SGI 1027, DNA 甲基转移酶 1 抑制剂

DNA甲基转移酶抑制剂
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
S420365-1ml
1ml 现货 Stock Image

基本描述

别名 N-[4-[(2-氨基-6-甲基-4-嘧啶基)氨基]苯基] -4-(4-喹啉基氨基)苯甲酰胺
规格或纯度 Moligand™, 10mM in DMSO
英文名称 SGI 1027
生化机理 DNA甲基转移酶抑制剂。抑制哺乳动物DNA甲基转移酶DNMT3B,DNMT3A和DNMT1(IC50值为7.5、8和12.5μM,以Poly(dl-dC)为底物)。通过减少CpG岛超甲基化来重新激活沉默的肿瘤抑制基因。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 DNA 甲基转移酶 1 抑制剂
产品介绍

SGI-1027 是 DNA 甲基转移酶 (DNMT) 抑制剂,对以 poly(dI-dC) 为底物的 DNMT3B,DNMT3A 和 DNMT1 的 IC50 值分别为 7.5 μM,8 μM 和 12.5 μM。

Application:

SGI-1027 has been used as a DNA methyltransferase inhibitor to study its effects on gene expression during osteogenic differentiation. It has also been used as a DNA methyltransferase 3a inhibitor to study its effects on interleukin-6 (IL-6)-induced loss of forkhead box P3 (Foxp3) gene expression in B-lymphocyte-induced maturation protein 1 (Blimp1)-Treg cells.


关联靶点(人)

DNMT3A Tclin DNA(胞嘧啶-5)-甲基转移酶 3A(DNA (cytosine-5)-methyltransferase 3A) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
DNMT1 Tclin DNA(胞嘧啶-5)-甲基转移酶1(DNA (cytosine-5)-methyltransferase 1) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (978 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT3A Tclin DNA (cytosine-5)-methyltransferase 3A (310 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K3 Tchem Dual specificity mitogen-activated protein kinase kinase 3 (632 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AOX1 Tchem Aldehyde oxidase (429 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
K562 (73714 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Raji (5516 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U-937 (7138 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KG-1 (867 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MDA-MB-231 (73002 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PBMC (10003 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (150 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EHMT1 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (407 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT3A Tclin DNMT3A2/3L complex (48 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MYC Tchem c-Myc/c-Max (51 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prmt1 Protein arginine N-methyltransferase 1 (55 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IUPAC Name N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
INCHI InChI=1S/C27H23N7O/c1-17-16-25(34-27(28)30-17)32-20-10-12-21(13-11-20)33-26(35)18-6-8-19(9-7-18)31-24-14-15-29-23-5-3-2-4-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34)
InChi Key QSYLKMKIVWJAAK-UHFFFAOYSA-N
Canonical SMILES CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54
Isomeric SMILES CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54
PubChem CID 24858111
分子量 461.52

化学和物理性质

分子量 461.500 g/mol
XLogP3 4.800
氢键供体数Hydrogen Bond Donor Count 4
氢键受体数Hydrogen Bond Acceptor Count 7
可旋转键计数Rotatable Bond Count 6
精确质量Exact Mass 461.196 Da
单同位素质量Monoisotopic Mass 461.196 Da
拓扑极表面积Topological Polar Surface Area 118.000 Ų
重原子数Heavy Atom Count 35
形式电荷Formal Charge 0
复杂度Complexity 676.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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