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
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IKZF Family Related Products (72)
Related Products (72)
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IKZF Family Isoform Comparison
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MGD-28
0 ImagesMGD-28 is an orally effective cereblon-dependent molecular glue degrader that potently degrades CK1α, IKZF1, IKZF2, and IKZF3, with respective DC50 values of 7.8, 3.8, 56.3, and 7.1 nM. MGD-28 also induces the degradation of multiple novel substrate proteins including ZFP91, DTWD1, ZNFX1, MBD1, and MBD3 via a CRBN/Cullin- and proteasome-dependent mechanism. MGD-28 induces cell apoptosis. MGD-28 is used in the research of multiple myeloma, acute myeloid leukemia, diffuse large B-cell lymphoma, and related malignancies.
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(Rac)-BMS-986449
0 ImagesCat. No.: HY-173630APurity: 99.05%(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.
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PVTX-405
0 ImagesCat. No.: HY-172930CAS No.: 2991021-08-8PVTX-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 Crbn391V C57BL/6 mice.
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FIZ1 degrader 1
0 ImagesFIZ1 degrader 1 is an IMiD-based molecular glue degrader. FIZ1 degrader 1 induces CRBN-dependent FIZ1 ubiquitination and proteasomal degradation; inhibition of the proteasome, ubiquitination or ubiquitination-like processes blocks this degradation. FIZ1 degrader 1 also induces the degradation of IKZF1, IKZF3 and ZFP91. FIZ1 degrader 1 is applicable to molecular glue-related research.
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BMS-986449
0 ImagesCat. No.: HY-173630BMS-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.
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Cisd2 agonist 2
0 ImagesCisd2 agonist 2 (compound 6) is a Cisd2 activator (EC50=191 nM), and Cisd2 levels are associated with non-alcoholic fatty liver disease (NAFLD). Cisd2 agonist 2 has no significant in vivo toxicity in Cisd2hKO-het mice (heterozygous hepatocyte-specific Cisd2 knockout). Cisd2 (CDGSH iron sulfur domain 2) is a zinc finger protein that is mainly localized in the endoplasmic reticulum or mitochondrial membrane. Cisd2 participates in mitochondrial function by forming homodimers containing two redox-active 2Fe-2S clusters.
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(1S,2S,3R)-PLX-4545
0 ImagesCat. No.: HY-159647BCAS No.: 2892066-42-9(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.
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BMS-986482
0 ImagesCat. No.: HY-182467CAS No.: 3062993-48-7BMS-986482 is a CRBN-mediated IKZF1-4 (Ikaros family zinc finger 1-4) molecular glue degrader. BMS-986482's activity is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 can be used for the research of advanced solid tumors.
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Lenalidomide-d5
0 ImagesSynonyms: CC-5013-d5Lenalidomide-d5 (CC-5013-d5) is the d5-labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
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MGD-4
0 ImagesCat. No.: HY-168614CAS No.: 2991817-99-1MGD-4 is an orally active cereblon-dependent molecular glue degrader with a phthalazinone scaffold. MGD-4 degrades the Ikaros family proteins IKZF1, IKZF2 and IKZF3 in a dose-dependent manner, with DC50 values of 67.2 nM, 918.2 nM and 95.8 nM, respectively. MGD-4 exhibits weak degradation activity against CK1α. MGD-4 inhibits the viability of multiple myeloma (MM) and acute myeloid leukemia (AML) cells and induces cell apoptosis. MGD-4 is used for the research of multiple myeloma, acute myeloid leukemia, diffuse large B-cell lymphoma and related hematological malignancies .
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BMS-986482 acetate
0 ImagesCat. No.: HY-182467APurity: 98.04%BMS-986482 acetate is a CRBN-mediated IKZF1-4 (Ikaros family zinc finger 1-4) molecular glue degrader. BMS-986482 acetate's activity is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 acetate can be used for the research of advanced solid tumors.
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GATA4-NKX2-5-IN-1
0 ImagesGATA4-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.
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USP3 ZnF-UBD ligand-1
0 ImagesUSP3 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.
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Lenalidomide hydrochloride
0 ImagesCat. No.: HY-A0003ACAS No.: 1243329-97-6Synonyms: CC-5013 hydrochlorideLenalidomide hydrochloride (CC-5013 hydrochloride) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide hydrochloride induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide hydrochloride promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide hydrochloride can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
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NVP-KFA115
0 ImagesCat. No.: HY-189390CAS No.: 2408998-17-2
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PROTAC BCL6/IKZF1/3 Degrader-1
0 ImagesCat. No.: HY-179075PROTAC BCL6/IKZF1/3 Degrader-1 is an orally active bifunctional PROTAC‑IMiD protein degrader that targets and degrades BCL6, IKZF1 and IKZF3. PROTAC BCL6/IKZF1/3 Degrader-1 induces ubiquitination and proteasome-mediated degradation of target proteins by recruiting E3 ubiquitin ligase, and triggers cell cycle arrest and apoptosis. PROTAC BCL6/IKZF1/3 Degrader-1 exhibits favorable anti-tumor activity in diffuse large B-cell lymphoma xenograft models. PROTAC BCL6/IKZF1/3 Degrader-1 can be used for the research of diffuse large B-cell lymphoma.
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IKZF2-degrader 3
0 ImagesCat. No.: HY-177754CAS No.: 2983841-46-7IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM.
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IKZF-IN-1
0 ImagesCat. No.: HY-170518IKZF-IN-1 is a molecular glue and an IKZF protein degrader that mediates the degradation of IKZF1/IKZF2/IKZF3/IKZF4 proteins. IKZF-IN-1 promotes the ubiquitination of target proteins via the CUL4‑CRBN E3 ubiquitin ligase complex, thereby triggering the degradation of target proteins. IKZF-IN-1 can be used in cancer-related research.
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PROTAC BRD9 Degrader-12
0 ImagesCat. No.: HY-189226PROTAC BRD9 Degrader-12 is a BRD9 PROTAC degrader, with DC50 values of 57 pM and 62 pM against BRD9 and IKZF1, respectively. PROTAC BRD9 Degrader-12 promotes CRL-CRBN-dependent ubiquitination and proteasome-mediated BRD9 degradation by simultaneously binding to BRD9 and CRBN, and concurrently recruits IKZF1 as a neosubstrate via CRBN to induce its degradation. PROTAC BRD9 Degrader-12 selectively degrades BRD9 and IKZF1. The synergistic degradation of BRD9/IKZF1 downregulates MYC-related signaling, induces apoptosis and S-phase cell cycle arrest, and thereby inhibits the proliferation of hematological malignant cells. PROTAC BRD9 Degrader-12 is used for research related to hematological malignancies.
