產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 200mg
CAS	1271738-62-5
別名	Menin-MLL inhibitor 2;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-propyl-
化學名	4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-propylthieno[2,3-d]pyrimidine
分子式	C18H25N5S2
分子量	375.55
溶解度	≥ 15.1 mg/mL in DMSO, ≥ 46.4 mg/mL in EtOH with gentle warming
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

MI-2 is a Menin-MLL inhibitor with IC50 value of 0.45 μM [1].

Mixed-lineage leukemia (MLL) is a common target of chromosomal translocations in patients with acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). The leukemogenic activity of MLL fusion proteins is dependent on their direct interaction with menin, which is a tumor suppressor that directly controls cell growth in endocrine organs [1].

MI-2 is a Menin-MLL inhibitor. MI-2 bound to the wild-type menin but didn’t bind M278K and Y323K menin mutants. In HEK293 cells transfected with Flag-MLL-AF9, MI-2 effectively inhibited the menin-MLL-AF9 interaction without affecting the expression level of menin and MLL-AF9. In mouse bone marrow cells (BMC) transduced with MLL-AF9 and MLL-ENL, MI-2 blocked proliferation of BMC with GI50 value of about 5 μM. Also, MI-2 inhibited colony formation in BMC transduced with MLL-AF9. In a series of human MLL leukemia cell lines, MI-2 significantly inhibited translocation in a dose dependant way [1].

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原創(chuàng)作者：上海莼試生物技術有限公司

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