Home Epigenetics Histone Methyltransferase inhibitor - MLL inhibitor MI-136 For research use only.

MI-136

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

MI-136 Chemical Structure

MI-136 Chemical Structure

CAS No. 1628316-74-4

Purity & Quality Control

Batch: S781501 DMSO]94 mg/mL]false]Ethanol]94 mg/mL]false]Water]Insoluble]false Purity: 99.91%
99.91

MI-136 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models VCaP tumor-bearing mice（VCaP xenografts）
Dosages 40 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 470.51 Formula

C23H21F3N6S
CAS No. 1628316-74-4 SDF Download MI-136 SDF
Smiles C1CN(CCC1NC2=C3C=C(SC3=NC=N2)CC(F)(F)F)CC4=CC5=C(C=C4)NC(=C5)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble


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In vivo
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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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