Gossypetin

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天然产物 黄酮类 Flavonoids

Gossypetin  纯度: 99.23%

Gossypetin 是六羟基化的类黄酮，是一种有效的 MKK3 和 MKK6 抑制剂，可强烈减弱 MKK3/6-p38 信号传导途径，具有多种药理活性，包括抗氧化，抗菌和抗癌活性。

Gossypetin

Gossypetin Chemical Structure

CAS No. : 489-35-0

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1 mg ￥9500 In-stock
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生物活性

Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities[1].

IC50 & Target[1]

p38 MAP kinase

 

体外研究
(In Vitro)

Gossypetin (20-60 μM; 48 hours; KYSE30, KYSE450 and KYSE510 cells) treatment significantly inhibits anchorage-dependent esophageal cancer cell growth in dose dependent manner. Gossypetin strongly suppresses anchorage-independent cell growth in esophageal cancer cells[1].
Gossypetin (60 μM; 3 hours; KYSE30 and KYSE410 cells) treatment strongly inhibits p38 activity in a dose-dependent manner and confirms that Gossypetin directly suppresses MKK3 or MKK6 activity[1].
Gossypetin (20-40 μM; 48 hours; KYSE450 and KYSE510 cells) treatment reduces S phase and induces G2 phase cell cycle arrest in a dose-dependent manner[1].
Gossypetin (20-40 μM; 72 hours; esophageal cancer cells) treatment induces intrinsic apoptosis of esophageal cancer cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: KYSE30, KYSE450 and KYSE510 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: Anchorage-dependent esophageal cancer cell growth was significantly inhibited.

Western Blot Analysis[1]

Cell Line: KYSE30 and KYSE410 ccells
Concentration: 60 μM
Incubation Time: 3 hours
Result: p38 activity was strongly inhibited in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: KYSE450 and KYSE510 cells
Concentration: 20 μM, 40 μM
Incubation Time: 48 hours
Result: Reduced S phase and induces G2 phase cell cycle arrest in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Esophageal cancer cells
Concentration: 20 μM, 40 μM
Incubation Time: 72 hours
Result: Induced apoptosis of esophageal cancer cells.

体内研究
(In Vivo)

Gossypetin (100 mg/kg; oral administration; 5 times per week; for 21 days; severe combined immunodeficiency (SCID) female mice) treatment significantly decreases the volume of esophageal tumor growth and without significant loss of body weight. The expression of Ki67 is significantly decreased by Gossypetin. There are no obvious morphological differences between tissues from treated or untreated mic. The phosphorylation of p38, the direct downstream protein of MKK3/6 strongly inhibited in the Gossypetin-treated group[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) injection with esophageal cancer tissue[1]
Dosage: 100 mg/kg
Administration: Oral administration; 5 times per week; for 21 days
Result: Suppressed patient-derived esophageal xenograft tumor growth in an in vivo mouse model.

分子量

318.24

Formula

C15H10O8
CAS 号

489-35-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Xie X, et al. Gossypetin is a novel MKK3 and MKK6 inhibitor that suppresses esophageal cancer growth in vitro and in vivo. Cancer Lett. 2019 Feb 1;442:126-136.