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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 94345-47-8
- 分子式: C21H28N4O2
- 分子量:368.47
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
Kd: 6.9 μM (calcium-binding protein S100B)[1]
|
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] |
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.
-
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.
化学情報
-
CAS 番号 94345-47-8
-
分子量 368.47
-
分子式 C21H28N4O2
-
SMILES
N=C(C1=CC=C(OCCCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N
-
別名
SBi4211
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Heptamidine 関連分類
HY-16918 関連分類
Powered by Bioz