2. Epigenetics TGF-beta/Smad
  3. PKC
  4. MS-553

MS-553 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.

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MS-553

MS-553 Chemical Structure

CAS No. : 1046787-18-1

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
50 mg En stock
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500 mg   Obtenir un devis  

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MS-553 Related Antibodies

Top Publications Citing Use of Products

Voir tous les produits spécifiques à Isoform PKC:

Voir toutes les isoformes
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

  • Activité biologique

  • Protocole

  • Pureté et documentation

  • Références

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Description

MS-553 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

MS-553 (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.

MS-553 Related Antibodies
In Vivo

MS-553 (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.
Essai clinique
Masse moléculaire

500.61

Formule

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 200 mg/mL (399.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
Références
Administration animale
[1]

Rats[1]
MS-553 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. MS-553 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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références

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
50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
60 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8323 mL
80 mM 0.0250 mL 0.1248 mL 0.2497 mL 0.6242 mL
100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4994 mL
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MS-553 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:

MS-5531046787-18-1MS553MS 553PKCProtein kinase CInhibitorinhibitorinhibit

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