MI-136

SKU: orb1300373

Description

MI-136 is a small molecule inhibitor that suppresses the expression of androgen receptor (AR) target genes induced by dihydrotestosterone (DHT). It is a research tool for investigating AR signaling in prostate cancer models, applicable in both in vitro and in vivo experimental settings.

Research Area

Cell Biology, Epigenetics & Chromatin, Metabolism Research

Key Properties

• CAS Number: 1628316-74-4
• MW: 470.51
• Purity: >99.99% (May vary between batches)
• Formula: C₂₃H₂₁F₃N₆S
• SMILES: FC(F)(F)Cc1cc2c(NC3CCN(Cc4ccc5[nH]c(cc5c4)C#N)CC3)ncnc2s1
• Target: Apoptosis,Epigenetic Reader Domain,Androgen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.01 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:87 mg/mL (184.91 mM);DMSO:150 mg/mL (318.8 mM)

Bioactivity

• In Vivo:
  Treatment of VCaP tumor-bearing mice with MI-136 (40 mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight.
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• 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.
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• Cell Research:
  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 10 nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CRPC, castration, Apoptosis, Androgen Receptor, AndrogenReceptor, cancer, MI 136, MI136, MI-136, inhibit, Inhibitor, Epigenetic Reader Domain, EpigeneticReaderDomain, PPI, prostate, resistant

Compound Identifiers

PubChem CID

86297077