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IKZF2 degradation

" in MedChemExpress (MCE) Product Catalog:

20

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Peptides

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-122542B
    PPACK TFA
    2 Publications Verification

    Ligands for E3 Ligase Molecular Glues IKZF Family Cardiovascular Disease
    PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8 + T cell responses, and modulates the Teff:Treg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .
    PPACK TFA
  • HY-173630

    Molecular Glues IKZF Family Cancer
    BMS-986449 is a potent and orally active CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors .
    BMS-986449
  • HY-172931

    Molecular Glues Casein Kinase IKZF Family Cancer
    DEG-35 is a CRBN-dependent, dual IKZF2 and CK1α molecule glue degrader, with DC50 values of 1.4 nM and 4.4 nM for CK1α and IKZF2, respectively. DEG-35 activates the p53 apoptosis pathway. DEG-35 can be used in the research for Acute Myeloid Leukemia (AML) .
    DEG-35
  • HY-145776

    Molecular Glues Ligands for E3 Ligase IKZF Family Interleukin Related Inflammation/Immunology Cancer
    ALV1 is a molecular glue degrader for Ikaros (IKZF1) and Helios (IKZF2) with DC50 of 2.5 nM and 10.3 nM respectively. ALV1 bind CRBN with an IC50 of 0.55 μM, and induces CRBN-Helios dimerization. ALV1 can be used to study the properties and functions of regulatory T cells .
    ALV1
  • HY-159647A

    Molecular Glues IKZF Family Cancer
    (S,S)-PLX-4545 (Compound I) is an orally active and cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios). (S,S)-PLX-4545 can be used for the study of IKZF2-mediated diseases or disorders, such as proliferative diseases or disorders and/or cancer .
    (S,S)-PLX-4545
  • HY-122542A
    PPACK dihydrochloride
    2 Publications Verification

    Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl

    Ligands for E3 Ligase Molecular Glues IKZF Family Cardiovascular Disease
    PPACK dihydrochloride is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK dihydrochloride binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8 + T cell responses, and modulates the Teff:Treg balance. PPACK dihydrochloride also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK dihydrochloride can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .
    PPACK dihydrochloride
  • HY-159647

    Molecular Glues Ligands for E3 Ligase IKZF Family Cancer
    PLX-4545 is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PLX-4545 binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8 + T cell responses, and modulates the Teff:Treg balance. PLX-4545 also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PLX-4545 can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1 .
    PLX-4545
  • HY-173630A

    Molecular Glues IKZF Family Cancer
    (R)-BMS-986449 is the racemic mixture of BMS-986449 (HY-173630). BMS-986449 is a CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors .
    (Rac)-BMS-986449
  • HY-159647B

    Molecular Glues IKZF Family Cancer
    (1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545 (HY-159647). PLX-4545 is an orally active and selective cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios). PLX-4545 can reprogram immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses .
    (1S,2S,3R)-PLX-4545
  • HY-168615

    IKZF Family Casein Kinase Cancer
    MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research .
    MGD-28
  • HY-172930

    Molecular Glues IKZF Family Potassium Channel Inflammation/Immunology Cancer
    PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50  of  0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
    PVTX-405
  • HY-172882

    Molecular Glues IKZF Family Cancer
    IKZF2-degrader 1 (Compound 31) is a IKZF2 molecular glue degrader, with an DC50 of 0.5 nM. IKZF2-degrader 1 has minimal CK1α degradation activity relatively (DC50: 210 nM). IKZF2-degrader 1 can be used for research of IKZF2-dependent cancers .
    IKZF2-degrader 1
  • HY-177754

    Molecular Glues IKZF Family Inflammation/Immunology
    IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM .
    IKZF2-degrader 3
  • HY-W1128213

    Molecular Glues IKZF Family Inflammation/Immunology Cancer
    IKZF2-degrader 2 is a selective and orally active IKZF2 molecular glue degrader with DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS. The IKZF2-degrader 2 mediates the ubiquitination and degradation of target proteins by recruiting the CRL4-CRBN E3 ubiquitin ligase. IKZF2-degrader 2 displays moderate degradation against SALL4 with a DC50 of 9 nM but does not induce any significant degradation towards IKZF1, IKZF3, CK1α and GSPT1. IKZF2-degrader 2 can be used for the study of cancer immunology .
    IKZF2-degrader 2
  • HY-168614

    IKZF Family Cancer
    MGD-4 is an orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM) in a dose-dependent manner. MGD-4 effectively inhibits the growth of multiple myeloma .
    MGD-4
  • HY-182945

    Molecular Glues IKZF Family HOXA Interleukin Related NF-κB Cancer
    IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma .
    IKZF2-degrader 5
  • HY-185300

    IKZF Family Molecular Glues Cancer
    IKZF2-degrader 4 (Page 650, third compound from the top in the right column) is an IKZF2 Molecular glue degrader. IKZF2-degrader 4 degrades IKZF2 protein. IKZF2-degrader 4 can be used in the research of cancer .
    IKZF2-degrader 4
  • HY-182799

    PROTACs Molecular Glues IKZF Family Cancer
    IBA-12 is a IKZF2 molecular glue/PROTAC degrader with a DC50 of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC50 of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research .
    IBA-12
  • HY-182808

    E3 Ligase Ligand-Linker Conjugates Others
    E3 Ligase Ligand-linker Conjugate 230 is an E3 ligase ligand-linker conjugate that can be used for the synthesis of PROTACs, such as IBA-12 (HY-182799) .
    E3 Ligase Ligand-linker Conjugate 230

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