BI-9321
CAS No. : 2387510-86-1
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| Cat. No. : | HY-114208 |
| M.Wt: | 360.43 |
| Formula: | C22H21FN4 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1]. IC50 & Target: Kd: 166 nM (NSD3-PWWP1)[1] In Vitro: BI-9321 is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1?μM. As a single agent, BI-9321 downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].
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