2. Signaling Pathways
  3. Immunology/Inflammation
  4. IKZF Family

IKZF Family

Ikaros zinc finger protein family

IKZF family is a group of transcription factor families that play a crucial role in processes such as lymphopoiesis, differentiation, and functional regulation of lymphocytes. The proteins of its members have specific zinc finger domains in their structures, which can interact with DNA or other proteins, thus regulating the gene transcription process. As transcriptional repressors and activators, members of the IKZF family are of great significance in the differentiation of hematopoietic stem cells into lymphocytes, as well as in the differentiation and function exertion of T and B cells. In addition, members of the IKZF family can regulate gene expression through various mechanisms, including remodeling chromatin structure, promoting the activity of the RNA Pol II transcription initiation complex, and inducing chromosome conformational changes, etc. Mutations or abnormal functions of the members of the IKZF family are associated with a variety of diseases, such as B cell deficiency, leukemia, and autoimmune diseases[1].

IKZF Family Isoform Specific Products:

IKZF Family Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-168614
    MGD-4
    		Degrader
    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-103484
    GATA4-NKX2-5-IN-1
    		Inhibitor 99.24%
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
    GATA4-NKX2-5-IN-1
  • HY-157428
    USP3 ZnF-UBD ligand-1
    		99.61%
    USP3 ZnF-UBD ligand-1 (compound 59) is a ligand that binds to the zinc finger ubiquitin-binding domain (ZnF-UBD) of USP3 with a KD of 14 μM.
    USP3 ZnF-UBD ligand-1
  • HY-174458
    MD-4251
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model. Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • HY-179075
    PROTAC BCL6/IKZF1/3 Degrader-1
    		Degrader
    PROTAC BCL6/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BCL6/IKZF1/3 Degrader-1 exhibits superior antiproliferative effects in various germinal center B-cell-like (GCB) and activated B-cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cell lines. PROTAC BCL6/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179064); Blue: CRBN ligand (HY-41547); Black: linker (HY-42427); CRBN ligand-Linker: (HY-179066))
    PROTAC BCL6/IKZF1/3 Degrader-1
  • HY-177754
    IKZF2-degrader 3
    		Degrader
    IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM.
    IKZF2-degrader 3
  • HY-170518
    IKZF-IN-1
    		Inhibitor
    IKZF-IN-1 (Compound I) is the molecular glue, that degrades ikaros zinc finger family (IKZF) IKZF 1/2/3/4, and can be used as an immunomodulator in research of cancer and viral infections.
    IKZF-IN-1
  • HY-181651
    SZU305
    		Inhibitor
    SZU305 is a RAD51 PROTAC degrader, with DC50 values of 307.45 nM and 84.19 nM in SK-HEP-1 and Huh-7 cells, respectively. SZU305 inhibits DNA damage repair, induces cell cycle arrest and apoptosis. SZU305 moderately reduces the protein levels of IKZF1 and IKZF3 at high concentrations. SZU305 can be used in studies related to hepatocellular carcinoma.
    SZU305
  • HY-182799
    IBA-12
    		Degrader
    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-169077
    IKZF3 degrader 1
    		Degrader
    IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3.
    IKZF3 degrader 1
  • HY-175601
    DD-04-038
    		Degrader
    DD-04-038 is a molecular glue degrader. DD-04-038 induces proteins (such as IKZF1/3, ZBED3 and PATZ1) to bind to CRBN, promoting their ubiquitination and degradation.
    DD-04-038
  • HY-180836
    DIX-01
    		Degrader
    DIX-01 is a molecular gel degrader that can simultaneously induce the degradation of IKZF1/3 and GSPT1 mediated by CRBN. Its DC50 values are: IKZF1 (19.80 nM), IKZF3 (45.31 nM), and GSPT1 (120.1 nM). DIX-01 exhibits nanomolar-level potent anti-proliferative activity in various cancer cell lines. DIX-01 induces apoptosis in MV4-11 cells and significantly inhibits the growth of leukemia cells in zebrafish. DIX-01 can be used for the study of malignant hematological tumors.
    DIX-01
  • HY-175502
    MGD-22
    		Degrader
    MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).
    MGD-22
  • HY-175040
    PROTAC FLT-3 degrader 5
    		Degrader
    PROTAC FLT-3 degrader 5 is a FLT3 PROTAC degrader (DC50 = 1.2 nM). PROTAC FLT-3 degrader 5 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT-3 degrader 5 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide: (HY-14658); Black: linker; Thalidomide + linker: (HY-W1123823)).
    PROTAC FLT-3 degrader 5
  • HY-179076
    BTK/IKZF1/3 ligand 1
    		Ligand
    BTK/IKZF1/3 ligand 1 is a BTK/IKZF1/3 PROTAC ligand. BTK/IKZF1/3 ligand 1 can be conjugated with E3 ligase Ligand (HY-41547) and linker to synthesize PROTAC BTK/IKZF1/3 Degrader-1 (HY-179077). PROTAC BTK/IKZF1/3 Degrader-1 can be used for cancer research.
    BTK/IKZF1/3 ligand 1
  • HY-160533
    IKZF1-degrader-2
    		Degrader
    IKZF1-degrader-2 (Compound 3) is an IKZF1 molecular glues degrader. IKZF1-degrader-2 has anticancer activity and low toxicity.
    IKZF1-degrader-2
  • HY-W1128213
    IKZF2-degrader 2
    		Degrader
    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-182945
    IKZF2-degrader 5
    		Degrader
    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-175602
    TM-04-064-02
    		Degrader
    TM-04-064-02 is a molecular glue degrader. TM-04-064-02 induces proteins (such as IKZF1/3, PPIL4, ETF1 and PDE6D) to bind to CRBN, promoting their ubiquitination and degradation.
    TM-04-064-02
  • HY-172882
    IKZF2-degrader 1
    		Degrader
    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
IKZF Family Isoform Comparison

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