyrtios erectus, is an inhibitor of the N-terminal domain (NTD) of HIV-1 integrase (HIV-1 IN) with an IC50 value of 9.60-0.86 μM. Hyrtiosal binds to the Ser17, Trp19, and Lys34 sites on the NTD of HIV-1 IN, inhibiting the binding of HIV-1 viral DNA to integrase and interfering with the formation of the pre-integrated complex of HIV-1. Hyrtiosal is promising for research of anti-HIV agents .
    Hyrtiosal
  • HY-172736

    PROTACs BCL6 Cancer
    BMS-986458 is a highly selective and orally active BCL6 PROTAC degrader. BMS-986458 simultaneously co-opts cereblon (CRBN) and the BCL6 N-terminal BTB domain to catalyze proximity induced degradation of BCL6. BMS-986458 can be used for the study of B-cell Non-Hodgkin's lymphoma (Pink: Target protein ligand (HY-172740); Black: linker (HY-W267161); Blue: E3 ligase ligand (HY-W593794)) .
    BMS-986458
  • HY-149434

    Androgen Receptor PROTACs Apoptosis Cancer
    PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
    PROTAC AR-NTD degrader 1
  • HY-164373

    Androgen Receptor Apoptosis Cancer
    SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
    SC428
  • HY-149433

    Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
    BWA-522
  • HY-P990816

    SARS-CoV Infection
    Anti-SARS-CoV-2 S protein Antibody (NTD, SARS2-29) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to SARS-CoV-2 S protein. Anti-SARS-CoV-2 S protein Antibody (NTD, SARS2-29) reacts with the N-terminal domain (NTD) in the spike (S) protein of SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2). Anti-SARS-CoV-2 S protein Antibody (NTD, SARS2-29) can be used for the detections of flow cytometry and ELISA in SARS-CoV-2 infection .
    Anti-SARS-CoV-2 S protein Antibody (NTD, SARS2-29)
  • HY-143418

    SARS-CoV Infection
    SARS-CoV-2-IN-17 (Compound 16) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-17 exhibits potent anti-viral activity with the EC50 of 2.18 μM. SARS-CoV-2-IN-17 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-17 is a potent NPro ligand .
    SARS-CoV-2-IN-17
  • HY-143417

    SARS-CoV Infection
    SARS-CoV-2-IN-16 (Compound 12) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-16 exhibits potent anti-viral activity with the EC50 of 3.69 μM. SARS-CoV-2-IN-16 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-16 is a potent NPro ligand .
    SARS-CoV-2-IN-16

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