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MI-2

Cat. No. M9145
MI-2 Structure
Synonym:

Menin-MLL Inhibitor 2

Size Price Availability Quantity
10mg USD 220  USD220 In stock
25mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

MI-2 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM. In HEK293 cells, MI-2 accessed the protein target and effectively inhibits the menin-MLL-AF9 interaction. MI-2 effectively blocks MLL fusion protein-mediated leukemic transformation by downregulating the expression of target genes required for MLL fusion protein oncogenic activity. MI-2 also effectively blocks cell proliferation, and induces cell apoptosis in human MLL leukemia cell lines harboring different MLL translocations.

Chemical Information
Molecular Weight 375.55
Formula C18H25N5S2
CAS Number 1271738-62-5
Solubility (25°C) DMSO: ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Grembecka J, et al. Nat Chem Biol. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia.

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Keywords: MI-2, Menin-MLL Inhibitor 2 supplier, Histone Methyltransferase, inhibitors, activators


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