MI-2 (Menin-MLL Inhibitor)

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MI-2 (Menin-MLL Inhibitor) 是一种有效的 menin-MLL 相互作用抑制剂，IC50 为 446 nM。

MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC50 values in the nanomolar range, including MI-2 (IC50= 446±28 nM) and MI-3 (IC50=648±25 nM).The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, Kd=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI50>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI50 values below 10 μM in MV4;11 (harboring MLL-AF4; GI50=9.5 μM), KOPN-8 (MLL-ENL; GI50=7.2 μM) and ML-2 (MLL-AF6; GI50=8.7 μM), and in MonoMac6 (MLL-AF9; GI50=18 μM).

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Menin-MLL Inhibitor

Chromatin/Epigenetic

HMTase

Menin-MLL

Cancer

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1271738-62-5

375.55

C18H25N5S2

>98% (HPLC)

Ethanol: 75 mg/mL (199.7 mM); DMSO: 75 mg/mL warmed (199.7 mM)

CCCC1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1

4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-propylthieno[2,3-d]pyrimidine

(-20℃)

With Ice Pack

≥ 2 years