| Identification | Back Directory | [Name]
SBi4211 dimethanesulfonate | [CAS]
161374-55-6 | [Synonyms]
SBi4211 dimethanesulfonate
Heptamidine dimethanesulfote
Heptamidine dimethanesulfonate | [Molecular Formula]
C22H32N4O5S | [MOL File]
161374-55-6.mol | [Molecular Weight]
464.58 |
| Hazard Information | Back Directory | [Uses]
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2]. | [in vivo]
Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) causes a dose-dependent reduction of exon 7a inclusion in?HSALR?mice, returning to wild type levels (6±1%) when at 20 mg/kg dose, the myotonia is reduced from grade 3 to grade 1 (occasional myotonic discharge) or grade 0 at both 20 or 30 mg/kg[2]. | Animal Model: | Homozygous?HSALR?transgenic mice in line 20b (FVB inbred background)?with a Myotonic dystrophy (DM) mouse model[2] | | Dosage: | 20 or 30 mg/kg | | Administration: | Intraperitoneal injection; 7 days; once daily | | Result: | Reversed splicing defects and rescues myotonia in a DM mouse model.
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| [storage]
Store at -20°C | [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. DOI:10.1021/ml300166s
[2] Coonrod LA, et al. Reducing levels of toxic RNA with small molecules.ACS Chem Biol.?2013 Nov 15;8(11):2528-37. DOI:10.1021/cb400431f |
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