Drug intelligence / Profile preview

KTX-1030

Development stage
Discontinued
Lead developer
K36 Therapeutics
Modality
Small Molecules
01

Overview

KTX-1030 is a small molecule that serves as the substantially inactive enantiomer of KTX-1031, a catalytic inhibitor of Nuclear receptor binding SET domain protein 2 (NSD2). Developed by K36 Therapeutics, KTX-1030 is primarily utilized in preclinical research as a negative control to validate the specificity of NSD2 inhibition in models of multiple myeloma, particularly those harboring the t(4;14) translocation. While its active counterpart KTX-1031 is designed to deplete H3K36me2 levels and suppress oncogenic gene expression programs, KTX-1030 lacks significant inhibitory activity against the NSD2 enzyme, allowing researchers to distinguish between target-specific effects and non-specific chemical toxicity in cell-based assays.

02

Targets

NSD2 (Histone-lysine N-methyltransferase NSD2)

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