2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. RAR/RXR PPAR Aldose Reductase
  4. Drupanin

Drupanin 是具有口服活性且选择性的 AKR1C3 enzyme 抑制剂和 RXRα 激动剂，其 EC50 值为 4.8 μM，发现于绿色蜂胶。Drupanin 还适度激活 PPARγ。Drupanin 诱导脂肪生成，并提高 3T3-L1 成纤维细胞中 aP2 mRNA 的水平。Drupanin 在乳腺癌和前列腺癌研究中具有潜力。

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Drupanin Chemical Structure

Drupanin Chemical Structure

CAS No. : 53755-58-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300
In-stock
1 mg ￥1363
In-stock
5 mg ￥3000
In-stock
10 mg ￥4800
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

Drupanin 相关抗体

Top Publications Citing Use of Products

查看 RAR/RXR 亚型特异性产品:

查看所有亚型
RXRα RXRβ RXRγ

查看 PPAR 亚型特异性产品:

查看所有亚型
PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers[1][2][3].

IC50 & Target

PPARα

39.0 μM (EC50)

PPARγ

14.6 μM (EC50)

PPARδ

N.D.(not d ()

RXR α

2.1 μM (EC50)

RXRγ

4.6 μM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
HEK293 IC50
25.6 μM
Compound: 9
Modulation of HIF1 expressed in HEK293 cells assessed as luciferase activity under hypoxic condition after 24 hrs by luminometer analysis
Modulation of HIF1 expressed in HEK293 cells assessed as luciferase activity under hypoxic condition after 24 hrs by luminometer analysis
[PMID: 21865046]
HeLa IC50
10.3 μg/mL
Compound: 3
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
[PMID: 19942440]
MCF-10A CC50
> 200 μM
Compound: 2
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MCF7 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MDA-MB-231 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PC-3 IC50
> 200 μM
Compound: 2
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PNT2 CC50
> 200 μM
Compound: 2
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
体外研究
(In Vitro)

Drupanin (2.5-25 μM，1 小时) 在 HEK 293 细胞中刺激 PPARγ 和 cAMP 响应元件结合蛋白-结合蛋白之间的相互作用 (EC50 值：14.6 μM)[2]。
Drupanin (25 μM，5 天) 增强小鼠 3T3-L1 成纤维细胞的脂肪生成[2]。
Drupanin (101.7-103.5 μM, 48 小时) 对 PC3 和 LnCaP 细胞显示出细胞毒性[3].

Drupanin 对每种 RXR 亚型辅因子的 EC50 值[2]

subtypes RXRα RXRγ RXRδ
EC50 (μM) 2.1 4.6 7.0

Drupanin 对每种 PPAP 亚型辅因子的 EC50 值[2]
subtypes PPARα PPARγ PPARδ
EC50 (μM) 39.0 14.6 N.D. (not detected)

Drupanin 的生长抑制作用[3]
NCI-H460 MCF7 PC3 LnCaP HL60 U937 S-180
GI50 (μM) 158.5 141.3 501.2 338.8 166.0 323.6 416.9
LC50 (μM) N.D. N.D. 885.1 1331.4 N.D. N.D. N.D.

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

Drupanin 相关抗体:

Real Time qPCR[2]

Cell Line: HEK 293 cells
Concentration: 2.5-25 μM
Incubation Time: 1 h
Result: Slightly increased luciferase activity for each PPAR subtype (α, γ, and δ).
体内研究
(In Vivo)

Drupanin (100 mg/kg，口服，每天服用, 持续 28 天) 在移植了肉瘤 S-180 的 DDY 小鼠中可以抑制肿瘤生长，并引起基因毒性损伤[3]。

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

Animal Model: DDY mice allografted with sarcoma S-180[2]
Dosage: 100 mg/kg
Administration: p.o., daily for 28 days
Result: Resulted in a significant decrease of tumor mass at a dosage of 100 mg/kg/d (p<0.05) and caused DNA damage in sarcoma S-180.
分子量

232.28

Formula

C14H16O3
CAS 号
性状

固体

颜色

Off-white to light yellow

结构分类
初始来源

A. Mellifera
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
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (430.51 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 4.3051 mL 21.5257 mL 43.0515 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 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
参考文献

Drupanin 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 4.3051 mL 21.5257 mL 43.0515 mL 107.6287 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 mL 21.5257 mL
10 mM 0.4305 mL 2.1526 mL 4.3051 mL 10.7629 mL
15 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
20 mM 0.2153 mL 1.0763 mL 2.1526 mL 5.3814 mL
25 mM 0.1722 mL 0.8610 mL 1.7221 mL 4.3051 mL
30 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
40 mM 0.1076 mL 0.5381 mL 1.0763 mL 2.6907 mL
50 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1526 mL
60 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
80 mM 0.0538 mL 0.2691 mL 0.5381 mL 1.3454 mL
100 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 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:

Drupanin53755-58-1RAR/RXRPPARAldose ReductaseRetinoic acid receptorsRetinoid X receptorsPeroxisome proliferator-activated receptorsorally activeAKR1C3 enzymeRXRαPPARγ3T3-L1 fibroblastsbreast and prostate cancersInhibitorinhibitorinhibit

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