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JMJD7-IN-1

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Chemical Structure| 311316-96-8 同义名 : -
CAS号 : 311316-96-8
货号 : A1481144
分子式 : C16H8Cl2N2O4
纯度 : 98%+
分子量 : 363.152
MDL号 : MFCD00825934
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(19.28 mM)，配合低频超声，并水浴加热至45℃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 JMJD5 and JMJD7 (JMJD5/7) are responsible for the clipping of arginine methylated histone tails to generate "tailless nucleosomes", which could release the pausing RNA polymerase II (Pol II) into productive transcription elongation. JMJD5/7 function as endopeptidases that cleave histone tails specifically adjacent to methylated arginine residues and continue to degrade N-terminal residues of histones via their aminopeptidase activity[2]. Knockouts of JMJD5 and JMJD7 dramatically increase the content of arginine-methylated histone tails as well as the overall content of histone subunits in cells. Deletion of JMJD7 genes in human breast cancer cells drastically reduces their growth in soft agar[3]. JMJD7 was present at gene promoters and its promoter occupancy changed upon osteoclast differentiation. Further, JMJD7 downregulation caused more rapid osteoclast differentiation[4]. The JMJD7-PLA2G4B fusion protein does not encompass the full JmjC domain of JMJD7-predicting absence of any enzymatic activity - but consists of nearly the whole PLA2G4B protein, the functions of JMJD7-PLA2G4B are likely to match those of PLA2G4B. In the same vein, the association of a sequence variant of the JMJD7-PLA2G4B gene with high-risk autism is unlikely due to dysregulated JMJD7 enzymatic activity[5]. JMJD7-IN-1 efficiently binds to JMJD7, with an IC50 of 3.80 μM. JMJD7-IN-1 (72 h) inhibits the growth of T-47d, SK-BR-3, Jurkat and Hela cells, with IC50s of 9.40 μM, 13.26 μM, 15.03 μM and 16.14 μM, respectively. JMJD7-IN-1 (0.1-1000 μM) dose-dependently inhibits the activity of JMJD7, with an IC50 of 6.62 μM[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.75mL

0.55mL

0.28mL

13.77mL

2.75mL

1.38mL

27.54mL

5.51mL

2.75mL
参考文献

[1]Zhang W, Li K, Wang T, Wu M, Li L. Discovery of JMJD7 inhibitors with the aid of virtual screening and bioactivity evaluation. Bioorg Med Chem Lett. 2021 Aug 1;45:128139. doi: 10.1016/j.bmcl.2021.128139. Epub 2021 May 25. PMID: 34048880.

[2] Haolin Liu,et al. Specific Recognition of Arginine Methylated Histone Tails by JMJD5 and JMJD7. Sci Rep. 2018 Feb 19;8(1):3275.

[3]Haolin Liu,et al. Clipping of arginine-methylated histone tails by JMJD5 and JMJD7. Proc Natl Acad Sci U S A. 2017 Sep 12;114(37):E7717-E7726.

[4]Y. Liu,et al.Histone demethylase Jmjd7 negatively regulates differentiation of osteoclast, Chin. J. Dent. Res. 21 (2018) 113-118.

[5]N. Matsunami, et al. Identification of rare DNA sequence variants in high-risk autism families and their prevalence in a large case/control population, Mol. Autism 5 (2014) 5.

[6]Zhang W, et, al. Discovery of JMJD7 inhibitors with the aid of virtual screening and bioactivity evaluation. Bioorg Med Chem Lett. 2021 May 25;45:128139.