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  2. Metabolic Enzyme/Protease Anti-infection
  3. Aminopeptidase Bacterial Antibiotic
  4. Bestatin

Bestatin  (Synonyms: 烏苯美司; Ubenimex)

目錄號(hào): HY-B0134 純度: 99.96%
COA 產(chǎn)品使用指南 技術(shù)支持

Bestatin (Ubenimex) 是 CD13 (Aminopeptidase N)/APN 和 leukotriene A4 hydrolase 抑制劑，常用于癌癥研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Bestatin Chemical Structure

Bestatin Chemical Structure

CAS No. : 58970-76-6

1.  客戶無(wú)需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥794
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1 mg ￥225
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5 mg ￥451
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10 mg ￥722
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50 mg ￥2063
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100 mg ￥3537
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Customer Review

Other Forms of Bestatin:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects[1][2].

IC50 & Target[1][2][3][4]

CD13

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 30737134]
A549 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 29859750]
A549 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 29202398]
A549 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 27670098]
A549 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 27322756]
A549 IC50
15.93 μM
Compound: 1
Antiproliferative activity against human A549 cells in presence of 5-FU after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells in presence of 5-FU after 48 hrs by MTT assay
[PMID: 29202398]
A549 IC50
512.9 μM
Compound: Bestatin
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 22901392]
AGS IC50
> 200 μM
Compound: Bestatin
Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34917257]
B16-BL6 GI50
> 500 μM
Compound: Bestatin
Cytotoxicity against mouse B16-BL6 cells assessed as cell growth inhibition after 24 hrs by MTT assay
Cytotoxicity against mouse B16-BL6 cells assessed as cell growth inhibition after 24 hrs by MTT assay
[PMID: 24900417]
ES-2 IC50
> 500 μM
Compound: Bestatin
Cytotoxicity against human ES2 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human ES2 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32791404]
HCT-116 IC50
> 1000 μM
Compound: Bestatin
Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 22901392]
HCT-116 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 29859750]
HCT-116 IC50
315.25 μM
Compound: 1; Ube
Antiproliferative activity against human HCT-116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells after 48 hrs by MTT assay
[PMID: 27322756]
HCT-116 IC50
357.61 μM
Compound: 1
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 29202398]
HCT-116 IC50
42.54 μM
Compound: Bestatin
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by WST1 assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by WST1 assay
[PMID: 28065501]
HCT-116 IC50
44.06 μM
Compound: 1
Antiproliferative activity against human HCT116 cells in presence of 5-FU after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells in presence of 5-FU after 48 hrs by MTT assay
[PMID: 29202398]
HEL IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human HEL cells after 48 hrs by MTT assay
Antiproliferative activity against human HEL cells after 48 hrs by MTT assay
[PMID: 27670098]
HEL IC50
416.65 μM
Compound: 1; Ube
Antiproliferative activity against human HEL cells after 48 hrs by MTT assay
Antiproliferative activity against human HEL cells after 48 hrs by MTT assay
[PMID: 27322756]
HeLa IC50
> 100 μM
Compound: Bestatin
Inhibition of HDAC1/HDAC2 in human HeLa cells nuclear extract preincubated for 5 mins before Boc-Lys (acetyl)-AMC substrate addition for 30 mins by microplate reader analysis
Inhibition of HDAC1/HDAC2 in human HeLa cells nuclear extract preincubated for 5 mins before Boc-Lys (acetyl)-AMC substrate addition for 30 mins by microplate reader analysis
[PMID: 26629857]
HeLa IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 27670098]
HeLa IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 27322756]
HeLa IC50
154.9 μM
Compound: Bestatin
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
[PMID: 22901392]
HepG2 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 29202398]
HepG2 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 27322756]
HepG2 IC50
> 500 μM
Compound: Bestatin
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32791404]
HepG2 IC50
14.52 μM
Compound: 1
Antiproliferative activity against human HepG2 cells in presence of 5-FU after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells in presence of 5-FU after 48 hrs by MTT assay
[PMID: 29202398]
HL-60 EC50
> 100 μM
Compound: 2
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
[PMID: 28803047]
HL-60 IC50
0.92 mM
Compound: bestatin
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
[PMID: 19782572]
HL-60 IC50
0.92 mM
Compound: Bestatin
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 19299146]
HL-60 IC50
1.13 mM
Compound: Bestatin
Cytotoxicity against human HL60 cells expressing aminopeptidase N after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells expressing aminopeptidase N after 72 hrs by MTT assay
[PMID: 20637634]
HL-60 IC50
1.34 mM
Compound: Bestatin
Antiproliferative activity against human HL60 cells expressing high levels of APN after 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells expressing high levels of APN after 48 hrs by MTT assay
[PMID: 21802307]
HL-60 IC50
1.65 mM
Compound: bestatin
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
[PMID: 19423354]
HL-60 IC50
1.65 mM
Compound: Bestatin
Antiproliferative activity against human HL-60 cells after 48 hrs by MTT assay
Antiproliferative activity against human HL-60 cells after 48 hrs by MTT assay
[PMID: 18996018]
HL-60 IC50
22.89 μM
Compound: Bestatin
Inhibition of APN in human HL60 cells assessed as hydrolysis of L-Leu-p-nitroanilide by spectrophotometry
Inhibition of APN in human HL60 cells assessed as hydrolysis of L-Leu-p-nitroanilide by spectrophotometry
[PMID: 21802307]
HL-60 IC50
245 μM
Compound: Bestatin
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
[PMID: 22206607]
HL-60 IC50
245 μM
Compound: Bestatin
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 19683842]
HL-60 IC50
86.4 μM
Compound: Bestatin
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 22901392]
HUVEC IC50
> 2000 μM
Compound: 1
Antiproliferative activity against HUVEC after 48 hrs by MTT assay
