PKC-IN-4

Names

[ CAS No. ]:
2636771-29-2

[ Name ]:
PKC-IN-4

Biological Activity

[Description]:

PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC
Research Areas >> Inflammation/Immunology
Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

PKC:0.52 μM (IC50)


[In Vitro]

PKC-IN-4 (compound 7l) shows VEGF - induced endothelial permeability with an EC50 of 0.071 µM[1].

[In Vivo]

PKC-IN-4 (10 mg/kg for i.v.; 20 mg/kg for p.o.) shows orally active with oral bioavailability of 81.7%[1]. Animal Model: Animal Model: CD-1 mice[1] Dosage: 10, 20 mg/kg Administration: 10 mg/kg for i.v.; 20 mg/kg for p.o. Result: Showed good PK parameters with oral bioavailability of 81.7%.

[References]

[1]. Liu X, et al. Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidines as atypical protein kinase C inhibitors to control retinal vascular permeability and cytokine-induced edema. Bioorg Med Chem. 2020 Jun 1;28(11):115480.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H25N5S

[ Molecular Weight ]:
379.52

Related Compounds