1. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR Apoptosis
  2. CDK GSK-3 Apoptosis
  3. Alsterpaullone

Alsterpaullone  (Synonyms: 9-Nitropaullone; NSC 705701)

目录号: HY-108359 纯度: 98.38%
COA 产品使用指南

Alsterpaullone (9-Nitropaullone) 是一种高效的 CDK 抑制剂,作用于 CDK1/cyclin BCDK2/cyclin ACDK2/cyclin ECDK5/p35IC50 值分别为 35 nM、15 nM、200 nM 和 40 nM。Alsterpaullone 是 ATP 竞争性的 GSK-3alpha/GSK-3beta 抑制剂,且作用的 IC50 值都为 4 nM。Alsterpaullone 具有抗肿瘤活性,有用于神经退行性和增生性疾病研究的潜力。Alsterpaullon 诱导白血病细胞凋亡 (apoptosis)。

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Alsterpaullone Chemical Structure

Alsterpaullone Chemical Structure

CAS No. : 237430-03-4

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders[1]. Alsterpaullone induces apoptosis in leukemia cell line[2].

IC50 & Target[1]

Cdk1/cyclin B

35 nM (IC50)

cdk2/cyclin A

15 nM (IC50)

CDK2/Cyc E

200 nM (IC50)

CDK5/p35

40 nM (IC50)

GSK-3α

4 (IC50)

GSK-3β

4 nM (IC50)

体外研究
(In Vitro)

Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line[2].
Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too[3].
Alsterpaullone (20 μM) induces cell death depending on caspase activity[3].

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

Cell Viability Assay[3]

Cell Line: HeLa cells
Concentration: 5, 10, 15, 20, 25, 30 μM
Incubation Time: 48 and 72 hours
Result: The growth of HeLa cells was inhibited in a dose-dependent manner for 48 h and 72 h ranging from 0 to 30 μM.

Apoptosis Analysis[2]

Cell Line: Jurkat cell line
Concentration: 0.3, 1, 3 μM
Incubation Time: 8 hours
Result: Induced dose-dependent apoptosis. 1 μM was sufficient to cause apoptosis, 3 μM demonstrated maximal apoptotic effects[2].

Western Blot Analysis[3]

Cell Line: HeLa cells
Concentration: 2, 4, 6, 12, 24 hours
Incubation Time: 8 hours
Result: The cleavage of PARP started at 4 h, while the activation of caspase-3 occurred at 2 h.
体内研究
(In Vivo)

Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts[4].

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

Animal Model: 5-6 week old athymic nude mice[4]
Dosage: 30 mg/kg
Administration: Subcutaneous injections, daily for 2 weeks
Result: Antitumor effect in Group 3 medulloblastomas.
分子量

293.28

Formula

C16H11N3O3

CAS 号
性状

固体

颜色

Light yellow to yellow

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 2 years
-20°C 1 year
纯度 & 产品资料

纯度: 98.38%

参考文献
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  • 稀释计算器

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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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Alsterpaullone
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HY-108359
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