MI-2, Menin-MLL Inhibitor

MI-2 is a potent and specific Menin-MLL inhibitor with an IC50 ~446 nM. It specifically binds to Menin and inhibits Menin’s interaction with MLL fusion proteins in cells. It can effectively reverse MLL fusion protein–mediated leukemic transformation by downregulating the expression of target genes downstream of MLL fusion protein oncogenic activity. MI-2 is a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of Menin as an oncogenic cofactor of MLL fusion proteins.

Product information

CAS Number: 1271738-62-5

Molecular Weight: 375.55

Formula: C18H25N5S2

Chemical Name: 4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine

Smiles: CCCC1=CC2=C(N=CN=C2S1)N1CCN(CC1)C1=NCC(C)(C)S1

InChiKey: SRQYLNYQAPCPIR-UHFFFAOYSA-N

InChi: InChI=1S/C18H25N5S2/c1-4-5-13-10-14-15(20-12-21-16(14)24-13)22-6-8-23(9-7-22)17-19-11-18(2,3)25-17/h10,12H,4-9,11H2,1-3H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

MI-2 was used at 10-25 µM concentration in vitro and in the cellular assays.

References:

1. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. (2012) Nat Chem Biol. 8(3):277-84.

Products are for research use only. Not for human use.