产品名称

英文名称：UNC1215

同义词

UNC1215、1415800-43-9、(2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)、UNC-1215、UNC 1215、CHEMBL2426364、N-Phenyl-2,5-bis({[4-(pyrrolidin-1-yl)piperidin-1-yl]carbonyl})aniline、[3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbon

产品性质

CAS编号：1415800-43-9

分子式：C32H43N5O2

分子量：529.72

PubChem编号：57339144

英文别名：UNC1215|1415800-43-9|(2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)|UNC-1215|UNC 1215|CHEMBL2426364|N-Phenyl-2,5-bis({[4-(pyrrolidin-1-yl)piperidin-1-yl]carbonyl})aniline|[3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbon

规格或纯度：≥98%

英文名称：UNC1215

生化机理：UNC1215 binds L3MBTL3 with a K(d) of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 22 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍UNC1215是L3MBTL3的有效的抑制剂，其对L3MBTL3的抑制强度比MBT家族其他成员更强。HEK293细胞转染了L3MBTL3的3 MBT区域的GFP融合蛋白后，用UNC1215处理可以减少剂量依赖性的反应时间通过结合和与L3MBTL3的共定位。通过AlphaScreen○R甲基化组蛋白肽竞争分析，UNC1215对L3MBTL3显示出较高的拮抗能力，IC50值为24±7.6 nM。作为甲基赖氨酸阅读蛋白L3MBTL3的第一个有效的，选择性的抑制剂，UNC1215通过拮抗L3MBTL3单或双甲基赖氨酸阅读功能显示出高度选择性。UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family.

IUPAC Name：[3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone

INCHI：InChI=1S/C32H43N5O2/c38-31(36-20-12-27(13-21-36)34-16-4-5-17-34)25-10-11-29(30(24-25)33-26-8-2-1-3-9-26)32(39)37-22-14-28(15-23-37)35-18-6-7-19-35/h1-3,8-11,24,27-28,33H,4-7,12-23H2

InChi Key：PQOOIERVZAXHBP-UHFFFAOYSA-N

Canonical SMILES：C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6

Isomeric SMILES：C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6

WGK Germany：3

PubChem CID：57339144

ChEMBL Ligand：CHEMBL2426364

CAS Registry No.：1415800-43-9

RCSB PDB Ligand：UWN

溶解性：25°C DMSO

产品包装