MI-2 (hydrochloride) |
| Catalog No.GC10388 |
menin-MLL interaction inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with an IC50 value of 446 ± 28 nM.
Menin is an oncogenic cofactor in leukemic transformations which could bind to the N-terminal fragment of MLL existed in all MLL fusion proteins. Menin is a highly specific and direct binding partner of MLL and MLL fusion proteins which is essential for regulation of their target genes. Disruption of the menin-MLL protein interaction abrogates oncogenic properties of MLL fusion proteins and blocks the development of acute leukemia [2].
In vitro: In HEK293 cells, MI-2 accessed the protein target menin-MLL and effectively inhibited the menin-MLL-AF9 interaction. MI-2 effectively blocked cell proliferation, and induced cell apoptosis in human MLL leukemia cell lines harboring different MLL translocations MLL-AF9 and MLL-ENL, with the GI50 value of about 5 μM for MI-2. MI-2 showed little effect on the cell growth of E2A-HLF transduced BMC with the GI50 of > 50 μM. MI-2 specifically reduced the immortalization potential of cells transformed with MLL fusion oncoproteins by downregulating the expression of target genes required for MLL fusion protein oncogenic activity [1].
In vivo: After 7 days treatment with MI-2, MLL-AF9 transformed BMC showed great morphology changes and the expression of CD11b was greatly increased [1].
References:
[1]. Grembecka J, He S, Shi A, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia[J]. Nature chemical biology, 2012, 8(3): 277-284.
[2]. Borkin D, He S, Miao H, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo[J]. Cancer Cell, 2015, 27(4): 589-602.
| Cas No. | SDF | ||
| Chemical Name | 4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine, dihydrochloride | ||
| Canonical SMILES | CCCC(S1)=CC(C1=NC=N2)=C2N3CCN(C4=NCC(C)(C)S4)CC3.Cl.Cl | ||
| Formula | C18H25N5S2 • 2HCl | M.Wt | 448.5 |
| Solubility | ≤30mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2297 mL | 11.1483 mL | 22.2965 mL |
| 5 mM | 0.4459 mL | 2.2297 mL | 4.4593 mL |
| 10 mM | 0.223 mL | 1.1148 mL | 2.2297 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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