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Submit ReviewPD 407824
Description: Potent and selective inhibitor of Chk1 and Wee1
Chemical Name: 9-Hydroxy-4-phenyl-pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione
Purity: ≥98% (HPLC)
Biological Activity for PD 407824
PD 407824 is a potent and selective inhibitor of checkpoint kinases Chk1 and Wee1 (IC50 values are 47 and 97 nM respectively). Displays selectivity over a range of other protein kinases; IC50 values are 3.4, 3.75, > 5, > 50, > 50 and > 50 μM for PKC, CDK4, other CDKs, c-Src, PDGFR and FGFR respectively. Also sensitizes hESCs to BMP4 to induce differentiation.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PD 407824
PD 407824 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for PD 407824
| M. Wt | 328.32 |
| Formula | C20H12N2O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 622864-54-4 |
| PubChem ID | 4369491 |
| InChI Key | IAUZTOZLTFSMIE-UHFFFAOYSA-N |
| Smiles | OC1=CC2=C(NC3=C2C2=C(C(=O)NC2=O)C(=C3)C2=CC=CC=C2)C=C1 |
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.
Solubility Data for PD 407824
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.83 | 100 | |
| ethanol | 8.2 | 25 |
Preparing Stock Solutions for PD 407824
The following data is based on the product molecular weight 328.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.05 mL | 15.23 mL | 30.46 mL |
| 5 mM | 0.61 mL | 3.05 mL | 6.09 mL |
| 10 mM | 0.3 mL | 1.52 mL | 3.05 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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Product Datasheets for PD 407824
References for PD 407824
References are publications that support the biological activity of the product.
Squire et al (2005) Structure and inhibition of the human cell cycle checkpoint kinase, Wee1A kinase: an atypical tyrosine kinase with a key role in CDK1 regulation. Structure 13 541 PMID: 15837193
Palmer et al (2006) 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenylring substitutions. J.Med.Chem. 49 4896 PMID: 16884302
Feng et al (2016) Discovery of a small-molecule BMP sensitizer for human embryonic stem cell differentiation. Cell Rep. 15 2063 PMID: 27210748
If you know of a relevant reference for PD 407824, please let us know.
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Keywords: PD 407824, PD 407824 supplier, Selective, inhibitors, inhibits, Chk1, Wee1, Checkpoint, Control, Kinases, PD407824, Pfizer, BMP4, sensitizes, sensitizers, BMP, and, Other, Activin, Receptors, ESCs, iPSC, 2694, Tocris Bioscience
3 Citations for PD 407824
Citations are publications that use Tocris products. Selected citations for PD 407824 include:
Azorsa et al (2009) Synthetic lethal RNAi screening identifies sensitizing targets for gemcit. therapy in pancreatic cancer. J Transl Med 7 43 PMID: 19519883
Kishikawa et al (2015) Decreased miR122 in hepatocellular carcinoma leads to chemoresistance with increased arginine. Oncotarget 6 8339 PMID: 25826076
Pouliot et al (2012) Cisplatin sensitivity mediated by WEE1 and CHK1 is mediated by miR-155 and the miR-15 family. Cancer Res 72 5945 PMID: 22942255
Do you know of a great paper that uses PD 407824 from Tocris? Please let us know.
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.