Alsterpaullone, CDK, GSK Inhibitor

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Catalog numberSIH-431-1MG
NameAlsterpaullone, CDK, GSK Inhibitor
Size1 mg
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Stock availabilitIn StockIn Stock
CAS number237430-03-4
DescriptionCDK, GSK Inhibitor
Molecular weight293,3 g/mol
Primary research fieldsCell Signaling, Cancer, Apoptosis, Cancer Growth Inhibitors, Tyrosine Kinase Inhibitors
Other name9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5)-one
Product categorySmall Molecules
Product typeInhibitor
Chemical formulaC16H11N3O3
Purity pourcentage≥98% (HPLC)
Soluble inSoluble in DMSO; insoluble in water or 100% ethanol
Physical appearanceYellow to brown powder
Storage recommendations-20ºC
Shipping recommendationsShipped Ambient
Safety informationClassification: Skin irritation (Category 2), H315 Eye irritation (Category 2A), H319 Specific target organ toxicity - single exposure (Category 3), Respiratory system, H335 Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. Hazard statements: H315 Causes skin irritation. H319 Causes serious eye irritation. H335 May cause respiratory irritation. Precautionary statements: P261 Avoid breathing dust/ fume/ gas/ mist/ vapours/ spray. P264 Wash skin thoroughly after handling. P271 Use only outdoors or in a well - ventilated area. P280 Wear protective gloves/ eye protection/ face protection. P302 + P352 IF ON SKIN: Wash with plenty of soap and water. P304 + P340 IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312 Call a POISON CENTER or doctor/ physician if you feel unwell. P321 Specific treatment (see supplemental first aid instructions on this label). P332 + P313 If skin irritation occurs: Get medical advice/ attention. P337 + P313 If eye irritation persists: Get medical advice/ attention. P362 Take off contaminated clothing and wash before reuse. P403 + P233 Store in a well - ventilated place. Keep container tightly closed. P405 Store locked up. P501 Dispose of contents/ container to an approved waste disposal plant.
PubChem number5005498
Scientific contextAlsterpaullone is a potent inhibitor of CDK1/cyclin B. It is also a potent and selective inhibitor of GSK-3β and CDK5/p25. Alsterpaullone induces apoptosis by activating caspase-8 and caspase-9, followed by disruption of the mitochondrial potential. It is cell-permeable.
Bibliography1. Zaharevitz D.W., et al. (1999). Cancer Research. 59(11): 2566–2569. 2. Lahusen T., De Siervi A., Kunick C., & Senderowicz A.M. (2003) Mol. Carcinogenesis. 36(4): 183–194. 3. Schultz C., et al. (1999) J. Med. Chem. 42(15): 2909–2919.
Release date1-Oct-2014
PubMed numberRefer to PubMed
Tested applicationsTo be tested
Tested reactivityTo be tested
Representative figure legendChemical structure of Alsterpaullone (SIH-431), a GSK3beta kinase inhibitor, CDK5/p25 inhibitor. CAS #: 237430-03-4. Molecular Formula: C16H11N3O3. Molecular Weight: 293.3 g/mol. Chemical structure of Alsterpaullone, a GSK3beta kinase inhibitor, CDK5/p25 inhibitor (SIH-431). CAS # 237430-03-4. Molecular Formula: C16H11N3O3.
Warning informationNon-hazardous
Country of productionCanada
Total weight (kg)0.25
Net weight (g)0.001
Additional descriptionTissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.