NIK-SMI1
Inhibitor of MAP3K14
Structure
In Cells
In Model Organisms
Probe NIK-SMI1 is in the process of SERP review.
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SERP ratings and comments
SERP Ratings
SERP Comments:
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.
- Inhibits expression of NF-κB response element regulated firefly luciferase reporter gene in HEK293 cells at an IC50 of 34 nM.
- has a favorable pharmacokinetic profile across species.
- Inhibits BAFF-induced B cell survival in vitro (close to phenotype assay) at an IC50 of 373 nM.
- Inhibits BAFF signalling and reduces splenic marginal zone B cells in mice at doses from 60-200 mg/kg.
(last updated: 8 Dec 2020 )
SERP Ratings
SERP Comments:
The primary references provide strong support for on target NIK (MAP3K14) potency, efficacy and selectivity within the kinome for NIK SM1. In functional assays ~1 uM in cells and 200 mg/kg BID orally in C57BL/6 mice are recommended based on the data in the provided references. Selectivity profiling outside the kinome for safety pharmacology is not available and this unknown should modulate interpretation of in vivo results if readouts differ from the systems investigated in the references.
(last updated: 2 Mar 2021 )