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CBFβInhibitor
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。
CBFβInhibitor图片
CAS NO:493028-20-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt234.3
Cas No.493028-20-9
FormulaC12H14N2OS
SynonymsCore Binding Factor-β Inhibitor
Solubility≤25mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide
Chemical Name5-ethyl-4-(4-methoxyphenyl)-2-thiazolamine
Canonical SMILESCOC1=CC=C(C2=C(CC)SC(N)=N2)C=C1
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

资料参考

CBFβ inhibitor is a small molecule which binds to CBFβ and inhibits its association with Runx1 [1].

Core binding factors (CBFs) are heterodimeric transcription factors containing a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ. CBF dimers plays important roles in hematopoiesis and, when dysfunctional, in leukemia [2].The interaction of CBFβwith Runx2 has a critical role in bone development [3].

In vitro: The ELISA results have shown that CBFβ Inhibitor is very effective in inhibiting the CBFβ-Runx1 interaction with an IC50 of 3.2 μM. In the leukemia cell line ME-1 expressing CBFβ-SMMHC, CBFβ Inhibitor reduced cell proliferation dose-dependently. Treatment with CBFβ Inhibitor for 3 days showed an increase in apoptotic cells. Treatment with CBFβ Inhibitor for 14 days individually or with all-trans-retinoic acid (ATRA) resulted in cells with greater variation in size and shape, lower nuclear-to-cytoplasmic ratio, increased folding and lobation of nuclei, and more clumped chromatin. All of these morphology changes are consistent with differentiation to more mature forms. CBFβ Inhibitor at 50 μM increased proliferation of Hep-G2 cells. CBFβ treatment with Inhibitor resulted in a statistically significant reduction in Runx1 bound to DNA [1].

References:
[1].  Gorczynski M J, Grembecka J, Zhou Y, et al. Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFβ[J]. Chemistry & biology, 2007, 14(10): 1186-1197.
[2].  Swiers G, De Bruijn M, Speck N A. Hematopoietic stem cell emergence in the conceptus and the role of Runx1[J]. The International journal of developmental biology, 2010, 54: 1151.
[3].  Kundu M, Javed A, Jeon J P, et al. Cbfβ interacts with Runx2 and has a critical role in bone development[J]. Nature genetics, 2002, 32(4): 639-644.