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Heptamidine (SBi4211) 是一種強效的 Pentamidine-related 鈣結(jié)合蛋白 S100B 的抑制劑 (Kd=6.9 μM),選擇性地殺死表達(dá) S100B 的黑素瘤細(xì)胞。Heptamidine 是研究強直性肌營養(yǎng)不良 (DM) 的有效工具。

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Heptamidine Chemical Structure

Heptamidine Chemical Structure

CAS No. : 94345-47-8

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Heptamidine 的其他形式現(xiàn)貨產(chǎn)品:

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生物活性

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]

細(xì)胞效力
(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]
體外研究
(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].

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

體內(nèi)研究
(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].

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.
分子量

368.47

Formula

C21H28N4O2

CAS 號
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

純度 & 產(chǎn)品資料
參考文獻(xiàn)
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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.

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產(chǎn)品名稱:
Heptamidine
目錄號:
HY-16918
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