2. Epigenetics TGF-beta/Smad
  3. PKC
  4. 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.

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PKC-IN-4 Chemical Structure

PKC-IN-4 Chemical Structure

CAS No. : 2636771-29-2

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PKC-IN-4 Related Antibodies

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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].

IC50 & Target[1]

PKC

0.52 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
6.65 μM
Compound: 7l
Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells preincubated for 2 hrs followed by TNFalpha stimulation by luciferase assay
Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells preincubated for 2 hrs followed by TNFalpha stimulation by luciferase assay
[PMID: 32327351]
In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PKC-IN-4 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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%.
Molecular Weight

379.52

Formula

C21H25N5S
CAS No.
SMILES

NCC1CCN(CC1)C2=NC(C3=CC=NC=C3)=NC4=C2C5=C(S4)CCCC5
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PKC-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKC-IN-42636771-29-2PKCProtein kinase Cretinal vasculatureVEGFTNFαNF-κBCD-1 miceorally activeBREC cellsInhibitorinhibitorinhibit

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