NIK SMI1

SKU: orb1307970

Description

NIK SMI1 is a potent and selective inhibitor of NF-κB inducing kinase (NIK), effectively blocking its ATPase activity with an IC50 of 0.23±0.17 nM. This small molecule is a valuable research tool for studying the non-canonical NF-κB pathway in both cellular and animal models of inflammation and oncology.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1660114-31-7
• MW: 365.38
• Purity: 99.99% (May vary between batches)
• Formula: C₂₀H₁₉N₃O₄
• SMILES: COc1cc(nc(c1)-c1cccc(c1)C#C[C@]1(O)CCN(C)C1=O)C(N)=O
• Target: NF-κB
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.95 mM);DMSO:100 mg/mL (273.69 mM)

Bioactivity

• In Vivo:
  The pharmacology of NIK SMI1 is examined in SD rat, CD-1 mouse, beagle, and cynomologous monkey with 20, 32, 18, and 7.8 mL/kg per min, respectively. The volume of distribution (Vd, L/kg) is 1.35, 1.58, 0.778, and 1.39, respectively. C57BL/6 mice are treated twice daily for 7 days with orally administered NIK SMI1 or with three injections of recombinant BAFF receptor fusion protein (Br3- mIgG2a) over the course of the 7-day experiment as a positive control .
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• In Vitro:
  NIK SMI1 inhibits the expression of NIK SMI1 response element regulated firefly luciferase reporter gene in HEK293 cells (IC50: 34±6 nM). NIK SMI1 inhibits BAFF-induced B cell (mouse) survival in vitro with an IC50 of 373±64 nM. Consistent with expectations for a NIK inhibitor, NIK SMI1 is shown to inhibit nuclear translocation of p52 (RelB) (IC50=70 nM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, NIK, NIK SMI 1, NIK SMI1, NIK SMI-1, NFkB, NF-kB, NF-κB, NFκB, Nuclear factor-κB, Nuclear factor-kappaB, Inhibitor

Compound Identifiers

PubChem CID

117902000