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Anticancer agent 160 (Compound 6) 是一种来源于 Parthenium hysterophorus 的天然产物。Anticancer agent 160 对 HCT-116 细胞有细胞毒性,IC50=5.0 μM。

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Anticancer agent 160 Chemical Structure

Anticancer agent 160 Chemical Structure

CAS No. : 2983122-03-6

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 160 (Compound 6) is a natural product derived from Parthenium hysterophorus. Anticancer agent 160 is cytotoxic to HCT-116 cells, IC50=5.0 μM[1].

IC50 & Target

Caspase 3

23.4 nM (EC50)

体外研究
(In Vitro)

M109S (0.1-10000 nM, 24 ~ 48 h)对Bax和Bak诱导的细胞凋亡均有抑制作用[1]
M109S (0-10μM, 4 h)抑制Staurosporine (HY-15141 STS)诱导的MEF细胞凋亡[1]
M109S (0-10μM, 24 h)抑制依托泊苷(HY-13629 Etoposide)诱导的Neuro2a细胞凋亡[1]
M109S (500 nM, 24 h)抑制Obatoclax(HY-10969A)诱导的ARPE19细胞凋亡[1]
M109S (500 nM, 48 h)抑制构象变化(N端暴露) [1]
M109S (500 nM, 48 h)抑制Bax的线粒体易位[1]
M109S(1.0 μM, 4h)降低线粒体耗氧量和活性氧,而M109S(0.1-1 mM)增加糖酵解[1]

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

Apoptosis Analysis[1]

Cell Line: MEF(Wt, Bax only, Bak only)
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM
Incubation Time: 24 h((WT and Bax-only), 48 h (Bak-only)
Result: Showed a dose-dependent suppression of caspase activation in all three types of MEFs.

Apoptosis Analysis[1]

Cell Line: Showed a dose-dependent suppression of caspase activation in all three types of MEFs.
Concentration: 0 nM, 1.6 nM,8 nM, 40 nM, 200 nM, 10 μM
Incubation Time: 4 h
Result: Suppressed STS-induced caspase activation in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Neuro2a
Concentration: 0 nM, 40 nM, 200 nM, 10 μM
Incubation Time: 24 h
Result: Suppressed Etoposide -induced caspase activation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: ARPE19
Concentration: 500 nM
Incubation Time: 24 h
Result: Significantly inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control.

Immunofluorescence[1]

Cell Line: iBax cells
Concentration: 500 nM
Incubation Time: 48 h
Result: The frequency of the punctuated staining was significantly reduced by M109S.
体内研究
(In Vivo)

M109S(10mg/kg灌胃, 48 h 内注射三次)可保护视网膜免受强光诱导的光感受器死亡[1]
M109S(腹腔注射, 1mg /kg,静脉注射, 5mg /kg,或口服灌胃, 10mg /kg))是一种穿透血脑/视网膜屏障的口服生物活性细胞死亡抑制剂[1]

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

Animal Model: Abca4-/-Rdh8-/- mice
Dosage: 10mg/kg
Administration: Oral Gavage (PO)
Result: Comparing to micewith M109S, the number of AF spots was similar to that detected in the dark-adapted mice
Animal Model: Mice and Rat
Dosage: Intraperitoneal injection (IP, 1 mg/kg), Intravenous injection (IV, 5 mg/kg), or Oral gavage (OP, 10 mg/kg).
Administration: Intraperitoneal injection (IP, 1 mg/kg), Intravenous injection (IV, 5 mg/kg), or Oral gavage (OP, 10 mg/kg).
Result: In mice, M109S reached 1.0 mg/mL (2.6 mM) plasma concentration within 30 min from administration, and it remained at 596± 134 ng/mL (1.6± 0.36 mM) 24 h after the oral gavage administration, the same as in rat. At 24 h after the oral gavage administration, the level of M109S in the plasma was 565.3± 188.3 nM in rats.The level of M109S in the rat retina and brain reached 171.0± 52.0 nM and 222.7± 74.7 nM, respectively, 24 h after its oral administration.
分子量

475.53

Formula

C28H29NO6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献

Anticancer agent 160 相关分类

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  • 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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Anticancer agent 160
目录号:
HY-156186
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