PS-432

Names

[ CAS No. ]:
2083630-26-4

[ Name ]:
PS-432

[Synonym ]:
1H-Pyrrole-3-carboxylic acid, 2-[5-(4-chlorophenyl)-2-furanyl]-2,5-dihydro-4-hydroxy-1-(6-methyl-2-benzothiazolyl)-5-oxo-, ethyl ester
2-[5-(4-chlorophenyl)-2-furanyl]-2,5-dihydro-4-hydroxy-1-(6-methyl-2-benzothiazolyl)-5-oxo-1H-pyrrole-3-carboxylic acid ethyl ester
PS432
Ethyl 2-[5-(4-chlorophenyl)-2-furyl]-4-hydroxy-1-(6-methyl-1,3-benzothiazol-2-yl)-5-oxo-2,5-dihydro-1H-pyrrole-3-carboxylate

Biological Activity

[Description]:

PS-432 is an allosteric inhibitor of PKCι and PKCζ with IC50 of 16.9 and 18.5 uM, respectively; has no inhibitory activity against PKCα, PKCβ, PKCδ and PKCθ nor the activity of related kinases such as PDK1, PKB/Akt, RSK1, MSK1 and Aurora A; inhibits the proliferation of the lung cancer cell lines A549 (IC50=14.8 ± 4.2 uM) and A427 (IC50=10.4± 0.3 uM) as well as androgen-independent prostate cancer cell line DU145 (IC50 = 20.8 ± 9.0 uM); well tolerated in vivo.

[References]

References 1. Arencibia JM, et al. ACS Chem Biol. 2017 Feb 17;12(2):564-573. View Related Products by Target PKC

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
662.5±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₅H₁₉ClN₂O₅S

[ Molecular Weight ]:
494.947

[ Flash Point ]:
354.5±34.3 °C

[ Exact Mass ]:
494.070313

[ LogP ]:
5.81

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.686

Related Compounds

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