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homologous targeting

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14805
    Tecovirimat
    1 Publications Verification

    ST-246

    Orthopoxvirus Arenavirus Infection
    Tecovirimat (ST-246) is an orally bioavailable and selective compound against orthopoxviruses including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus .
    Tecovirimat
  • HY-174374

    Topoisomerase Cardiovascular Disease
    Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .
    Topobexin
  • HY-145685

    DNA/RNA Synthesis Cancer
    RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells .
    RECQL5-IN-1
  • HY-14805A
    Tecovirimat monohydrate
    1 Publications Verification

    ST-246 monohydrate

    Orthopoxvirus Arenavirus Infection
    Tecovirimat (ST-246) monohydrate is the monohydrate form of Tecovirimat (HY-14805). Tecovirimat monohydrate is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat monohydrate is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat monohydrate targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat monohydrate exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat monohydrate could be used in the study for orthopoxvirus-induced diseases .
    Tecovirimat monohydrate
  • HY-W023758

    4-(4-Bromo-1H-pyrazol-5-yl)pyridine

    DNA/RNA Synthesis Cancer
    HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
    HDGFRP2/PSIP1-IN-1
  • HY-14805S

    ST-246-d4

    Isotope-Labeled Compounds Orthopoxvirus Arenavirus Infection
    Tecovirimat-d4 (ST-246-d4) is a deuterium-labelled Tecovirimat (HY-14805). Tecovirimat is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat could be used in the study for orthopoxvirus-induced diseases .
    Tecovirimat-d4
  • HY-177971

    Antibody-Oligonucleotide Conjugates (AOCs) Neurological Disease
    Braxlosiran, one of the components of the AOC Delpacibart braxlosiran (HY-177566), is composed of a siRNA targeting DUX4 (dual homologous box protein) and SMCC linker (HY-42360). Abnormal expression of the DUX4 protein leads to changes in gene expression in muscle cells, and these changes are associated with the loss of muscle function in facioscapulohumeral muscular dystrophy (FSHD) .
    Braxlosiran
  • HY-174499

    mRNA Others
    Cas9 Nickase D10A mRNA expresses a version of the Streptococcus pyogenes SF370 Cas9 protein (CRISPR Associated Protein 9) that contains a D10A amino acid substitution. This mRNA also contains a C-terminal nuclear localization signal followed by a HA tag.Cas9 functions as part of the CRISPR (clustered regularly interspaced short palindromic repeats) genome editing system. In the CRISPR system, an RNA guide sequence targets the site of interest and the Cas9 protein is employed to perform the DNA cleavage. While wild-type Cas9 creates a double-stranded break at the target site, Cas9 nickase creates a single-stranded break. This favors homology-directed repair and decreases the occurrence of non-homologous end joining.
    Cas9 Nickase D10A mRNA (5moU)
  • HY-175466

    PARP DNA/RNA Synthesis Apoptosis Cancer
    BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib (HY-10162). BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
    BER-IN-1
  • HY-149489

    PKC Neurological Disease
    JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases .
    JH-131e-153
  • HY-120750

    Endogenous Metabolite Cancer
    A 62176 hydrochloride is a compound that targets DNA topoisomerase II and has the activity of inhibiting purine synthesis in cancer cells. A 62176 hydrochloride interferes with c-MYC mRNA expression by interacting with G-quadruplex. The main mechanism of action of A 62176 hydrochloride is by displacing nucleosomes from the quadruplex of non-template strand rDNA, resulting in rapid redistribution of nucleosomes. The application potential of A 62176 hydrochloride is that it causes DNA damage and relies on BRCA1/2-mediated homologous recombination and DNA-PK-mediated non-homologous end-joining pathways to repair the damage .
    A 62176 hydrochloride
  • HY-N10648

    Phosphatase Metabolic Disease
    PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
    PTP1B-IN-20
  • HY-168646

    Ligands for E3 Ligase Molecular Glues Cancer
    SJ46411-Br is one of CRL2 KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs .
    SJ46411-Br
  • HY-P992033

    Interleukin Related Cancer
    Anti-Mouse IL-4Rα Antibody (REGN1103) is a mouse homologous antibody targeting IL-4Rα, as well as an inhibitor of IL-4 signaling. Anti-Mouse IL-4Rα Antibody (REGN1103) can be used in studies related to alveolar rhabdomyosarcoma .
    Anti-Mouse IL-4Rα Antibody (REGN1103)
  • HY-181694

    Topoisomerase HDAC Apoptosis Kinesin RAD51 Cancer
    SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity .
    SeSA-HCPT
  • HY-P11757

    EGFR Cancer
    Cyclo[K(N3)larllt] is a seven-membered cyclic peptide targeting EGFR, with a Kd value of 5.09 μM, and exhibits binding selectivity toward homologous proteins HER2 and HER3. Cyclo[K(N3)larllt] has no cytotoxicity and shows no growth inhibitory effect on cancer cells overexpressing EGFR. Cyclo[K(N3)larllt] can serve as a ligand for EGFR-targeted fluorescent conjugates, which is applicable to the detection of cancers with EGFR overexpression. Cyclo[K(N3)larllt] can be used in the research of colorectal cancer .
    Cyclo[K(N3)larllt]
  • HY-P992365

    CCR Cancer
    HFB101110 is a human-derived inhibitor and Treg depleter that specifically targets CCR8. It does not bind to the homologous CCR4 receptor and is mainly used in research on solid tumors, renal cell carcinoma and colorectal cancer. HFB101110 blocks hCCL1 binding by interacting with the N-terminal extracellular domain of hCCR8, thereby inhibiting hCCL1-induced calcium influx, chemotaxis and downstream signaling pathways. Meanwhile, HFB101110 can mediate ADCC effects to specifically deplete CCR8-positive cells, including intratumoral Tregs. HFB101110 exhibits favorable anti-tumor activity and pharmacokinetic properties .
    HFB101110

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