[CAS NO. 1628316-74-4] MI-136
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PRODUCTS SPECIFICATIONS [1628316-74-4]
Catalog
SLK-S7815
Brand
Selleck
CAS
1628316-74-4
DESCRIPTION [1628316-74-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 470.51 |
| Molecular Formula | C23H21F3N6S |
| SMILES | N#CC(N1)=CC2=C1C=CC(CN3CCC(NC4=C(C=C(CC(F)(F)F)S5)C5=NC=N4)CC3)=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1254 mL | 10.6268 mL | 21.2535 mL |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2507 mL |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 mL |
| 50 mM | 0.0425 mL | 0.2125 mL | 0.4251 mL |
Description
MI-136 can specifically inhibit the interaction. It inhibits DHT-induced expression of target genes.
Targets
| Menin-MLL interaction [1] |
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.
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.
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