Cat. No.: HY-108359

Alsterpaullone

(Synonyms: 9-Nitropaullone; NSC 705701)

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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.

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Pureté: 99.85%
CAS No.: 237430-03-4
Formule: C₁₆H₁₁N₃O₃
Masse moléculaire:293.28

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Alsterpaullone Chemical Structure

CAS No.: 237430-03-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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)

Voir tous les produits spécifiques à Isoform CDK :

Voir tous les produits spécifiques à Isoform GSK-3 :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	>1 μM Compound: 76	Cytotoxicity against human CEM cells Cytotoxicity against human CEM cells	[PMID: 33539089]
DU-145	IC₅₀	1.1 μM Compound: Alsterpaullone	Cytotoxicity against human DU145 cells after 24 hrs by MTT assay Cytotoxicity against human DU145 cells after 24 hrs by MTT assay	[PMID: 20627564]
HCT-15	IC₅₀	0.62 μM Compound: 4b	Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay	[PMID: 19217301]
Jurkat	CC₅₀	>1 μM Compound: 76	Cytotoxicity against human Jurkat cells Cytotoxicity against human Jurkat cells	[PMID: 33539089]
K562	IC₅₀	1.58 μM Compound: 4b	Cytotoxicity against human K562 cells after 48 hrs by SRB assay Cytotoxicity against human K562 cells after 48 hrs by SRB assay	[PMID: 19217301]
LoVo	IC₅₀	<1 μM Compound: Alsterpaullone	Cytotoxicity against human LoVo cells after 24 hrs by MTT assay Cytotoxicity against human LoVo cells after 24 hrs by MTT assay	[PMID: 20627564]
MCF7	IC₅₀	1.24 μM Compound: 4b	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 19217301]
MCF7	IC₅₀	2.7 μM Compound: Alsterpaullone	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 20627564]
Oocyte	IC₅₀	0.035 μM Compound: 4j	In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes. In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes.	[PMID: 10425100]
PC-3	IC₅₀	1.12 μM Compound: 4b	Cytotoxicity against human PC3 cells after 48 hrs by SRB assay Cytotoxicity against human PC3 cells after 48 hrs by SRB assay	[PMID: 19217301]
RAW264.7	IC₅₀	2.2 μM Compound: Alsterpaullone	Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay	[PMID: 20627564]
Sf9	IC₅₀	0.004 μM Compound: 1b	Inhibition of GSK3-beta expressed in insect Sf9 cells Inhibition of GSK3-beta expressed in insect Sf9 cells	[PMID: 19906467]
U-251	IC₅₀	0.68 μM Compound: 4b	Cytotoxicity against human U251 cells after 48 hrs by SRB assay Cytotoxicity against human U251 cells after 48 hrs by SRB assay	[PMID: 19217301]
U-937	CC₅₀	>1 μM Compound: 76	Cytotoxicity against human U-937 cells Cytotoxicity against human U-937 cells	[PMID: 33539089]

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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS No. 237430-03-4
Appearance Solid
Masse moléculaire 293.28
Formule C₁₆H₁₁N₃O₃
Color Light yellow to yellow
SMILES

O=C1NC2=CC=CC=C2C(NC3=C4C=C([N+]([O-])=O)C=C3)=C4C1
Synonyms

9-Nitropaullone; NSC 705701
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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EMBO Rep

CDK inhibitor Palbociclib targets STING to alleviate autoinflammation. [Abstract]

2022 Jun 7;23(6):e53932. PMID: 35403787

Solvant et solubilité

In Vitro:

DMSO : 5 mg/mL (17.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4097 mL

17.0486 mL

34.0971 mL

5 mM

0.6819 mL

3.4097 mL

6.8194 mL

10 mM

0.3410 mL

1.7049 mL

3.4097 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Leost M, et al. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000 Oct;267(19):5983-94. [Content Brief]

[2]. Lahusen T, et al. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003 Apr;36(4):183-94. [Content Brief]

[3]. Chunying Cui, et al. Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect. J Anal Methods Chem. 2013;2013:602091. [Content Brief]

[4]. Claudia C Faria, et al. Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma. Oncotarget. 2015 Aug 28;6(25):21718-29. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Alsterpaullone

1 Cited Publications

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Alsterpaullone

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Publications Citing Use of MedChemExpress (MCE) Alsterpaullone

Voir tous les produits spécifiques à Isoform CDK

Voir tous les produits spécifiques à Isoform GSK-3

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Alsterpaullone Related Classifications

HY-108359 Related Classifications