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Art. -Nr.: HY-147712

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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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CAS. Nr.: 2636771-29-2
Formel: C₂₁H₂₅N₅S
Molecular Weight:379.52

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

PKC-IN-4 Chemical Structure

CAS. Nr.: 2636771-29-2

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PKC

0.52 μM (IC₅₀)

Alle PKC Isoform-spezifische Produkte anzeigen :

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.

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%.

Related Protocols :

Chemical Information

CAS. Nr. 2636771-29-2
Molecular Weight 379.52
Formel C₂₁H₂₅N₅S
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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