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KCC-07

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Chemical Structure| 315702-75-1 同义名 : -
CAS号 : 315702-75-1
货号 : A1327322
分子式 : C14H11N3OS
纯度 : 99%+
分子量 : 269.322
MDL号 : MFCD01121976
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(445.56 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 DNA methylation is a process by which methyl groups are added to cytosine or adenine. DNA methylation can change the activity of the DNA molecule without changing the sequence. Methylation of 5-methylcytosine (5mC) is widespread in both eukaryotes and prokaryotes, and it is a very important epigenetic modification event, which can regulate gene activity and influence a number of key processes such as genomic imprinting, cell differentiation, transcriptional regulation, and chromatin remodeling[2]. 5-Methylcytosine binding domain (MBD) family proteins are essential readers of DNA methylation[3].Proteins containing a methyl-CpG-binding domain (MBD) bind 5mC and convert the methylation pattern information into appropriate functional cellular states. The correct readout of epigenetic marks is of particular importance in the nervous system where abnormal expression or compromised MBD protein function, can lead to disease and developmental disorders[4]. The methylcytosine-binding domain 2 (MBD2) protein recruits the nucleosome remodeling and deacetylase complex (NuRD) to methylated DNA to modify chromatin and regulate transcription. Importantly, MBD2 functions within CpG islands that contain 100s to 1000s of potential binding sites. Since NuRD physically rearranges nucleosomes, the dynamic mobility of this complex is directly related to function[5]. KCC-07 is a selective, potent and brain-penetrant inhibitor of methyl-CpG-binding domain protein 2(MBD2) with anticancer activity. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. In vitro, KCC-07 treatment Medulloblastomas (MB) cells clearly inhibited MB cell growth, consistent with induction of anti-proliferative BAI1/p53/p21 signaling[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.57mL

3.71mL

1.86mL

37.13mL

7.43mL

3.71mL
参考文献

[1]Zhu D, Osuka S, Zhang Z, et al. BAI1 Suppresses Medulloblastoma Formation by Protecting p53 from Mdm2-Mediated Degradation. Cancer Cell. 2018;33(6):1004-1016.e5. doi:10.1016/j.ccell.2018.05.006

[2]Lingfang Feng,et al. DNA Methylation Analysis. Methods Mol Biol. 2019;1894:181-227.

[3]Albert Jeltsch, Biotechnological Applications of MBD Domain Proteins for DNA Methylation Analysis. J Mol Biol. 2019 Sep 5;S0022-2836(19)30544-3.

[4]T Gupta,et al. Functional conservation of MBD proteins: MeCP2 and Drosophila MBD proteins alter sleep. Genes Brain Behav. 2016 Nov;15(8):757-774.

[5] Hai Pan,et al. CpG and methylation-dependent DNA binding and dynamics of the methylcytosine binding domain 2 protein at the single-molecule level. Nucleic Acids Res. 2017 Sep 6;45(15):9164-9177.

[6]Dan Zhu, et al. BAI1 Suppresses Medulloblastoma Formation by Protecting p53 From Mdm2-Mediated Degradation. Cancer Cell. 2018 Jun 11;33(6):1004-1016.e5.