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.
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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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet