PKC-IN-4

Modify Date: 2023-01-14 16:58:47

PKC-IN-4 Structure
PKC-IN-4 structure
Common Name PKC-IN-4
CAS Number 2636771-29-2 Molecular Weight 379.52
Density N/A Boiling Point N/A
Molecular Formula C21H25N5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PKC-IN-4


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].

 Names

Name PKC-IN-4

 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
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