Drug intelligence / Profile preview

SL-IST-001

Development stage
Preclinical
Lead developer
Isosterix
Modality
Small Molecules
Administration
Oral
01

Overview

SL-IST-001 is an orally bioavailable small molecule inhibitor of the epigenetic regulatory histone acetyltransferase KAT6A (lysine acetyltransferase 6A), developed by Isosterix. It selectively binds to the active site of KAT6A within the acetyl-CoA substrate binding pocket, inhibiting histone H3 lysine 23 (H3K23) acetylation. In preclinical studies, SL-IST-001 demonstrated single-digit nanomolar biochemical potency, reduced cell viability in breast cancer cell lines, and showed anti-tumor efficacy in ZR-75-1 mouse xenograft models. It is being developed for the treatment of estrogen receptor-positive (ER+) breast cancer and other solid tumors.

02

Targets

KAT6A (Lysine acetyltransferase 6A)KAT6B (Histone acetyltransferase KAT6B)

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