Drug intelligence / Profile preview

UnAcH416

Development stage
Preclinical
Modality
Modified Peptides → Peptides
01

Overview

**UnAcH416 (P2)** is an unacetylated peptoid-based inhibitor derived from the histone H4 N-terminal tail (H4-16), featuring a chloracetamidine warhead at the Arg3 position to enable selective, irreversible inhibition of **protein arginine methyltransferase 1 (PRMT1)** over PRMT5, with an IC50 in the low micromolar range (8.73 μM). Developed as a research compound, it demonstrates superior potency and stability compared to peptide analogs, significantly reducing cell viability, proliferation, and colony formation in **MDA-MB-468 breast carcinoma** and **HCT116 colon carcinoma** cell lines (e.g., 75% viability reduction at 20 μM in MDA468), while sparing normal cells; it induces both **apoptosis** and **autophagy**, positioning it as a potentially less toxic cytostatic anticancer agent.[1][4]

02

Targets

PRMT1 (Protein Arginine Methyltransferase 1)

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