MLN120B

Catalog No.S7736 Batch:S773601

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Technical Data

Formula

C19H15ClN4O2
Molecular Weight 366.80 CAS No. 783348-36-7
Solubility (25°C)* In vitro DMSO 73 mg/mL (199.01 mM)
Ethanol 5 mg/mL (13.63 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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>
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>

Protocol (from reference)

Cell Assay:

[2]
  • 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. 
Animal Study:

[2]
  • Animal Models

    NF-kB2-luc2 transfected mice

  • Dosages

    300 mg/kg

  • Administration

    p.o.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.