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Heptamidine dimethanesulfonate

Catalog No. T11553   CAS 161374-55-6
Synonyms: SBi4211 dimethanesulfonate

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).

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Heptamidine dimethanesulfonate Chemical Structure
Heptamidine dimethanesulfonate, CAS 161374-55-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 87.00
5 mg In stock $ 213.00
10 mg In stock $ 347.00
25 mg In stock $ 589.00
50 mg In stock $ 842.00
100 mg In stock $ 1,160.00
500 mg In stock $ 2,330.00
1 mL * 10 mM (in DMSO) In stock $ 238.00
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Purity: 98.24%
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
Targets&IC50 S100B:(kd)6.9 μM
In vitro Heptamidine rescues the mis-splicing of minigene reporters in a HeLa cell DM1 model (EC50: 15 μM). Heptamidine (20 μM) does not decrease CUG levels significantly when compares to Propamidine and Pentamidine, and exhibits cytotoxic at concentrations above 17.5 μM in HeLa cells expressing 960 CUG repeats [2].
In vivo Heptamidine (i.p.; 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].
Synonyms SBi4211 dimethanesulfonate
Molecular Weight 560.68
Formula C23H36N4O8S2
CAS No. 161374-55-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (111.47 mM), Sonification is recommended.

TargetMolReferences and Literature

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.

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Keywords

Heptamidine dimethanesulfonate 161374-55-6 Others Heptamidine dystrophy SBi 4211 Myotonic SBi4211 inhibit Calcium-Binding cancer melanoma SBi-4211 S100B HeLa Inhibitor cell SBi4211 dimethanesulfonate inhibitor

 

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