BI-9321

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-9321 

BI-9321 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。

BI-9321

BI-9321 Chemical Structure

CAS No. : 2387510-86-1

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BI-9321 的其他形式现货产品:

BI-9321 trihydrochloride

生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

360.43

Formula

C22H21FN4
CAS 号

2387510-86-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

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