2982574-79-6
Chemical Structure
HBI-2375
Synonym(s): HYBI-084
- CAS 番号: 2982574-79-6
- Formula:C29H36ClF2N9O2
- Molecular Weight:616.11
IUPAC Name: 5-amino-2-chloro-4-fluoro-N-(4-fluoro-5-(4-(4-methylpiperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)-2-((3R,5S)-3,4,5-trimethylpiperazin-1-yl)phenyl)-3-methylbenzamide
InChIKey: ZAAAXOTWIKLEGP-CALCHBBNSA-N
SMILES: ClC1=C(C)C(F)=C(N)C=C1C(NC(C=C(N2C=C(C(N3CCN(C)CC3)=O)N=N2)C(F)=C4)=C4N5C[C@@H](C)N(C)[C@@H](C)C5)=O
Biological Activity: HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8+ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM[1][2].
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HBI-2375 | 98.06% | HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8+ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM. | ||||||||||||||||||||
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- [1]. Coker JA, et al. Development and characterization of triazole-based WDR5 inhibitors for the treatment of glioblastoma. JCI Insight. Published online May 5, 2026. [Content Brief]
- [2]. Shojaei F, et al. HBI-2375, a first-in-class IND ready selective MLL1-WDR5 inhibitor, retains desirable preclinical characteristics in solid tumors and in leukemias to be pursued in clinical studies[J]. Cancer Research, 2024, 84(6_Supplement): 2640-2640.
Keywords
