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PF-4950834

Names

[ CAS No. ]:
1256264-62-6

[ Name ]:
PF-4950834

[Synonym ]:
unii-4a0by63lar
PF-4950834

Biological Activity

[Description]:

PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC
Signaling Pathways >> Metabolic Enzyme/Protease >> SGK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA
Signaling Pathways >> Stem Cell/Wnt >> PKA
Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Stem Cell/Wnt >> ROCK
Signaling Pathways >> TGF-beta/Smad >> PKC
Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

ROCK2:8.35 nM (IC50)

ROCK1:33.12 nM (IC50)

PKCη:756 nM (IC50)

PKA:424 nM (IC50)


[In Vitro]

PF-4950834 shows inhibition against the AGC (cAMP-dependent protein kinase/protein kinase G/protein kinase C) kinase family with IC50 values of 8.35, 33.12, 102, 216, 321, 384, 411, 424, 457, 578, 736, 756 and 2900 nM for ROCK2, ROCK1, PRKG1, PKN1, SGK2, PRKG2, MSK1, PKA, PRKX, MSK2, P70S6K, PKCη and SGK1, respectively[1].

[References]

[1]. Rajagopalan LE, et al. Biochemical, cellular, and anti-inflammatory properties of a potent, selective, orally bioavailable benzamide inhibitor of Rho kinase activity. J Pharmacol Exp Ther. 2010 Jun;333(3):707-16.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H19N3O2

[ Molecular Weight ]:
345.39

[ Exact Mass ]:
345.14800

[ PSA ]:
74.58000

[ LogP ]:
4.00390

Related Compounds