MI-136

Catalog No.S7815

For research use only.

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

MI-136 Chemical Structure

CAS No. 1628316-74-4

Selleck's MI-136 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: VCaP tumor-bearing mice(VCaP xenografts)
  • Dosages: 40 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 94 mg/mL
(199.78 mM)
Ethanol 94 mg/mL
(199.78 mM)
Water Insoluble

Chemical Information

Molecular Weight 470.51
Formula

C23H21F3N6S

CAS No. 1628316-74-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1NC2=C3C=C(SC3=NC=N2)CC(F)(F)F)CC4=CC5=C(C=C4)NC(=C5)C#N

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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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