PD 0332991 isethionate
Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one isethionate salt
Purity: ≥98%
Biological Activity
PD 0332991 isethionate is a potent cyclin-dependent kinase 4 (cdk4) and cdk6 inhibitor (IC50 values are 11 nM and 15 nM respectively). Also displays activity at cdk2, cdk5 and cdk9 (IC50 values reported to be 1.6, 1.8 and 0.42-1.1 μM, respectively). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant.External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PD 0332991 isethionate is reviewed on the Chemical Probes website.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105
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Citations for PD 0332991 isethionate
The citations listed below are publications that use Tocris products. Selected citations for PD 0332991 isethionate include:
8 Citations: Showing 1 - 8
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Selective activation and down-regulation of Trk receptors by neurotrophins in human neurons co-expressing TrkB and TrkC.
Authors: Jia Et al.
J Neurochem 2022;161:463-477
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Human cells lacking CDC14A and CDC14B show differences in ciliogenesis but not in mitotic progression.
Authors: Elmar Et al.
J Cell Sci 2021;134
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Human cells lacking CDC14A and CDC14B show differences in ciliogenesis but not in mitotic progression.
Authors: Elmar Et al.
J Cell Sci 2021;134
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Differentiation of PTH-Expressing Cells From Human Pluripotent Stem Cells.
Authors: Michael A Et al.
Endocrinology 2020;161
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CEP44 ensures the formation of bona fide centriole wall, a requirement for the centriole-to-centrosome conversion.
Authors: Charlotta Et al.
Nat Commun 2020;11:903
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Human cells lacking CDC14A and CDC14B show differences in ciliogenesis but not in mitotic progression.
Authors: Elmar Et al.
J Cell Sci 2020;
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Huntington's Disease Patient-Derived Astrocytes Display Electrophysiological Impairments and Reduced Neuronal Support.
Authors: Garcia Et al.
Front Neurosci 2019;13:669
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Cell-Cycle Regulation Accounts for Variability in Ki-67 Expression Levels.
Authors: Jacques Et al.
Cancer Res 2017;77:2722-2734
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