| Description | Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) serves as a potent inhibitor related to Pentamidine, targeting the calcium-binding protein S100B with a dissociation constant (Kd) of 6.9 µM. It demonstrates specificity by preferentially killing melanoma cells overexpressing S100B compared to cells lacking this protein. Additionally, Heptamidine is employed as a valuable research tool in the study of Myotonic dystrophy (DM). |
| In vitro | Heptamidine在HeLa细胞DM1模型中纠正minigene报告基因片段剪接错误（EC50：15 μM）。与Propamidine和Pentamidine相比，Heptamidine（20 μM）并未显著降低CUG水平，且在表达960个CUG重复序列的HeLa细胞中，浓度超过17.5 μM时表现出细胞毒性[2]。 |
| In vivo | Heptamidine（i.p.；20或30 mg/kg；7天）在HSALR小鼠中引起剂量依赖性的exon 7a含量减少，20 mg/kg剂量时回复至野生型水平（6±1%），同时肌阵挛从3级（频繁的肌阵挛放电）降低至1级（偶尔的肌阵挛放电）[2]。 |
| Target activity | S100B:(kd)6.9 μM |
| Synonyms | SBi4211 dimethanesulfonate |
| molecular weight | 560.68 |
| Molecular formula | C23H36N4O8S2 |
| CAS | 161374-55-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 70 mg/mL (124.85 mM), Sonication is recommended. |
| References | 1. McKnight LE, et al. Structure-Based Discovery of a Novel Pentamidine-Related Inhibitor of the Calcium-Binding Protein S100B. ACS Med Chem Lett. 2012 Dec 13;3(12):975-979. Epub 2012 Sep 25. 2. Coonrod LA, et al. Reducing levels of toxic RNA with small molecules.ACS Chem Biol. 2013 Nov 15;8(11):2528-37. |
Heptamidine dimethanesulfonate
CAS No.: 161374-55-6
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) serves as a potent inhibitor related to Pentamidine, targeti
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