1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. PKC-IN-1

PKC-IN-1 

Cat. No.: HY-16903 Purity: 99.94%
Handling Instructions

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.

For research use only. We do not sell to patients.

PKC-IN-1 Chemical Structure

PKC-IN-1 Chemical Structure

CAS No. : 1046787-18-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 463 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 463 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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)[1]
Ki: 5.3 nM (Human PKCβ), 10.4 nM (Human PKCα)[1]

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[1].

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

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[1].

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

Molecular Weight

500.61

Formula

C₂₅H₃₇FN₈O₂

CAS No.
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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (49.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9976 mL 9.9878 mL 19.9756 mL
5 mM 0.3995 mL 1.9976 mL 3.9951 mL
10 mM 0.1998 mL 0.9988 mL 1.9976 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
PKC-IN-1 is tested in the experimental autoimmune encephalitis (EAE) model in Lewis rats. EAE is induced by MBP69-88/CFA immunization and pertussis toxin injection in Lewis rats. PKC-IN-1 is prepared as an oral suspension and dosed orally, twice per day (BID) at three doses, 7.5 and 15 and 30 mg/kg for total daily doses of 15, 30 and 60 mg/kg. The efficacy is compared to animals that receive the positive control FTY720 dosed once per day at a dose of 0.5 mg/kg. The treatment starts on Day 8, when 48% of the rats have signs of EAE[1].

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

References
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PKC-IN-1
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HY-16903
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