NIK SMI1

NIK SMI1 is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM for NIK-catalyzed hydrolysis of ATP to ADP.

Product information

CAS Number: 1660114-31-7

Molecular Weight: 365.38

Formula: C20H19N3O4

Chemical Name: (R)-6-(3-((3-Hydroxy-1-methyl-2-oxopyrrolidin-3-yl)ethynyl)phenyl)-4-methoxypicolinamide

Smiles: COC1=CC(=NC(=C1)C1=CC(=CC=C1)C#C[C@]1(O)CCN(C)C1=O)C(N)=O

InChiKey: LQSHXYHWYGKAMX-FQEVSTJZSA-N

InChi: InChI=1S/C20H19N3O4/c1-23-9-8-20(26,19(23)25)7-6-13-4-3-5-14(10-13)16-11-15(27-2)12-17(22-16)18(21)24/h3-5,10-12,26H,8-9H2,1-2H3,(H2,21,24)/t20-/m0/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO 73 mg/mL (199.79 mM)

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:

NIK SMI1 exhibits selective inhibition of LTβR-dependent p52 translocation and transcription of NF-κB2 related genes. NIK SMI1 is shown to have a favorable pharmacokinetic profile across species and to inhibit BAFF-induced B cell survival in vitro.

In Vivo:

NIK SMI1 inhibits BAFF signaling and reduces splenic marginal zone B cells in vivo.

References:

1. Blaquiere N, et al. J Med Chem. 2018 Aug 9;61(15):6801-6813.

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