1. Epigenetics
    Others
    Apoptosis
  2. Epigenetic Reader Domain
    Androgen Receptor
    Apoptosis
  3. MI-136

MI-136 

Cat. No.: HY-19319 Purity: 98.64%
Handling Instructions

MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.

For research use only. We do not sell to patients.

MI-136 Chemical Structure

MI-136 Chemical Structure

CAS No. : 1628316-74-4

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 116 In-stock
Estimated Time of Arrival: December 31
5 mg USD 105 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1125 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors[1][2].

In Vitro

MI-136 (0-20) exhibits IC50values of 5.59 μM, 7.15 μM, 5.37 μM and 19.76 μM in LNCaP, VCaP, 22rv1 and PNT2 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: AR positive cell lines such as VCaP, LNCaP and 22RV1.
Concentration: 0-20 μM.
Incubation Time: 24 h.
Result: Inhibited cell proliferation.
In Vivo

MI-136 exhibits T1/2 of 3.1 h after po administration[1].
MI-136 (40 mg/kg, ip) leads to a significant decrease in the growth of castration-resistant VCaP tumors[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: VCaP xenografts[2].
Dosage: 40 mg/kg.
Administration: Intraperitoneal injection, 5 days a week.
Result: Led to a significant decrease in the growth of castration-resistant VCaP tumors compared to vehicle controls.
Molecular Weight

470.51

Formula

C₂₃H₂₁F₃N₆S

CAS No.

1628316-74-4

SMILES

FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (233.79 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.84 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (5.84 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (5.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MI-136MI136MI 136Epigenetic Reader DomainAndrogen ReceptorApoptosisPPIcastrationresistantprostatecancerCRPCInhibitorinhibitorinhibit

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Product Name:
MI-136
Cat. No.:
HY-19319
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