AS2521780

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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

CAS No. : 1214726-89-2

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1 Publications Citing Use of MCE AS2521780

•Cell Cycle. 2021 Feb 22;1-11. [Abstract]

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•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

View All Isoforms

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

Biological Activity
Protocol
Purity & Documentation
References
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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)

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	10 nM Compound: 34	Inhibition of PKCtheta in human Jurkat cells assessed as reduction in IL2 production after 14 hrs by luciferase reporter gene assay Inhibition of PKCtheta in human Jurkat cells assessed as reduction in IL2 production after 14 hrs by luciferase reporter gene assay	[PMID: 30704835]

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.

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.

1214726-89-2

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

Handling Instructions (2659 KB)

References

[1]. Fukahori H, et al. Effect of AS2521780, a novel PKCθ selective inhibitor, on T cell-mediated immunity. Eur J Pharmacol. 2014 Dec 15;745:217-22. [Content Brief]

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	[1]. Fukahori H, et al. Effect of AS2521780, a novel PKCθ selective inhibitor, on T cell-mediated immunity. Eur J Pharmacol. 2014 Dec 15;745:217-22. [Content Brief]

AS2521780 Related Classifications

Inflammation/Immunology

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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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