BI-9321 trihydrochloride
目录号: PL15057 纯度: ≥98%
CAS No. :2387510-87-2
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中文名称
BI-9321 trihydrochloride
英文名称
BI-9321 trihydrochloride
英文别名
BI-9321 trihydrochloride;BI 9321;(4-(5-(7-Fluoroquinolin-4-yl)-1-methyl-1H-imidazol-4-yl)-3,5-dimethylphenyl)methanamine trihydrochloride;[4-[5-(7-fluoroquinolin-4-yl)-1-methylimidazol-4-yl]-3,5-dimethylphenyl]methanamine;trihydrochloride;BI-9321 (trihydrochloride)
Cas No.
2387510-87-2
分子式
C22H24Cl3FN4
分子量
469.81
包装储存
4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
产品详情
BI-9321 trihydrochloride 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 trihydrochloride 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。
生物活性
BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a K d value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC 50 of 1.2 μM in U2OS cells.
性状
Solid
IC50 & Target[1][2]
Kd: 166 nM (NSD3-PWWP1)
体外研究(In Vitro)
BI-9321 trihydrochloride 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 trihydrochloride downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
参考文献
[1]. B?ttcher 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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (532.13 mM; Need ultrasonic)H2O : 25 mg/mL (53.21 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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