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  1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. Pironetin

Pironetin 是從鏈霉菌屬物種分離的 α/β 不飽和內(nèi)酯。Pironetin 與 α-tubulin 結(jié)合,是微管聚合的有效抑制劑,具有細(xì)胞周期停滯和抗腫瘤活性。

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Pironetin Chemical Structure

Pironetin Chemical Structure

CAS No. : 151519-02-7

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].

IC50 & Target

Microtubule[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
0.0029 μM
Compound: Pironetin
Cytotoxicity against compound-sensitive human A2780 cells after 24 hrs by MTT assay
Cytotoxicity against compound-sensitive human A2780 cells after 24 hrs by MTT assay
[PMID: 21396747]
A2780 IC50
0.008 μM
Compound: pironetin
Cytotoxicity against human A2780 cells after 24 hrs by MTT assay
Cytotoxicity against human A2780 cells after 24 hrs by MTT assay
[PMID: 25426924]
A2780 GI50
22.2 nM
Compound: 1
Inhibition of tubulin alpha in human A2780 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Inhibition of tubulin alpha in human A2780 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30693770]
A2780 ADR IC50
0.003 μM
Compound: Pironetin
Cytotoxicity against compound-resistant human A2780AD cells after 24 hrs by MTT assay
Cytotoxicity against compound-resistant human A2780AD cells after 24 hrs by MTT assay
[PMID: 21396747]
A2780 ADR IC50
0.025 μM
Compound: pironetin
Cytotoxicity against human A2780AD cells after 24 hrs by MTT assay
Cytotoxicity against human A2780AD cells after 24 hrs by MTT assay
[PMID: 25426924]
A549 GI50
7.5 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human A549 cells assessed as reduction in growth after 4 days by HCS assay
Cytotoxicity against human A549 cells assessed as reduction in growth after 4 days by HCS assay
[PMID: 31130264]
DC3F GI50
9.5 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against hamster DC-3F cells assessed as reduction in growth after 4 days by HCS assay
Cytotoxicity against hamster DC-3F cells assessed as reduction in growth after 4 days by HCS assay
[PMID: 31130264]
EL4 GI50
15 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against C57BL/6 mouse EL4 cells assessed as reduction in growth after 3 days
Cytotoxicity against C57BL/6 mouse EL4 cells assessed as reduction in growth after 3 days
[PMID: 31130264]
HCT-15 IC50
< 0.015 μM
Compound: Pironetin
Cytotoxicity against human HCT15 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human HCT15 cells after 48 hrs by sulforhodamine B assay
[PMID: 30601004]
HEK293 IC50
0.017 μM
Compound: pironetin
Cytotoxicity against human HEK293 cells after 3 days by MTT assay
Cytotoxicity against human HEK293 cells after 3 days by MTT assay
[PMID: 25426924]
HEK293 IC50
0.017 μM
Compound: Pironetin
Cytotoxicity against HEK293 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 25240870]
HeLa IC50
0.092 μM
Compound: Pironetin
Cytotoxicity against human HeLa cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human HeLa cells after 48 hrs by sulforhodamine B assay
[PMID: 30601004]
HL-60 GI50
20 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human HL60 cells assessed as reduction in growth after 24 hrs by MTT assay
Cytotoxicity against human HL60 cells assessed as reduction in growth after 24 hrs by MTT assay
[PMID: 31130264]
HT-29 IC50
0.0064 μM
Compound: pironetin
Cytotoxicity against human HT-29 cells after 3 days by MTT assay
Cytotoxicity against human HT-29 cells after 3 days by MTT assay
[PMID: 25426924]
HT-29 IC50
0.0064 μM
Compound: Pironetin
Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 25240870]
K562 GI50
17.3 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human K562 cells assessed as reduction in growth after 4 days by MTT assay
Cytotoxicity against human K562 cells assessed as reduction in growth after 4 days by MTT assay
[PMID: 31130264]
K562/Adr GI50
16 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human K562/ADR cells assessed as reduction in growth after 4 days by MTT assay
Cytotoxicity against human K562/ADR cells assessed as reduction in growth after 4 days by MTT assay
[PMID: 31130264]
MCF7 IC50
0.006 μM
Compound: pironetin
Cytotoxicity against human MCF7 cells after 3 days by MTT assay
Cytotoxicity against human MCF7 cells after 3 days by MTT assay
[PMID: 25426924]
MCF7 IC50
0.006 μM
Compound: Pironetin
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
[PMID: 25240870]
MCF7 IC50
0.015 μM
Compound: Pironetin
Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
[PMID: 30601004]
MCF7 GI50
5 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human MCF7 cells assessed as reduction in growth after 3 days by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in growth after 3 days by MTT assay
[PMID: 31130264]
MDA-MB-231 GI50
4.6 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in growth after 4 days by HCS assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in growth after 4 days by HCS assay
[PMID: 31130264]
NCI-H69 GI50
17.5 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human H69 cells assessed as reduction in growth after 7 days by MTT assay
Cytotoxicity against human H69 cells assessed as reduction in growth after 7 days by MTT assay
[PMID: 31130264]
P388 GI50
100 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against mouse P388 cells assessed as reduction in growth after 24 hrs by MTT assay
Cytotoxicity against mouse P388 cells assessed as reduction in growth after 24 hrs by MTT assay
[PMID: 31130264]
T98G GI50
7.5 nM
Compound: 1; (-)-PA-48153C
Cytotoxicity against human T98G cells assessed as reduction in growth after 4 days by MTS assay
Cytotoxicity against human T98G cells assessed as reduction in growth after 4 days by MTS assay
[PMID: 31130264]
體外研究
(In Vitro)

Pironetin (20-100 ng/mL; 24 hours; 3Y1 cells) treatment arrests the cell cycle progression at G2/M in 3Y1 cells[1].
Pironetin (1-10000 ng/mL; 3 days; HeLa, A2780 and K-NRK cells) treatment inhibits the cell proliferation. IC50 values against these cell lines are almost 10 ng/mL[1].

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

Cell Cycle Analysis[1]

Cell Line: 3Y1 cells
Concentration: 20 ng/mL, 50 ng/mL, 100 ng/mL
Incubation Time: 24 hours
Result: Arrested the cell cycle progression at G2/M in3Y1 cells.

Cell Proliferation Assay[1]

Cell Line: HeLa, A2780 and K-NRK cells
Concentration: 1 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL and 10000 ng/mL
Incubation Time: 3 days
Result: Inhibited the cell proliferation.
體內(nèi)研究
(In Vivo)

Pironetin (0.78-6.25 mg/kg; intraperitoneal injection; daily; for 5 days; female CDF1-SLC mice) treatment shows a moderate antitumor effect, however, a severe weight loss is observed as a side effect[1].

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

Animal Model: Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells[1]
Dosage: 0.78 mg/kg, 1.56 mg/kg, 3.13 mg/kg, 6.25 mg/kg
Administration: Intraperitoneal injection; daily; for 5 days
Result: Showed a moderate antitumor effect.
分子量

324.45

Formula

C19H32O4

CAS 號
性狀

油狀物

顏色

Colorless to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗: 

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

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This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

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純度 & 產(chǎn)品資料
參考文獻(xiàn)
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:
Pironetin
目錄號:
HY-116446
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