Antiproliferative activity against HUVEC after 48 hrs by MTT assay
[PMID: 30737134]
K562 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
[PMID: 30737134]
K562 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
[PMID: 29859750]
K562 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
[PMID: 27670098]
K562 IC50
> 500 μM
Compound: Bestatin
Cytotoxicity against human K562 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human K562 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32791404]
K562 IC50
135.6 μM
Compound: Bestatin
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
[PMID: 22901392]
KG-1 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay
Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay
[PMID: 27670098]
KG-1 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay
Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay
[PMID: 27322756]
MCF7 IC50
> 1000 μM
Compound: Bestatin
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 22901392]
MCF7 IC50
> 200 μM
Compound: Bestatin
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34917257]
MCF7 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 27322756]
MCF7 IC50
149.6 μM
Compound: Bestatin
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
[PMID: 27624521]
MCF7 IC50
541 μM
Compound: Bestatin
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by resazurin dye-based fluorimetric analysis
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by resazurin dye-based fluorimetric analysis
[PMID: 27253989]
MDA-MB-231 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 29859750]
MDA-MB-231 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 27670098]
MDA-MB-231 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 27322756]
MDA-MB-231 IC50
5.08 mM
Compound: Bestatin
Antiproliferative activity against human MDA-MB-231 cells expressing low levels of APN after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells expressing low levels of APN after 48 hrs by MTT assay
[PMID: 21802307]
MDA-MB-231 IC50
50.6 μM
Compound: Bestatin
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 23510562]
MDA-MB-231 IC50
50.6 μM
Compound: Bestatin
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 22901392]
MDA-MB-231 IC50
753.18 μM
Compound: Bestatin
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 21911297]
MDA-MB-231 IC50
8.59 mM
Compound: Bestatin
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 20637634]
MOLT-4 EC50
> 100 μM
Compound: 2
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay
[PMID: 28803047]
NB-4 IC50
220.9 μM
Compound: Bestatin
Cytotoxicity against human NB4 cells after 48 hrs by MTT assay
Cytotoxicity against human NB4 cells after 48 hrs by MTT assay
[PMID: 22901392]
NCI-H1975 IC50
> 200 μM
Compound: Bestatin
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34917257]
NIH3T3 IC50
> 1000 μM
Compound: Bestatin
Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay
[PMID: 22901392]
PC-3 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
[PMID: 30737134]
PC-3 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
[PMID: 29859750]
PC-3 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay
[PMID: 27670098]
PC-3 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay
[PMID: 27322756]
PC-3 IC50
> 500 μM
Compound: Bestatin
Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32791404]
PC-3 IC50
399.4 μM
Compound: Bestatin
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
[PMID: 22901392]
PLC IC50
> 500 μM
Compound: 1
Antiproliferative activity against human PLC cells after 48 hrs by MTT assay
Antiproliferative activity against human PLC cells after 48 hrs by MTT assay
[PMID: 30737134]
PLC IC50
> 500 μM
Compound: 1
Antiproliferative activity against human PLC cells after 48 hrs by MTT assay
Antiproliferative activity against human PLC cells after 48 hrs by MTT assay
[PMID: 29859750]
PLC-PRF-5 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human PLC/PRF/5 cells after 48 hrs by MTT assay
Antiproliferative activity against human PLC/PRF/5 cells after 48 hrs by MTT assay
[PMID: 29202398]
PLC-PRF-5 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay
Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay
[PMID: 27670098]
PLC-PRF-5 IC50
> 500 μM
Compound: 1; Ube
Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay
Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay
[PMID: 27322756]
PLC-PRF-5 IC50
> 500 μM
Compound: Bestatin
Cytotoxicity against human PLC-PRF-5 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human PLC-PRF-5 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32791404]
PLC-PRF-5 IC50
22.81 μM
Compound: 1
Antiproliferative activity against human PLC/PRF/5 cells in presence of 5-FU after 48 hrs by MTT assay
Antiproliferative activity against human PLC/PRF/5 cells in presence of 5-FU after 48 hrs by MTT assay
[PMID: 29202398]
SK-OV-3 IC50
> 1000 μM
Compound: Bestatin
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
[PMID: 22901392]
U-266 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human U266 cells after 48 hrs by MTT assay
Antiproliferative activity against human U266 cells after 48 hrs by MTT assay
[PMID: 29202398]
U-266 IC50
> 500 μM
Compound: Ubenimex
Antiproliferative activity against human U266 cells after 48 hrs by MTT assay
Antiproliferative activity against human U266 cells after 48 hrs by MTT assay
[PMID: 27670098]
U-266 IC50
43.48 μM
Compound: 1
Antiproliferative activity against human U266 cells in presence of 5-FU after 48 hrs by MTT assay
Antiproliferative activity against human U266 cells in presence of 5-FU after 48 hrs by MTT assay
[PMID: 29202398]
U-937 IC50
> 1000 μM
Compound: Bestatin
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
[PMID: 23453219]
U-937 IC50
> 500 μM
Compound: 1
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
[PMID: 29859750]
U-937 IC50
> 500 μM
Compound: Bestatin
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32791404]
U-937 IC50
142.63 μM
Compound: 1
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
[PMID: 29202398]
U-937 IC50
142.63 μM
Compound: Ubenimex
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
[PMID: 27670098]
U-937 IC50
9.56 μM
Compound: 1
Antiproliferative activity against human U937 cells in presence of 5-FU after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells in presence of 5-FU after 48 hrs by MTT assay
[PMID: 29202398]
Vero CC50
≥ 25 μM
Compound: 2
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay
[PMID: 28803047]
體外研究
(In Vitro)

