MI-2 (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with an IC50 value of 446 ± 28 nM.
Menin is an oncogenic cofactor in leukemic transformations which could bind to the N-terminal fragment of MLL existed in all MLL fusion proteins. Menin is a highly specific and direct binding partner of MLL and MLL fusion proteins which is essential for regulation of their target genes. Disruption of the menin-MLL protein interaction abrogates oncogenic properties of MLL fusion proteins and blocks the development of acute leukemia [2].
In vitro: In HEK293 cells, MI-2 accessed the protein target menin-MLL and effectively inhibited the menin-MLL-AF9 interaction. MI-2 effectively blocked cell proliferation, and induced cell apoptosis in human MLL leukemia cell lines harboring different MLL translocations MLL-AF9 and MLL-ENL, with the GI50 value of about 5 μM for MI-2. MI-2 showed little effect on the cell growth of E2A-HLF transduced BMC with the GI50 of > 50 μM. MI-2 specifically reduced the immortalization potential of cells transformed with MLL fusion oncoproteins by downregulating the expression of target genes required for MLL fusion protein oncogenic activity [1].
In vivo: After 7 days treatment with MI-2, MLL-AF9 transformed BMC showed great morphology changes and the expression of CD11b was greatly increased [1].
References:
[1]. Grembecka J, He S, Shi A, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia[J]. Nature chemical biology, 2012, 8(3): 277-284.
[2]. Borkin D, He S, Miao H, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo[J]. Cancer Cell, 2015, 27(4): 589-602.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 448.5 |
Formula | C18H25N5S2·2HCl |
Solubility | ≤30mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | 4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine, dihydrochloride |
SDF | Download SDF |
Canonical SMILES | CCCC(S1)=CC(C1=NC=N2)=C2N3CCN(C4=NCC(C)(C)S4)CC3.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |