1. Epigenetics
    TGF-beta/Smad
  2. PKC

AS2521780 

Cat. No.: HY-12663
Handling Instructions

AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.

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

AS2521780 Chemical Structure

AS2521780 Chemical Structure

CAS No. : 1214726-89-2

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.

IC50 & Target[1]

PKCθ

0.48 nM (IC50)

PKCε

18 nM (IC50)

PKCα

160 nM (IC50)

PKCδ

160 nM (IC50)

In Vitro

AS2521780 exerts potent inhibition of recombinant human PKCθ enzyme activity (IC50=0.48 nM), which is more than 30-fold higher than that of other PKC isoforms. Further, AS2521780 exerts little or no inhibition on other protein kinases. AS2521780 suppresses CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and proliferation of human primary T cells. AS2521780 also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey peripheral blood mononuclear cells with similar potency[1].

In Vivo

AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8256 mL 9.1281 mL 18.2562 mL
5 mM 0.3651 mL 1.8256 mL 3.6512 mL
10 mM 0.1826 mL 0.9128 mL 1.8256 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Human peripheral T cells are incubated with AS2521780 and anti-human CD28 (0.5 μg/mL). After 48 h incubation, cell proliferation is detected using a CellTiter-Glo Luminescent Cell Viability Assay[1].

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

Animal Administration
[1]

AS2521780 or vehicle is orally administered twice daily from Day 1 to 24. On Day 25, the left hind paw of each rat is dissected above the ankle joint and fixed in 10% neutral buffered formalin. After decalcification, the paws are embedded in paraffin, sectioned longitudinally and stained with hematoxylin and eosin[1].

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

References
Molecular Weight

547.76

Formula

C₃₀H₄₁N₇OS

CAS No.

1214726-89-2

SMILES

CSC1=C(CNC2=NC=C(C#N)C(NC[[email protected]@]3(C[[email protected]@H](C4)C5NC[[email protected]]6CC[[email protected]](O)CC6)C[[email protected]]4C[[email protected]]5C3)=N2)C=CC=N1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AS2521780
Cat. No.:
HY-12663
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AS2521780

Cat. No.: HY-12663