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NIK SMI1 is an effective and selective NF-κB inducing kinase (NIK) inhibitor. It also inhibits NIK-catalyzed hydrolysis of ATP to ADP (IC50: 0.23±0.17 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $163 | In Stock | |
5 mg | $413 | In Stock | |
10 mg | $618 | In Stock | |
25 mg | $985 | In Stock | |
50 mg | $1,330 | In Stock | |
100 mg | $1,790 | In Stock | |
1 mL x 10 mM (in DMSO) | $455 | In Stock |
Description | NIK SMI1 is an effective and selective NF-κB inducing kinase (NIK) inhibitor. It also inhibits NIK-catalyzed hydrolysis of ATP to ADP (IC50: 0.23±0.17 nM). |
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). |
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 . |
Molecular Weight | 365.38 |
Formula | C20H19N3O4 |
Cas No. | 1660114-31-7 |
Smiles | COc1cc(nc(c1)-c1cccc(c1)C#C[C@]1(O)CCN(C)C1=O)C(N)=O |
Relative Density. | 1.39 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (273.69 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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