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

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 463 In-stock
Solution
10 mM * 1 mL in DMSO USD 463 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
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Based on 1 publication(s) in Google Scholar

PKC-IN-1 Related Antibodies

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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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[1]

Human PKCα

2.3 nM (IC50)

Human PKCβII

7.6 nM (IC50)

Human PKCβI

8.1 nM (IC50)

Human PKCθ

25.6 nM (IC50)

Human PKCγ

57.5 nM (IC50)

Human PKC mu

314 nM (IC50)

Human PKCε

808 nM (IC50)

Human PKCβ

5.3 nM (Ki)

Human PKCα

10.4 nM (Ki)

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].

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

PKC-IN-1 Related Antibodies
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].

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

500.61

Formula

C25H37FN8O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (49.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9976 mL 9.9878 mL 19.9756 mL 49.9391 mL
5 mM 0.3995 mL 1.9976 mL 3.9951 mL 9.9878 mL
10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9939 mL
15 mM 0.1332 mL 0.6659 mL 1.3317 mL 3.3293 mL
20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4970 mL
25 mM 0.0799 mL 0.3995 mL 0.7990 mL 1.9976 mL
30 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6646 mL
40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
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PKC-IN-1 Related Classifications

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-11046787-18-1PKCProtein kinase CInhibitorinhibitorinhibit

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