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)

Cat. No.: HY-108359 Purity: ≥98.0%
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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. Alsterpaullone induces apoptosis in leukemia cell line.

For research use only. We do not sell to patients.

Alsterpaullone Chemical Structure

Alsterpaullone Chemical Structure

CAS No. : 237430-03-4

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Solution
10 mM * 1 mL in DMSO USD 726 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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)

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.
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.
Molecular Weight

293.28

Formula

C₁₆H₁₁N₃O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: ≥98.0%

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Alsterpaullone
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HY-108359
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