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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $39 | In Stock | |
2 mg | $57 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $150 | In Stock | |
25 mg | $293 | In Stock | |
50 mg | $531 | In Stock | |
100 mg | $768 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
Description | MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced. |
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]. |
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. |
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) |
Molecular Weight | 470.51 |
Formula | C23H21F3N6S |
Cas No. | 1628316-74-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 87 mg/mL (184.9 mM) DMSO: 87 mg/mL (184.9 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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