I-138

Names

[ CAS No. ]:
2098211-50-6

[ Name ]:
I-138

Biological Activity

[Description]:

I-138 is an orally active compound structurally related to ML323 (HY-17543). I-138 and ML-323 are potent reversible inhibitors of USP1-UAF1. I-138 displays synergistic binding with ubiquitin and mutual exclusive binding with ML323. I-138 induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells. I-138 ablates USP1 autocleavage in cells[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Deubiquitinase

[References]

[1]. Simoneau A, et al. Ubiquitinated PCNA Drives USP1 Synthetic Lethality in Cancer. Mol Cancer Ther. 2023 Feb 1;22(2):215-226.  

Chemical & Physical Properties

[ Molecular Formula ]:
C26H23F3N6O

[ Molecular Weight ]:
492.50