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DNA-PK抑制剂V, 蛋白激酶抑制剂；DNA 激活；催化亚基

吗啉代-二苯甲酮A​​TP竞争性抑制剂
COA COA
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货号 (SKU) 包装规格 是否现货 价格 数量
D337627-1mg
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D337627-5mg
 5mg 现货 Stock Image
D337627-10mg
 10mg 现货 Stock Image
D337627-25mg
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D337627-50mg
 50mg 现货 Stock Image
D337627-100mg
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Cell Cycle/DNA Damage (2603) DNA Damage (3514) DNA-PK (29) PI3K/Akt/mTOR (764) protein kinase，DNA-activated，catalytic subunit Inhibitor (15)
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基本描述

英文别名 (2-Hydroxy-4-morpholin-4-yl-phenyl)-phenyl-methanone | 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)-phenyl-methanone | AMA37 | AM-A37 | AMA-37 | AMA 37 | 2-benzoyl-5-(morpholin-4-yl)phenol | CHEMBL478980
规格或纯度 Moligand™, ≥98%
英文名称 DNA-PK Inhibitor V
储存温度 避光,-20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 蛋白激酶抑制剂；DNA 激活；催化亚基
产品介绍

DNA-PK抑制剂V是吗啉代-二苯甲酮化合物。高效，选择性和ATP竞争性DNA-PK抑制剂（IC | 50 | = 270 nM）。在较高浓度下抑制PI 3-K催化亚基p110同工酶（α，β，δ和γ分别为IC | 50 | = 32μM，3.7μM，22μM和〜100μM），并弱抑制一组其他几种激酶即使浓度高达50μM，也包括ATM，ATR，CK2，GRK2，mTOR，PI3KC2α，PI3KC2β，PI3KC2γ和PI4Kβ。

DNA-PK Inhibitor V is a morpholino-benzophenone compound. Potent, selective and ATP-competitive inhibitor of DNA-PK (IC|50|= 270 nM). Inhibits PI 3-K catalytic subunit p110-isozymes at higher concentrations (IC|50|= 32 μM, 3.7 μM, 22 μM and ~ 100μM for α, β, δ and γ, respectively) and weakly inhibits a panel of several other kinases, including, ATM, ATR, CK2, GRK2, mTOR, PI 3KC2α, PI 3KC2β, PI 3KC2γ and PI 4Kβ, even at concentrations as high as 50μM.
纯度 ≥98%

产品属性

IC50 DNA-PK: IC₅₀= 270 nM; PI 3-K catalytIC₅₀ubunit p110-isozyme α: IC₅₀= 32 μM; PI 3-K catalytIC₅₀ubunit p110-isozyme β: IC₅₀= 3.7 μM; PI 3-K catalytIC₅₀ubunit p110-isozyme δ: IC₅₀= 22 μM; PI 3-K catalytIC₅₀ubunit p110-isozyme γ: IC₅₀= ~ 100 μM

关联靶点（人）

PRKDC Tchem DNA依赖性蛋白激酶催化亚基(DNA-dependent protein kinase catalytic subunit) (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)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DAPK3 Tchem Death-associated protein kinase 3 (2108 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKDC Tchem DNA-dependent protein kinase (1929 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR2 Tclin Fibroblast growth factor receptor 2 (3405 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMK2B Tchem CaM kinase II beta (1626 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IKBKB Tchem Inhibitor of nuclear factor kappa B kinase beta subunit (5554 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DAPK2 Tchem Death-associated protein kinase 2 (740 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCE Tchem Protein kinase C epsilon (1520 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCG Tchem Protein kinase C gamma (2471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKD1 Tchem Protein kinase C mu (1904 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ITK Tclin Tyrosine-protein kinase ITK/TSK (3699 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMK1 Tchem CaM kinase I alpha (1664 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMK4 Tbio CaM kinase IV (2116 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）

PIK3CA PI3-kinase p110-alpha subunit (51 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr4 Fibroblast growth factor receptor 4 (138 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 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

分子类型 小分子
IIUPAC Name (2-hydroxy-4-morpholin-4-ylphenyl)-phenylmethanone
INCHI 1S/C17H17NO3/c19-16-12-14(18-8-10-21-11-9-18)6-7-15(16)17(20)13-4-2-1-3-5-13/h1-7,12,19H,8-11H2
InChi Key FALILNHGILFDLC-UHFFFAOYSA-N
Smiles C1COCCN1C2=CC(=C(C=C2)C(=O)C3=CC=CC=C3)O
Isomeric SMILES C1COCCN1C2=CC(=C(C=C2)C(=O)C3=CC=CC=C3)O
分子量 283.32
Reaxy-Rn 9926550
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9926550&ln=

化学和物理性质

溶解性 Soluble in DMSO.
敏感性 对光线敏感
分子量 283.320 g/mol
XLogP3 3.200
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 4
可旋转键计数Rotatable Bond Count 3
精确质量Exact Mass 283.121 Da
单同位素质量Monoisotopic Mass 283.121 Da
拓扑极表面积Topological Polar Surface Area 49.800 Ų
重原子数Heavy Atom Count 21
形式电荷Formal Charge 0
复杂度Complexity 348.000
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）

预防措施声明

P264: 处理后要彻底洗手。

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批号(Lot Number) 证书类型 货号
I2403268 分析证书 D337627
I2403301 分析证书 D337627
I2403267 分析证书 D337627
I2403269 分析证书 D337627
I2403270 分析证书 D337627
I2403271 分析证书 D337627
I2403274 分析证书 D337627
I2403299 分析证书 D337627
I2403300 分析证书 D337627
I2403358 分析证书 D337627
I2403363 分析证书 D337627
I2403366 分析证书 D337627

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