2636771-29-2

2636771-29-2 structure

Name: PKC-IN-4
Chemical Name: PKC-IN-4
CAS Number: 2636771-29-2
Molecular Formula: C₂₁H₂₅N₅S
Molecular Weight: 379.52
Catalog: Signaling Pathways Epigenetics PKC
Create Date: 2022-08-18 00:54:39
Modify Date: 2024-09-09 19:25:34
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].

Name	PKC-IN-4

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.

Molecular Formula	C₂₁H₂₅N₅S
Molecular Weight	379.52