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Heptamidine (Synonyms: SBi4211)

Cat. No.: HY-16918
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Heptamidine (SBi4211) 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. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).

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Heptamidine Chemical Structure

Heptamidine Chemical Structure

CAS No. : 94345-47-8

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Description

Heptamidine (SBi4211) 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].

IC50 & Target

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

In Vitro

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].

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.
Molecular Weight

368.47

Formula

C₂₁H₂₈N₄O₂

CAS No.

94345-47-8

SMILES

N=C(C1=CC=C(OCCCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

HeptamidineSBi4211SBi 4211SBi-4211OthersS100BmelanomacancerMyotonicdystrophyHeLacellDMCalcium-BindingInhibitorinhibitorinhibit

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Heptamidine
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