HBI-2375

HBI-2375 (HYBI-084) is a selective, brain-penetrant and orally active MLL1-WDR5 interaction inhibitor. HBI-2375 inhibits WDR5 with an IC50 of 4.48 nM. HBI-2375 shows inhibition of proliferation in MV4;11 leukemia cells (IC50: 3.17 µM) . HBI-2375 is capable of targeted disruption of histone methyltransferase activity in cancer cells. HBI-2375 can be used for the study of leukemia, glioma and glioblastoma[1][2].

Product Specifications

CAS Number

[2982574-79-6]

Product Name Alternative

HYBI-084

UNSPSC

12352005

Target

Histone Methyltransferase; WDR5

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

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

Molecular Formula

C29H36ClF2N9O2

Molecular Weight

616.11

References & Citations

[1]Farbod Shojaei, et al. Abstract 2640: 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 Free. Cancer Res (2024) 84 (6_Supplement) : 2640.|[2]Coker JA, et al. WD repeat domain 5 (WDR5) inhibitors: a patent review (2016-present) . Expert Opin Ther Pat. 2025 Jan;35 (1) :31-45.