| Name | MI-136 |
| Description | MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced. |
| 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) |
| Kinase Assay | HSP90 binding, ATPase, and selectivity profiling assays: The potency of HSP90 inhibitors for HSP90α, HSP90β, and Grp94 is determined by AlphaScreen competition binding assays, and activity against TRAP-1 is assessed by an ATPase assay. |
| 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 (40 mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.01 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 87 mg/mL (184.91 mM), Sonication is recommended.
DMSO : 150 mg/mL (318.8 mM), Sonication is recommended.
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| Keywords | resistant | prostate | PPI | MI-136 | MI136 | MI 136 | Inhibitor | inhibit | EpigeneticReaderDomain | Epigenetic Reader Domain | CRPC | castration | cancer | Apoptosis | AndrogenReceptor | Androgen Receptor |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Methylation Compound Library | Reprogramming Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Compound Library |
United States
