Alsterpaullone

For research use only.

Catalog No.S0354 Synonyms: Alp, 9-Nitropaullone, NSC 705701

Alsterpaullone Chemical Structure

CAS No. 237430-03-4

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.

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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)
4 nM 4 nM 15 nM 35 nM

Protocol

Solubility (25°C)

Chemical Information

Molecular Weight 293.28
Formula
C16H11N3O3
CAS No. 237430-03-4
Storage powder
in solvent
Synonyms Alp, 9-Nitropaullone, NSC 705701
Smiles C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)[N+](=O)[O-]

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03744663 Suspended Drug: Suboxone® SL|Drug: Sublocade® Opioid Use Wake Forest University Health Sciences June 2022 Phase 2
NCT05033145 Not yet recruiting Drug: AZVUDINE|Drug: AZVUDINE placebo COVID-19 HRH Holdngs Limited|GALZU INSTITUTE OF RESEARCH TEACHING APPLIED SCIENCE AND TECHNOLOGY Brazil|SANTA CASA DE MISERICORDIA DE CAMPOS HOSPITAL (SCMCH) Brazil|UNIVERSIDADE ESTADUAL DO NORTE FLUMINENSE (UENF) Brazil October 2021 Phase 3
NCT04783428 Recruiting Other: No intervention Tumor-induced Osteomalacia (TIO) Ultragenyx Pharmaceutical Inc September 2021 --
NCT04908826 Recruiting Procedure: Indocyanine Green (ICG) administration Laparoscopic; Cholecystectomy|Cholelithiasis; Bile Duct|Choledocholithiasis|Stone - Biliary|Post-Op Complication|Cholangiography|Indocyanine Green|Intraoperative Complications|Bile Duct Injury Aristotle University Of Thessaloniki|George Papanicolaou Hospital September 1 2021 Not Applicable
NCT05011370 Not yet recruiting -- Intestinal Failure-associated Liver Disease Protara Therapeutics August 13 2021 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID