Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 2,140.00 | |
50 mg | 6-8 weeks | $ 2,785.00 | |
100 mg | 6-8 weeks | $ 3,520.00 |
Description | PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1] |
In vitro | PKC-IN-4 (compound 7l) shows VEGF - induced endothelial permeability with an EC 50 of 0.071 μM [1]. |
In vivo | PKC-IN-4, administered at doses of 10 mg/kg intravenously (i.v.) and 20 mg/kg orally (p.o.), demonstrates oral activity with an oral bioavailability of 81.7% in CD-1 mice. This compound, when tested, exhibited favorable pharmacokinetic (PK) parameters, substantiating its effectiveness and potential for further development. |
Molecular Weight | 379.52 |
Formula | C21H25N5S |
CAS No. | 2636771-29-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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PKC-IN-4 2636771-29-2 inhibitor inhibit