Heptamidine  (Synonyms: SBi4211)

Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (K_d=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].

Kd: 6.9 μM (calcium-binding protein S100B)^[1]

Heptamidine is a Pentamidine-S100B complex, two molecules of pentamidine bind per monomer of S100B, which performs to be an inhibitor for S100B^[1].
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].
Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model with an EC₅₀ value of 15 μM^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

368.47

C₂₁H₂₈N₄O₂

94345-47-8

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [2]. Coonrod LA, et al. Reducing levels of toxic RNA with small molecules.ACS Chem Biol. 2013 Nov 15;8(11):2528-37.  [Content Brief]