Bestatin enhances ATRA-induced differentiation and inhibits ATRA-driven phosphorylation of p38 MAPK in ATRA-sensitive APL NB4 cells. Bestatin can not reverse the differentiation block in ATRA-resistant APL MR2 cells. CD13 ligation with anti-CD13 antibody WM-15 results in phosphorylation of p38 MAPK, reduces the inhibition of Bestatin on the phosphorylation of p38 MAPK, and completely abolishes the enhancement of Bestatin on ATRA-inducing differentiation in NB4 cells[2]. Bestatin (600 μM)-treated cells progress slower through the cell cycle due to decreased rate of cell growth and the frequency of cell division. Bestatin inhibits the frequency of mitosis and the inherent multinuclearity in D. discoideum, and is not cytotoxic to D. discoideum cells at 0-600 μM. Bestatin inhibits aminopeptidase activity in lysates of PsaA-GFP- and GFP-expressing cells by 69.39% and 39.93% of control, respectively[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Bestatin (20 μM) significantly reduces CD13 expression in diabetic mice and results a significant inhibition of MMP-9 specific gelationolytic band densities compared to diabetic vehicle-treated mice. Bestatin treatment significantly inhibits the expression of VEGF and heparanase in diabetic mice. Intravitreal bestatin treatment significantly downregulates the expression of both HIF-1α and VEGF in diabetic mice retinas. Furthermore, the upregulated expression of heparanase in diabetic mice retinas is significantly inhibited by intravitreal bestatin treatment[1]. Bestatin (10, 1, and 0.1mg/kg, i.p.) treatment before the antigen-potentiated humoral response to SRBC results in an increased number of splenocytes producing hemolytic anti-SRBC antibodies (PFC) and the 2-ME-resistant serum hemagglutinin titer (at a dose of 0.1 mg/kg). Bestatin (1 and 0.1 mg/kg) administered to mice five times on alternate days after cyclophosphamide injection does not change the suppressive effect of the drug regarding the number of PFC, and even causes the further decrease of the total anti-SRBC hemagglutinins at dose of 1 mg/kg on day 7 after antigen stimulation[3].

