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  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)

目錄號: HY-108359 純度: 99.85%
COA 產(chǎn)品使用指南

Alsterpaullone (9-Nitropaullone) 是一種高效的 CDK 抑制劑,作用于 CDK1/cyclin BCDK2/cyclin A、CDK2/cyclin ECDK5/p35IC50 值分別為 35 nM、15 nM、200 nM 和 40 nM。Alsterpaullone 是 ATP 競爭性的 GSK-3alpha/GSK-3beta 抑制劑,且作用的 IC50 值都為 4 nM。Alsterpaullone 具有抗腫瘤活性,有用于神經(jīng)退行性和增生性疾病研究的潛力。Alsterpaullon 誘導(dǎo)白血病細(xì)胞凋亡 (apoptosis)。

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Alsterpaullone Chemical Structure

Alsterpaullone Chemical Structure

CAS No. : 237430-03-4

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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 5 mg/mL (17.05 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.4097 mL 17.0486 mL 34.0971 mL
5 mM 0.6819 mL 3.4097 mL 6.8194 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.85%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4097 mL 17.0486 mL 34.0971 mL 85.2428 mL
5 mM 0.6819 mL 3.4097 mL 6.8194 mL 17.0486 mL
10 mM 0.3410 mL 1.7049 mL 3.4097 mL 8.5243 mL
15 mM 0.2273 mL 1.1366 mL 2.2731 mL 5.6829 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.

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產(chǎn)品名稱:
Alsterpaullone
目錄號:
HY-108359
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