MLN120B

Synonyms: ML120B

MLN120B (ML120B) is a potent, selective, reversible, and ATP-competitive inhibitor of IkappaB kinase beta (IKKβ) with an IC50 of 45 nM for recombinant IKKβ. MLN120B does not inhibit other IKK isoforms at IC50 below 50 μM.

MLN120B Chemical Structure

MLN120B Chemical Structure

CAS: 783348-36-7

Purity & Quality Control

Batch: S773601 DMSO] 73 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

Description MLN120B (ML120B) is a potent, selective, reversible, and ATP-competitive inhibitor of IkappaB kinase beta (IKKβ) with an IC50 of 45 nM for recombinant IKKβ. MLN120B does not inhibit other IKK isoforms at IC50 below 50 μM.
Targets
recombinant IKKβ [1]
45 nM
In vitro
In vitro

MLN120B, a anti-inflammatory compound, is a NF-kB pathway blocker of inhibiting IKK2, and shows an inhibitory effect on LPS induced NF-kB activation. The IC50 value of MLN120B is 1.4, 14.8 or 27.3 μM for NF-kB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively, indicating that IKK2 inhibition affects the transcriptional activity of the NF-kB2 promoter most effective.<sup><a class="sref" href="#s_ref">[1]</a></sup><sup><a class="sref" href="#s_ref">[2]</a></sup>

Cell Research Cell lines TNFAIP3-luc2, NF-kB2-luc2 and IL8-luc2 transfected RAW264.7 cells
Concentrations 1-100 µM
Incubation Time --
Method

Transiently transfect the NF-kB reporters into RAW267.4 cells and induce inflammation in the cells with LPS. The effect of these compounds on LPS induced luciferase expression was assayed. 

In Vivo
In vivo

Significantly decreased levels of the pro-inflammatory chemokine MIP-1β and increased levels of the anti-inflammatory cytokine IL-10 were detected in the BAL of MLN120B pre-treated mice as opposed to LPS-treated positive controls.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Animal Research Animal Models NF-kB2-luc2 transfected mice
Dosages 300 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 366.80 Formula

C19H15ClN4O2

CAS No. 783348-36-7 SDF --
Smiles COC1=C(NC(=O)C2=CC=CN=C2C)C3=C(C=C1Cl)C4=C([NH]3)C=NC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 73 mg/mL ( (199.01 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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