2. Epigenetics TGF-beta/Smad
  3. PKC
  4. AS2521780

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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AS2521780 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AS2521780

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View All Isoforms
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

AS2521780 Related Antibodies
In Vivo

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

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

547.76

Formula

C30H41N7OS
CAS No.
SMILES

N#CC1=CN=C(NCC2=CC=CN=C2SC)N=C1NC[C@]34C[C@]5([H])[C@@H](NC[C@H]6CC[C@H](O)CC6)[C@@](C4)([H])CC(C5)C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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
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AS2521780 Related Classifications

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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.

Keywords:

AS25217801214726-89-2AS 2521780AS-2521780PKCProtein kinase CInhibitorinhibitorinhibit

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