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KTX-1031
- Development stage
- Preclinical
- Lead developer
- K36 Therapeutics
- Modality
- Small Molecules
01
Overview
**KTX-1031** is a small molecule catalytic inhibitor of NSD2 (also known as MMSET or WHSC1), a histone methyltransferase that deposits the H3K36me2 mark. It suppresses t(4;14) gene expression and reverses chromatin changes in multiple myeloma (MM) cell lines harboring the t(4;14) translocation, such as H929, KMS11, KMS18, KMS26, LP1, and XG-7, leading to reduced H3K36me2, increased H3K27me3, and modulation of gene expression (downregulation of 539 genes and upregulation of 133 genes in KMS11 cells). Developed by K36 Therapeutics, it is a preclinical analog related to KTX-1001, the first-in-class NSD2 inhibitor advanced to phase 1 trials for relapsed/refractory MM.
02
Targets
NSD2 (Histone-lysine N-methyltransferase NSD2)
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