PD 407824
Chemical Name: 9-Hydroxy-4-phenyl-pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione
Purity: ≥98%
Biological Activity
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.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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Cisplatin sensitivity mediated by WEE1 and CHK1 is mediated by miR-155 and the miR-15 family.
Pouliot L, Chen Y, Bai J, Guha R, Martin S, Gottesman M, Hall M
Cancer Res, 2012;72(22):5945-55. -
Inhibiting checkpoint kinase 1 protects bone from bone resorption by mammary tumor in a mouse model
S Liu, Y Liu, K Minami, A Chen, Q Wan, Y Yin, L Gan, A Xu, N Matsuura, M Koizumi, Y Liu, S Na, J Li, H Nakshatri, BY Li, H Yokota
Oncotarget, 2018;9(10):9364-9378. -
Structure and inhibition of the human cell cycle checkpoint kinase, Wee1A kinase: an atypical tyrosine kinase with a key role in CDK1 regulation.
Squire et al.
Structure, 2005;13:541 -
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.
Palmer et al.
J.Med.Chem., 2006;49:4896 -
Discovery of a small-molecule BMP sensitizer for human embryonic stem cell differentiation.
Feng et al.
Cell Rep., 2016;15:2063
Product Datasheets
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Citations for PD 407824
The citations listed below are publications that use Tocris products. Selected citations for PD 407824 include:
3 Citations: Showing 1 - 3
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Decreased miR122 in hepatocellular carcinoma leads to chemoresistance with increased arginine.
Authors: Kishikawa Et al.
Oncotarget 2015;6:8339
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Cisplatin sensitivity mediated by WEE1 and CHK1 is mediated by miR-155 and the miR-15 family.
Authors: Pouliot Et al.
Cancer Res 2012;72:5945
-
Synthetic lethal RNAi screening identifies sensitizing targets for gemcit. therapy in pancreatic cancer.
Authors: Azorsa Et al.
J Transl Med 2009;7:43
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