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).
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- No. CAS: 94345-47-8
- Fòrmula: C21H28N4O2
- Peso molecular:368.47
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Almacenamiento:
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Actividad biológica
Kd: 6.9 μM (calcium-binding protein S100B)[1]
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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] |
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.
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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No. CAS 94345-47-8
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Peso molecular 368.47
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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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