Heptamidine
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).
For research use only. We do not sell to patients.
- CAS No.: 94345-47-8
- Formula: C21H28N4O2
- Molecular Weight:368.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
Kd: 6.9 μM (calcium-binding protein S100B)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Malme-3M | IC50 |
4.2 μM
Compound: SBi4211
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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
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[PMID: 23264854] |
| Malme-3M | IC50 |
6.8 μM
Compound: SBi4211
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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
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[PMID: 23264854] |
| WM-115 | EC50 |
11.5 μM
Compound: 4a
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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
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[PMID: 26727270] |
| WM-115 | EC50 |
25.6 μM
Compound: 4a
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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
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[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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Homozygous HSALR transgenic mice in line 20b (FVB inbred background) with a Myotonic dystrophy (DM) mouse model[2]
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Dosage:20 or 30 mg/kg
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Administration:Intraperitoneal injection; 7 days; once daily
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Result:Reversed splicing defects and rescues myotonia in a DM mouse model.
Chemical Information
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CAS No. 94345-47-8
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Molecular Weight 368.47
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Formula C21H28N4O2
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SMILES
N=C(C1=CC=C(OCCCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N
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Synonyms
SBi4211
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Heptamidine Related Classifications
HY-16918 Related Classifications
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