2892065-45-9
Chemical Structure
PLX-4545
- CAS No.: 2892065-45-9
- Formula:C28H31N3O4
- Molecular Weight:473.56
InChIKey: DQYZQRGRHXEYPT-SDHOMARFSA-N
SMILES: O=C1CC[C@@H](C(N1)=O)N2CC3=C(C2=O)C=CC(O[C@H]4CCCC[C@@H]4N5CC(C5)C6=CC=CC=C6)=C3
Biological Activity: 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[1][3].
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PLX-4545 | 96.76% | 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. | ||||||||||||||||||||
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- [1]. Huang Y, et al. PLX-4545, a selective IKZF2 degrader, reprograms suppressive Tregs leading to tumor growth inhibition and combination benefit with immune checkpoint therapy[J]. Cancer Research, 2025, 85(8_Supplement_1): 6380-6380.
- [3]. Zhang X, et al. Discovery of a Novel Series of iso-Indolinone-Based Glutarimides as Highly Efficacious and Selective IKZF2 Molecular Glue Degraders. J Med Chem. 2025 Sep 11;68(17):18230-18257. [Content Brief]
Keywords
