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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
21 Results for "
IKZF2 degrader
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "IKZF2 degrader" in MCE Product Catalog:
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1 Cited Publications
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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 .
Cat. No.: HY-173630
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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 .
Cat. No.: HY-172931
CAS No.: 2734910-37-1
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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) .
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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 .
Cat. No.: HY-159647A
CAS No.: 2892065-49-3
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(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 .
Cat. No.: HY-159647
CAS No.: 2892065-45-9
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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 .
Cat. No.: HY-173630A
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(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 .
Cat. No.: HY-159647B
CAS No.: 2892066-42-9
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(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 .
Cat. No.: HY-172930
CAS No.: 2991021-08-8
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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 .
Cat. No.: HY-168615
CAS No.: 2991818-13-2
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MGD-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 .
Cat. No.: HY-172882
CAS No.: 2983840-43-1
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IKZF2-degrader 1 is a potent and selective molecular glue degrader that selectively degrades IKZF2, with DC50 values of 0.6 nM and 2.0 nM in HEK293T cells and Jurkat cells, respectively. IKZF2-degrader 1 exerts no degrading effect on CK1α, IKZF1 and GSPT1, and shows weak activity against IKZF3. IKZF2-degrader 1 can be used in studies related to IKZF2-dependent cancers .
Cat. No.: HY-177754
CAS No.: 2983841-46-7
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IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM .
Cat. No.: HY-W1128213
CAS No.: 2983841-00-3
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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 .
Cat. No.: HY-182945
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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 .
Cat. No.: HY-185300
CAS No.: 2989880-79-5
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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 .
Cat. No.: HY-168614
CAS No.: 2991817-99-1
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MGD-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 .
Cat. No.: HY-170518
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IKZF-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 .
Cat. No.: HY-182799
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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 .
Cat. No.: HY-172930B
CAS No.: 2991023-13-1
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(R)-PVTX-405 is a IKZF2 molecular glue degrader with a DC50 of 4.1 nM. (R)-PVTX-405 is the (R)-enantiomer of PVTX-405 (HY-172930). PVTX-405 is an orally active IKZF2 molecular glue degrader that significantly inhibits MC38 tumor growth in mouse tumor xenograft models. (R)-PVTX-405 can be used in cancer-related research .
Cat. No.: HY-189390
CAS No.: 2408998-17-2
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NVP-KFA115 is an IKZF2 and IKZF4 molecular glue degrader that mediates degradation via CRBN. NVP-KFA115 exhibits an improved cardiac profile. NVP-KFA115 can be used for the study of advanced cancers .
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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
