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MI-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MI-3图片
CAS NO:1271738-59-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
MI-3 (Menin-MLL inhibitor 3) 是一种有效且高亲和力的 menin-MLL 抑制剂,IC50 为 648 nM,Kd 为 201 nM。
Cas No.1271738-59-0
别名Menin-MLL inhibitor 3;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)-
化学名4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-isopropylthieno[2,3-d]pyrimidine
Canonical SMILESCC(C1=CC2=C(N3CCN(C(S4)=NCC4(C)C)CC3)N=CN=C2S1)C
分子式C18H25N5S2
分子量375.55
溶解度DMSO: slightly soluble,Ethanol: slightly soluble
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MI-3 is an inhibitor of Menin-Mixed linage leukemia (MML) protein interaction with IC50 value of 648 ± 25 nM [1].

MLL protein is a histone methyltransferase that positively regulates gene transcription. However, MLL gene is a common target for chromosomal translocations found in some leukemia. Fusion of MLL gene with one of over 50 different partner genes forms chimeric oncogenes encoding MLL fusion proteins. Translocations will disrupt the regulatory ability of MLL protein on HOX gene, resulting in enhanced cell proliferation and blocked hematopoietic differentiation. Menin is a tumor suppressor protein which directly controls cell growth in endocrine organs. Importantly, menin is also a highly specific partner of MLL. The regulatory function of MLL and MLL fusion protein is facilitated by the association of menin. Therefore, the interaction between MLL fusion protein and menin is critical for the pathology of leukemia [1].

In HEK293 cells expressing menin and MLL-AF9 fusion protein, treatment of MI-3 resulted in significant disruption of menin-MLL-AF9 complex without affecting expression level of menin and MLL-AF9 complex [1]. In mouse bone marrow cells (BMC) transduced with MLL-AF9 and MLL-ENL, MI-3 was observed to effectively inhibit menin-MLL interaction-induced cell proliferation, transformation and hematopoietic differentiation [1].

In human MLL leukemia cell lines harboring different translocations, MI-3 treatment showed an effective and dose-dependent growth inhibition of several cell lines with different MLL translocations [1].

Reference:
[1] Grembecka J et al. , Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology. 2012, 8(3): 277-284.