PKC-IN-1


Catalog No. size PriceQuantity
M6811-2 2mg solid $180
M6811-10 10mg solid $716

Description

Cas: 1046787-18-1

Product Information

PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

 

IC50 & Target

IC50: 2.3 nM (Human PKCα), 7.6 nM (Human PKCβII), 8.1 nM (Human PKCβI), 25.6 nM (Human PKCθ), 57.5 nM (Human PKCγ), 314 nM (Human PKC mu), 808 nM (Human PKCε)

Ki: 5.3 nM (Human PKCβ), 10.4 nM (Human PKCα)

 

Molecular Weight:500.61

 

Chemical Formula: C₂₅H₃₇FN₈O₂

 

Smiles Code:

 

O=C(N1[C@@H](C)CN(CC2CCOCC2)[C@H](C)C1)N(C3)C(C)(C)C4=C3C(NC5=NC(C)=NC=C5F)=NN4

 

Shipping:

 

Room temperature in continental US; may vary elsewhere.

 

Storage:

Powder    -20°C   3 years

4°C   2 years

In solvent -80°C   6 months

-20°C   1 month

 

 

In Vitro:

PKC-IN-1 (Compound A) is a potent, ATP-competitive and reversible of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

 

In Vivo

PKC-IN-1 (Compound A; 15 and 30 mg/kg, p.o., bid (twice a day)) dose-dependently and significantly reduces maximum EAE severity and end severity in autoimmune encephalitis (EAE) model in Lewis rats.

 

 

References

 

  1. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1.

 

Products are for research use only. Not for human use.

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