Alsterpaullone

Synonyms: Alp, 9-Nitropaullone, NSC 705701

Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 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 acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.

Alsterpaullone Chemical Structure

Alsterpaullone Chemical Structure

CAS No. 237430-03-4

Purity & Quality Control

Batch: S035401 DMSO]25 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.81%
99.81

Alsterpaullone Related Products

Signaling Pathway

Biological Activity

Description Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 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 acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
Targets
caspase-9 [2] GSK-3α [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
CDK2/cyclin A [1]
(Cell-free assay)
CDK1/cyclin B [1]
(Cell-free assay)
Click to View More Targets
4 nM 4 nM 15 nM 35 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03160430 Not yet recruiting
Kidney Failure Chronic
Resverlogix Corp
November 22 2024 Phase 1|Phase 2
NCT06377293 Not yet recruiting
End-Stage Kidney Disease
Far Eastern Memorial Hospital
November 2024 Not Applicable
NCT06405555 Not yet recruiting
Heart Failure With Reduced Ejection Fraction|Hypotension|LV Dysfunction
Ottawa Heart Institute Research Corporation
August 1 2024 Phase 2|Phase 3
NCT06398002 Not yet recruiting
Secondary Hyperparathyroidism|End-stage Kidney Disease
Iain Bressendorff|Herlev Hospital
August 1 2024 Phase 2
NCT06383403 Not yet recruiting
Primary Biliary Cholangitis
Ipsen
July 1 2024 Phase 3
NCT06095986 Not yet recruiting
Primary Sclerosing Cholangitis
Galmed Research and Development Ltd.|Virginia Commonwealth University|Galmed Pharmaceuticals Ltd
June 2024 Phase 2

Chemical Information & Solubility

Molecular Weight 293.28 Formula
C16H11N3O3
CAS No. 237430-03-4 SDF --
Smiles C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)[N+](=O)[O-]
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 25 mg/mL ( (85.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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