NIK SMI1

This product is for research use only, not for human use. We do not sell to patients.

NIK SMI1
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Size Price Stock
100mg$2350Check With Us
200mg$3525Check With Us
500mg$5950Check With Us

Cat #: V26503 CAS #: 1660114-31-7 Purity ≥ 99%

Description: NIK SMI1 (NIK-SMI1) is a novel, highly selective and potent inhibitor of NF-κB-inducing kinase (NIK).

References: Blaquiere N, et al. Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase. J Med Chem. 2018 Aug 9;61(15):6801-6813.

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Molecular Weight (MW)365.38
Molecular FormulaC20H19N3O4
CAS No.1660114-31-7
SMILES CodeO=C(N)C1=NC(C2=CC=CC(C#C[C@@]3(O)C(N(C)CC3)=O)=C2)=CC(OC)=C1
SynonymsNIK SMI1; NIKSMI1; NIK-SMI1;
ProtocolIn VitroNIK SMI1 (Compound 4f) inhibits NIK-catalyzed hydrolysis of ATP to ADP (fluorescence polarization, FP) with an IC50 of 0.23±0.17 nM. NIK SMI1 inhibits the expression of NIK SMI1 response elementregulated firefly luciferase reporter gene in HEK293 cells with an IC50 of 34±6 nM. Consistent with expectations for a NIK inhibitor, NIK SMI1 is shown to inhibit nuclear translocation of p52 (RelB) (IC50=70 nM). NIK SMI1 inhibits BAFF-induced B cell (mouse) survival in vitro with an IC50 of 373±64 nM.
In VivoC57BL/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. The nonlinearity of exposure relative to dose between 100 and 200 mg/kg is a result of saturation of clearance mechanisms. 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. Volume of distribution (Vd, L/kg) is 1.35, 1.58, 0.778, and 1.39, respectively.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.7369 mL13.6844 mL27.3688 mL54.7375 mL
5mM0.5474 mL2.7369 mL5.4738 mL10.9475 mL
10mM0.2737 mL1.3684 mL2.7369 mL5.4738 mL
20mM0.1368 mL0.6842 mL1.3684 mL2.7369 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
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Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.