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].

References:

[1]. Ichiyama K, et al. Transcription factor Ikzf1 associates with Foxp3 to repress gene expression in Treg cells and limit autoimmunity and anti-tumor immunity. Immunity. 2024 Sep 10;57(9):2043-2060.e10. [Content Brief]

IKZF Family Isoform Specific Products:

IKZF Family Isoform Comparison

IKZF Family Related Products (48)
IKZF Family Isoform Comparison

By Effects:	Inhibitors (9) Agonist (1) Degraders (33) Ligand (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-144998

NVP-DKY709	Inhibitor	99.66%
NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the D_max 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.

HY-122542B

PPACK TFA	Degrader	99.80%
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 (T_reg) into effector-like T cells, enhances CD8⁺ T cell responses, and modulates the T_eff:T_reg balance. PPACK TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of T_reg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.

HY-144841

Cemsidomide	Degrader	99.54%
Cemsidomide (CFT7455) is a ubiquitin ligase pathway based IKZF1/3 (Ikaros/Aiolos) degrader with molecular glue activity. Cemsidomide has a GI₅₀ of 0.05 nM for NCIH929.1 cells. Cemsidomide is used in the research of multiple myeloma (MM).

HY-157334

DEG-77	Degrader	99.03%
DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC₅₀ values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.

HY-145776

ALV1	Inhibitor	98.62%
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.

HY-W1135319

SB-405483		99.33%
SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.

HY-182467

BMS-986482	Degrader
BMS-986482 is a CELMoD, CRBN-mediated, selective IKZF1-4 Molecular Glue degrader. The activity of BMS-986482 is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 inhibits tumor growth in preclinical mouse models. BMS-986482 can be used for the research of advanced solid tumors. .

HY-181957

KB528	Inhibitor
KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC₅₀ values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma.

HY-159647

PLX-4545	Degrader
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 (T_reg) into effector-like T cells, enhances CD8⁺ T cell responses, and modulates the T_eff:T_reg balance. PLX-4545 also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of T_reg. PLX-4545 can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.

HY-122542A

PPACK dihydrochloride	Degrader	99.07%
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 (T_reg) into effector-like T cells, enhances CD8⁺ T cell responses, and modulates the T_eff:T_reg balance. PPACK dihydrochloride also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of T_reg. PPACK dihydrochloride can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.

HY-159647A

(S,S)-PLX-4545	Degrader
(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.

HY-172931

DEG-35	Degrader	98.88%
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).

HY-161101

MG degrader 1		99.83%
MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC₅₀ value of 1.385 nM in MM.1S cells.

HY-173630A

(Rac)-BMS-986449	Inhibitor	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.

HY-173630

BMS-986449	Inhibitor
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.

HY-168615

MGD-28	Degrader	99.73%
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.

HY-172930

PVTX-405	Degrader
PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC₅₀ of 0.7 nM and a D_max 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.

HY-155539

Cisd2 agonist 2	Agonist	99.17%
Cisd2 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.

HY-159647B

(1S,2S,3R)-PLX-4545	Degrader
(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.

HY-Y1863

3-Chlorobenzaldehyde	Degrader	99.58%
3-Chlorobenzaldehyde (m-Chlorobenzenecarboxaldehyde) is a kind of biological materials or organic compounds that are widely used in life science research.

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IKZF Family

IKZF Family Isoform Specific Products:

IKZF Family Isoform Specific Products:

IKZF Family Related Products (48)

IKZF Family Isoform Comparison

IKZF Family Related Products (48):