Home Epigenetics Histone Methyltransferase inhibitor MI-136

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MI-136 Histone Methyltransferase inhibitor

Cat.No.S7815

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

Chemical Structure

Molecular Weight: 470.51

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 470.51 Formula

C23H21F3N6S

 Storage (From the date of receipt)
CAS No. 1628316-74-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1NC2=C3C=C(SC3=NC=N2)CC(F)(F)F)CC4=CC5=C(C=C4)NC(=C5)C#N

Mechanism of Action

Targets/IC50/Ki
Menin-MLL interaction
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 this compound. Treatment with this chemical also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with this compound 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 this inhibitor on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer.
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.
References

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