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

308.37

Formula

C16H24N2O4
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

烏苯美司
結(jié)構(gòu)分類
初始來(lái)源

Streptomyces?olivoreticuli
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 8.33 mg/mL (27.01 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.2429 mL 16.2143 mL 32.4286 mL
5 mM 0.6486 mL 3.2429 mL 6.4857 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.83 mg/mL (2.69 mM); 澄清溶液

    此方案可獲得 ≥ 0.83 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 8.3 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.83 mg/mL (2.69 mM); 澄清溶液

    此方案可獲得 ≥ 0.83 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 8.3 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.97%

參考文獻(xiàn)
Kinase Assay
[4]

Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[4]

Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Bestatin is dissolved in PBS. The agent (doses of 10, 1, and 0.1 mg/kg) is injected i.p. to non-cyclophosphamide-treated mice, 5 or 10 times at 24-h intervals before SRBC immunization. The mice are immunized 24 h after the last dose of bestatin. Pharmacological immunosuppression is induced by a single intraperitoneal injection of cyclophosphamide administered at a dose of 350 mg/kg, 12 days before SRBC immunization. Bestatin at the doses of 1 and 0.1 mg/kg is injected to cyclophosphamide-immunosuppressed mice i.p. five times at 48-h intervals or 10 times at 24-h intervals before SRBC immunization. The first dose of bestatin is administered 24 h after cyclophosphamide, while the last dose of the drug is injected 24h before SRBC immunization.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2429 mL 16.2143 mL 32.4286 mL 81.0714 mL
5 mM 0.6486 mL 3.2429 mL 6.4857 mL 16.2143 mL
10 mM 0.3243 mL 1.6214 mL 3.2429 mL 8.1071 mL
15 mM 0.2162 mL 1.0810 mL 2.1619 mL 5.4048 mL
20 mM 0.1621 mL 0.8107 mL 1.6214 mL 4.0536 mL
25 mM 0.1297 mL 0.6486 mL 1.2971 mL 3.2429 mL
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：
Bestatin
目錄號(hào)：
HY-B0134
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