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UNC3866

组蛋白甲基转移酶拮抗剂
COA COA
    级别和纯度:
  • ≥95%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
U413984-5mg
 5mg 现货 Stock Image
U413984-25mg
 25mg 现货 Stock Image
U413984-100mg
 100mg 现货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
查看相关系列
Histone Modification (3105) 组蛋白甲基转移酶 (190) 表观遗传学 (1497)
main product photo

基本描述

英文别名 (3S,6S,9S,12S,15S)-methyl 3-benzyl-1-(4-(tert-butyl)phenyl)-12-(4-(diethylamino)butyl)-15-(hydroxymethyl)-9-isobutyl-6-methyl-1,4,7,10,13-pentaoxo-2,5,8,11,14-pentaazahexadecan-16-oate | L-​Serine | N-​[4-​(1,​1-​dimethylethyl)​benzoyl]​-​L-​phenylalanyl-
规格或纯度 ≥95%
英文名称 UNC3866
生化机理 UNC3866 是 Polycomb CBX 和 CDY 家族染色质的甲基赖氨酸（Kme）读取功能的强效拮抗剂。UNC3866 与 CBX4 和 CBX7 的染色质结合的效力最强，K(d) 均为∼100 nM，与其他七种 CBX 和 CDY 染色质相比，具有 6 至 18 倍的选择性。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Information

UNC3866 UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.


Targets

PRC1 chromodomains ; CBX4 chromodomains ; CBX7 chromodomains ; 94 nM(Kd); 97 nM(Kd)


In vitro

UNC3866 is a potent antagonist of the CBX7-H3 interaction(IC50 = 66±1.2 nM). The affinity of UNC3866 for CBX2, -4, -6 and -8 is also surprisingly well correlated with the percent sequence identity of each chromodomain relative to that of CBX7. UNC3866 is equipotent for CBX4, which is most similar to CBX7, while it is 18-, 6- and 12-fold selective for CBX4/7 over CBX2, -6 and -8, respectively. Additionally, UNC3866 is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2. UNC3866 antagonizes PRC1 chromodomains in cells. Thought the permeability of UNC3866 is low, it is sufficiently cell permeable and stable to evaluate its ability to engage and antagonize the functions of its chromodomain targets in cells. UNC3866 inhibits PC3 cell proliferation .


In vivo

UNC3866 is the predominant species in plasma at all time points tested relative to UNC4007 and shows 25% bioavailability and moderate clearance. While these PK results are promising for a peptidic compound, the use of UNC3866 in vivo may be limited because of the high circulating levels required for intracellular target engagement due to its poor cell permeability. The potential utility of UNC3866 at higher doses for in vivo experiments is currently under investigation.


Cell Research(from reference)

Cell lines：PC3 cells 

Concentrations：30 μM 

Incubation Time：24 hours 
纯度 ≥95%

产品属性

ALogP 4.291
HBD Count 6
Rotatable Bond 25

关联靶点（人）

CDYL Tchem 染色质结构域Y类蛋白(Chromodomain Y-like protein) (3 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)
CBX6 Tchem Chromobox 蛋白同源物 6(Chromobox protein homolog 6) (1 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)
CDYL2 Tchem 染色质结构域 Y 类蛋白 2(Chromodomain Y-like protein 2) (3 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)
CBX4 Tchem E3 SUMO 蛋白连接酶 CBX4(E3 SUMO-protein ligase CBX4) (3 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)
CBX7 Tchem Chromobox 蛋白同源物 7(Chromobox protein homolog 7) (3 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)
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX1 Tbio Chromobox protein homolog 1 (92434 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX7 Tchem Chromobox protein homolog 7 (354 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX8 Tchem Chromobox protein homolog 8 (73 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX4 Tchem E3 SUMO-protein ligase CBX4 (69 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX2 Tchem Chromobox protein homolog 2 (12 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX6 Tchem Chromobox protein homolog 6 (20 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX3 Tbio Chromobox protein homolog 3 (2 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX5 Tbio Chromobox protein homolog 5 (49 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDYL Tchem Chromodomain Y-like protein (97 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDYL2 Tchem Chromodomain Y-like protein 2 (104 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDY1 Tchem Testis-specific chromodomain protein Y 1 (56 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Schistosoma mansoni (6170 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 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 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 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

PubChem SID 488202581
分子类型 小分子
IIUPAC Name methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate
INCHI 1S/C43H66N6O8/c1-10-49(11-2)24-16-15-19-33(39(53)48-36(27-50)42(56)57-9)45-41(55)34(25-28(3)4)46-37(51)29(5)44-40(54)35(26-30-17-13-12-14-18-30)47-38(52)31-20-22-32(23-21-31)43(6,7)8/h12-14,17-18,20-23,28-29,33-36,50H,10-11,15-16,19,24-27H2,1-9H3,(H,44,54)(H,45,55)(H,46,51)(H,47,52)(H,48,53)/t29-,33-,34-,35-,36-/m0/s1
InChi Key UMRRDXVUROEIKJ-JCXBGQGISA-N
Smiles CCN(CC)CCCCC(C(=O)NC(CO)C(=O)OC)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=CC=C(C=C2)C(C)(C)C
Isomeric SMILES CCN(CC)CCCC[C@@H](C(=O)N[C@@H](CO)C(=O)OC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=CC=C(C=C2)C(C)(C)C
PubChem CID 101043861
分子量 795.02

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 100 mg/mL (125.78 mM); Ethanol: 100 mg/mL (125.78 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 125.7829992
Water(mg / mL) Max Solubility ＜1
分子量 795.000 g/mol
XLogP3 5.500
氢键供体数Hydrogen Bond Donor Count 6
氢键受体数Hydrogen Bond Acceptor Count 9
可旋转键计数Rotatable Bond Count 25
精确质量Exact Mass 794.494 Da
单同位素质量Monoisotopic Mass 794.494 Da
拓扑极表面积Topological Polar Surface Area 195.000 Ų
重原子数Heavy Atom Count 57
形式电荷Formal Charge 0
复杂度Complexity 1270.000
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 5
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

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批号(Lot Number) 证书类型 货号
C2327411 分析证书 U413984
C2327471 分析证书 U413984
C2327473 分析证书 U413984
C2327474 分析证书 U413984
C2327476 分析证书 U413984
C2327639 分析证书 U413984

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