An inhibitor of menin-MLL fusion protein interactions
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Isomer(s)
27214MI-3
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Transcription Factors

MI-2

Item No. 29218

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-propyl-thieno[2,3-d]pyrimidine
CAS Number
1271738-62-5
Molecular Formula
C18H25N5S2
Formula Weight
375.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
223, 287 nm
SMILES
CCCC(S1)=CC(C1=NC=N2)=C2N3CCN(C4=NCC(C)(C)S4)CC3
InChi Code
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
InChi Key
SRQYLNYQAPCPIR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    MI-2 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 446 nM).1 It binds to menin (Kd = 158 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. MI-2 inhibits the growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL-AF9 (GI50 = 5 μM). It also inhibits the growth of MV4, KOPN-8, ML-2, and MonoMac6 MLL cells expressing MLL fusion proteins (GI50s = 9.5, 7.2, 8.7, and 18 μM, respectively), as well as induces hematopoietic differentiation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grembecka, J., He, S., Shi, A., et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nat. Chem. Biol. 8(3), 277-284 (2012).