MI-136

Catalog No.S7815

MI-136 Chemical Structure

Molecular Weight(MW): 470.51

MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.

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Biological Activity

Description MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.
Targets
Menin-MLL interaction [1]
()
In vitro

MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage and blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer[1].

In vivo Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: VCaP cells
  • Concentrations: 5 μM
  • Incubation Time: 48 h
  • Method:

    To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM MI-136 for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and MI-136 for 48 hrs. Cells are then stimulated with 10nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: VCaP tumor-bearing mice(VCaP xenografts)
  • Formulation: 15% DMSO or 25% PEG + PBS
  • Dosages: 40 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (199.78 mM)
Ethanol 94 mg/mL (199.78 mM)
Water 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.

Chemical Information

Molecular Weight 470.51
Formula

C23H21F3N6S

CAS No. 1628316-74-4
Storage powder
Synonyms N/A

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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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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID