1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
  3. aPKC-IN-2

aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitory activity, providing the possibility for further development of small molecule aPKC inhibitors.

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aPKC-IN-2 Chemical Structure

aPKC-IN-2 Chemical Structure

CAS No. : 15854-08-7

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Description

aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitory activity, providing the possibility for further development of small molecule aPKC inhibitors[1].

Molecular Weight

261.34

Formula

C14H15NO2S

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(SC=C1C2=CC=C(C=C2)C)N)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (239.15 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 3.8264 mL 19.1322 mL 38.2643 mL
5 mM 0.7653 mL 3.8264 mL 7.6529 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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
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Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8264 mL 19.1322 mL 38.2643 mL 95.6608 mL
5 mM 0.7653 mL 3.8264 mL 7.6529 mL 19.1322 mL
10 mM 0.3826 mL 1.9132 mL 3.8264 mL 9.5661 mL
15 mM 0.2551 mL 1.2755 mL 2.5510 mL 6.3774 mL
20 mM 0.1913 mL 0.9566 mL 1.9132 mL 4.7830 mL
25 mM 0.1531 mL 0.7653 mL 1.5306 mL 3.8264 mL
30 mM 0.1275 mL 0.6377 mL 1.2755 mL 3.1887 mL
40 mM 0.0957 mL 0.4783 mL 0.9566 mL 2.3915 mL
50 mM 0.0765 mL 0.3826 mL 0.7653 mL 1.9132 mL
60 mM 0.0638 mL 0.3189 mL 0.6377 mL 1.5943 mL
80 mM 0.0478 mL 0.2392 mL 0.4783 mL 1.1958 mL
100 mM 0.0383 mL 0.1913 mL 0.3826 mL 0.9566 mL
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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.

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Product Name:
aPKC-IN-2
Cat. No.:
HY-W030338
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