AS2521780


Catalog No. Size PriceQuantity
M20009-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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

Product information

CAS Number: 1214726-89-2

Molecular Weight: 547.76

Formula: C30H41N7OS

Chemical Name: 2-({[2-(methylsulfanyl)pyridin-3-yl]methyl}amino)-4-({[(1s,3R,5S,7s)-4-({[(1r,4r)-4-hydroxycyclohexyl]methyl}amino)adamantan-1-yl]methyl}amino)pyrimidine-5-carbonitrile

Smiles: CSC1N=CC=CC=1CNC1=NC=C(C#N)C(NC[C@]23C[C@@H]4C[C@H](C2)C(NC[C@@H]2CC[C@@H](O)CC2)[C@@H](C4)C3)=N1

InChiKey: YMYFRDZTZVZUPF-FLHLMAANSA-N

InChi: InChI=1S/C30H41N7OS/c1-39-28-21(3-2-8-32-28)16-34-29-35-17-24(14-31)27(37-29)36-18-30-11-20-9-22(12-30)26(23(10-20)13-30)33-15-19-4-6-25(38)7-5-19/h2-3,8,17,19-20,22-23,25-26,33,38H,4-7,9-13,15-16,18H2,1H3,(H2,34,35,36,37)/t19-,20-,22-,23+,25-,26?,30-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

In Vivo:

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

Products are for research use only. Not for human use.

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