PD 407824

Names

[ Name ]:
PD 407824

[Synonym ]:
MFCD09753286

Biological Activity

[Description]:

PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Wee1

[Target]

Chk1:47 nM (IC50)

WEE1:97 nM (IC50)

[In Vitro]

PD 407824 is sufficient to block CHK1, leading to a significant down-regulation of p21, causing activation of CDK8/9, which in turn causes depletion of SMAD2/3[1]. PD 407824 is selective for Chk1 and WEE1 over PKC and Cdk4 with IC50s of 3.4 µM and 3.75 µM, respectively[3].

[References]

[1]. Palmer BD, et al. 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. J Med Chem. 2006 Aug 10;49(16):4896-911.

[2]. Feng L, et al. Discovery of a Small-Molecule BMP Sensitizer for Human Embryonic Stem Cell Differentiation. Cell Rep. 2016 May 31;15(9):2063-75.

[3]. Smaill JB, et al. Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpointkinases. Eur J Med Chem. 2008 Jun;43(6):1276-96. Epub 2007 Aug 6.

Chemical & Physical Properties

[ Density]:
1.507g/cm3

[ Molecular Formula ]:
C₂₀H₁₂N₂O₃

[ Molecular Weight ]:
328.32100

[ Exact Mass ]:
328.08500

[ PSA ]:
85.95000

[ LogP ]:
3.33320

[ Index of Refraction ]:
1.81

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport