An inhibitor of menin-MLL fusion protein interactions
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Isomer(s)
29218MI-2 11620MI-2 (hydrochloride)
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Transcription Factors

MI-3

Item No. 27214

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-(1-methylethyl)-thieno[2,3-d]pyrimidine
CAS Number
1271738-59-0
Molecular Formula
C18H25N5S2
Formula Weight
375.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: slightly solubleEthanol: slightly soluble
λmax
224, 288 nm
SMILES
CC(C)C1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1
InChi Code
InChI=1S/C18H25N5S2/c1-12(2)14-9-13-15(20-11-21-16(13)24-14)22-5-7-23(8-6-22)17-19-10-18(3,4)25-17/h9,11-12H,5-8,10H2,1-4H3
InChi Key
FUGQNAUKABUDQI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $41

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    1 mg

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    5 mg

    $255

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    Product Description

    MI-3 is an inhibitor of the interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 648 nM).1 MI-3 binds to menin (Kd = 201 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. It inhibits growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL fusion proteins MLL-AF9 or MLL-ENL (IC50 = 5 µM for both), as well as reduces colony formation and induces differentiation of MLL-AF9-transformed BMCs. MI-3 inhibits growth of human leukemia cell lines containing MLL translocations and decreases the expression of the transcription factors HOXA9, HOXA10, and MEIS1 in THP-1 cells.

    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).