Heptamidine (Synonyms: SBi4211)

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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. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).

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Heptamidine Chemical Structure

CAS No. : 94345-47-8

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Other Forms of Heptamidine:

Heptamidine dimethanesulfonate Get quote

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Description

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].

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
Malme-3M	IC₅₀	4.2 μM Compound: SBi4211	Growth inhibition of human MALME-3M cells overexpressing calcium-binding protein S100B after 4 days by SYBR green assay Growth inhibition of human MALME-3M cells overexpressing calcium-binding protein S100B after 4 days by SYBR green assay	[PMID: 23264854]
Malme-3M	IC₅₀	6.8 μM Compound: SBi4211	Growth inhibition of human MALME-3M cells transfected with S100B siRNA after 4 days by SYBR green assay Growth inhibition of human MALME-3M cells transfected with S100B siRNA after 4 days by SYBR green assay	[PMID: 23264854]
WM-115	EC₅₀	11.5 μM Compound: 4a	Growth inhibition of human WM115 cells expressing high levels of S100-B by SYBR Green based fluorescence method Growth inhibition of human WM115 cells expressing high levels of S100-B by SYBR Green based fluorescence method	[PMID: 26727270]
WM-115	EC₅₀	25.6 μM Compound: 4a	Growth inhibition of human WM115 cells expressing low levels of S100-B by SYBR Green based fluorescence method Growth inhibition of human WM115 cells expressing low levels of S100-B by SYBR Green based fluorescence method	[PMID: 26727270]

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].

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

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].

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

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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. [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]

Heptamidine Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Heptamidine94345-47-8SBi4211SBi 4211SBi-4211OthersS100BmelanomacancerMyotonicdystrophyHeLacellDMCalcium-BindingInhibitorinhibitorinhibit

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