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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
规格:98%
分子量:234.3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
CBFβ inhibitor
CAS:493028-20-9
分子式:C12H14N2OS
分子量:234.3
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.