2. Metabolic Enzyme/Protease Apoptosis
  3. Aminotransferases (Transaminases) Apoptosis
  4. Aspulvinone O

Aspulvinone O 是谷氨酸草酰乙酸转氨酶 GOT1 的选择性抑制剂。Aspulvinone O 可抑制谷氨酰胺代谢并减少 NADPH 生成，从而诱导胰腺导管腺癌 (PDAC) 细胞氧化应激和凋亡 (apoptosis)。Aspulvinone O 在体外抑制 PDAC 细胞增殖，在异种移植模型中抑制肿瘤生长。

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Aspulvinone O Chemical Structure

Aspulvinone O Chemical Structure

CAS No. : 914071-54-8

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规格 价格 是否有货
1 mg ￥8600
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Aspulvinone O 相关抗体

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GOT/AST

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aspulvinone O is a selective inhibitor of glutamate oxaloacetate aminotransferase GOT1. Aspulvinone O inhibits glutamine metabolism and reduces NADPH production, thereby inducing oxidative stress and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cells. Aspulvinone O inhibits PDAC cell proliferation in vitro and tumor growth in xenograft models[1][2].

IC50 & Target

GOT/AST

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
J774.1 IC50
3 μM
Compound: 11
Anti-inflammatory activity against mouse J774A.1 macrophage assessed as reduction in LPS-induced LDH release incubated for 1 hr in presence of nigericin by LDH assay
Anti-inflammatory activity against mouse J774A.1 macrophage assessed as reduction in LPS-induced LDH release incubated for 1 hr in presence of nigericin by LDH assay
[PMID: 35293744]
体外研究
(In Vitro)

Aspulvinone O (0.1-100 μM；48 h) 抑制胰腺导管腺癌细胞系 (SW1990、PANC-1、AsPC-1) 增殖，IC50 为 20.54-26.80 μM，对癌细胞选择性高于正常细胞[1]。
Aspulvinone O (10-40 μM；48 h) 将 SW1990 细胞的细胞周期阻滞于 S 期，并诱导凋亡[1]。
Aspulvinone O (10-40 μM；24 h) 降低 SW1990 细胞谷氨酰胺代谢中间产物 (OAA、苹果酸) 水平，并降低 NADPH/NADP+ 比率[1]。

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

Aspulvinone O 相关抗体:

Cell Viability Assay[1]

Cell Line: SW1990, PANC-1, AsPC-1 (human PDAC cells)
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Dose-dependent growth inhibition with IC50 of 20.54 μM (SW1990), 26.80 μM (PANC-1), and 23.12 μM (AsPC-1), respectively, while showed no significant cytotoxicity (IC50 >100 μM) against normal HPDE6C7 cells.
体内研究
(In Vivo)

Aspulvinone O (2.5 mg/kg，5 mg/kg；腹腔注射；每日一次；14 d) 显著抑制 CB17/scid 小鼠 SW1990 PDAC 细胞异种移植模型的肿瘤生长，肿瘤重量减少 40-60%，且无明显全身毒性[1]。

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

Animal Model: CB17/scid male mice (8 weeks old, ~20 g), SW1990 cell-derived xenograft model[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: Intraperitoneal injection (i.p.), daily for 14 days, starting when tumors reached ~3 mm diameter
Result: Significantly reduced tumor volume and weight compared to control. Showed a 60% reduction in tumor weight in the 5 mg/kg group, at day 14 and a 55% reduction in tumor volume.
Decreased levels of oxaloacetate (OAA) and malate (~50% reduction), increased aspartate (Asp) and glutamine (Gln) (~30% increase), and a 45% decrease in NADPH/NADP+ ratio compared to control.
No significant changes in body weight or histomorphology, indicating good tolerability.
分子量

448.51

Formula

C27H28O6
CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源

Aspergillus terreus
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (55.74 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2296 mL 11.1480 mL 22.2960 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥96.0%

COA (284 KB)

产品使用指南 (1538 KB)
参考文献

Aspulvinone O 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2296 mL 11.1480 mL 22.2960 mL 55.7401 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL 11.1480 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL 5.5740 mL
15 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7160 mL
20 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7870 mL
25 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
50 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 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.

Keywords:

Aspulvinone O914071-54-8Aminotransferases (Transaminases)ApoptosisAminotransferases (Transaminases) GOT1ROSenergy metabolismPDACgrowthglutamine metabolismInhibitorinhibitorinhibit

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