CBFβ Inhibitor
(Synonyms: Core Binding Factor-β Inhibitor) 目录号 : GC15474
Binds CBFβ and disrupts CBF function
Cas No.:493028-20-9
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 493028-20-9 | SDF | |
别名 | Core Binding Factor-β Inhibitor | ||
化学名 | 5-ethyl-4-(4-methoxyphenyl)-2-thiazolamine | ||
Canonical SMILES | COC1=CC=C(C2=C(CC)SC(N)=N2)C=C1 | ||
分子式 | C12H14N2OS | 分子量 | 234.3 |
溶解度 | ≤25mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 4.268 mL | 21.3402 mL | 42.6803 mL |
5 mM | 0.8536 mL | 4.268 mL | 8.5361 mL |
10 mM | 0.4268 mL | 2.134 mL | 4.268 mL |
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工作液浓度: mg/ml;
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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