BT5 is a selective small-molecule inhibitor of NSD1 (nuclear receptor binding SET domain protein 1), a histone methyltransferase implicated in oncogenesis through H3K36 methylation. According to available data, BT5 binds directly to the SET domain of NSD1 with a K<sub>D</sub> of 44 nM as measured by surface plasmon resonance (SPR) and exhibits potent enzymatic inhibition with an IC<sub>50</sub> of 67 nM in biochemical methyltransferase assays. In cellular assays, BT5 effectively reduces H3K36me2 levels in NSD1-dependent cell lines with EC<sub>50</sub> values around 300–500 nM, demonstrating selective target engagement. Notably, BT5 shows antiproliferative activity in NSD1-mutant cancer cell models, such as certain head and neck squamous cell carcinoma (HNSCC) lines, with GI<sub>50</sub> values in the low micromolar range. These data support BT5 as a promising tool compound for probing NSD1 biology and validating its therapeutic potential in epigenetic-driven cancers.
MedKoo Cat#: 124068
Name: NSD1 inhibitor BT5
CAS#: 2351225-46-0
Chemical Formula: C10H11N3OS
Exact Mass: 221.0623
Molecular Weight: 221.28
Elemental Analysis: C, 54.28; H, 5.01; N, 18.99; O, 7.23; S, 14.49
The following data is based on the product molecular weight 221.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |