NIBR3049

NIBR3049, also known as TCS-21311, is a potent and selective JAK3 inhibitor IC50 values of 8 nM..

Product information

CAS Number: 1260181-14-3

Molecular Weight: 526.51

Formula: C27H25F3N4O4

Synonym:

TCS-21311

Chemical Name:  3-[5-[4-(2-Hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

Smiles: CC(C)(O)C(=O)N1CCN(CC1)C1=CC(C2=C(C3=CNC4=CC=CC=C43)C(=O)NC2=O)=C(C=C1)C(F)(F)F

InChiKey: CLGRAWDGLMENOD-UHFFFAOYSA-N

InChi: InChI=1S/C27H25F3N4O4/c1-26(2,38)25(37)34-11-9-33(10-12-34)15-7-8-19(27(28,29)30)17(13-15)21-22(24(36)32-23(21)35)18-14-31-20-6-4-3-5-16(18)20/h3-8,13-14,31,38H,9-12H2,1-2H3,(H,32,35,36)

Technical Data

Appearance: Solid Power.

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

Solubility: Soluble in DMSO

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:

NIBR3049 exhibits IC50 values of 1.017, 2.550 and 8.055 μM for JAK1, JAK2 and TYK2, respectively in a enzymatic Jak assay. NIBR3049 shows moderate activity in this cellular assay (IC50=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity.

References:

1. Thoma G, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.J Med Chem. 2011 Jan 13;54(1):284-8.

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