DC Chemicals · Product datasheet

MI 2 (Menin-MLL Inhibitor) — Datasheet

CAT. NO. DC7621

Product page and current package options

ParameterValue
Chemical Name4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine
CAS No.1271738-62-5
Synonyms4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine;MI-2;4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)-piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine;MI-?2;MI-2 (Menin-MLL Inhibitor);AK118880;CS-0771;HY-15222;Menin-MLL inhibitor 2;QCR-218;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-propyl-;4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-propylthieno[2,3-d]pyrimidine;4-[4-(5,5-Dimethyl-4,5-Dihydro-1,3-Thiazol-2-Yl)piperazin-1-Yl]-6-Propylthieno[2,3-D]pyrimidine;mi-2-menin-mll-inhibitor;MI 2 (Menin-MLL Inhibitor);MI-2, Menin-MLL inhibitor 2;AOB1818;Menin-MLL inhibitor MI-2
FormulaC18N5S2H25
M.Wt375.5546
SMILESS1C(=NC([H])([H])C1(C([H])([H])[H])C([H])([H])[H])N1C([H])([H])C([H])([H])N(C2=C3C([H])=C(C([H])([H])C([H])([H])C([H])([H])[H])SC3=NC([H])=N2)C([H])([H])C1([H])[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.

In Vitro

The 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)[1].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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