KU-55933(ATM激酶抑制剂), ATM 丝氨酸/苏氨酸激酶抑制剂

高效,选择性,竞争性ATM激酶抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
K126884-5mg
5mg 现货 Stock Image
K126884-25mg
25mg 现货 Stock Image
K126884-100mg
100mg 现货 Stock Image

基本描述

英文别名 CS-0146 | KU-55933, >=98% (HPLC) | 2-Morpholin-4-yl-6-thianthren-1-yl-pyran-4-one | ATM Kinase Inhibitor | HMS3265N15 | HMS3413P10 | 2-Morpholino-6-(thianthren-1-yl)-4H-pyran-4-one | HMS3244P07 | SCHEMBL1984941 | NCGC00263190-13 | BCP01834 | EC-000.1920 |
规格或纯度 Moligand™, ≥98%
英文名称 KU-55933 (ATM Kinase Inhibitor)
生化机理 KU-55933 是一种非常有效的共济失调毛细血管扩张症(A-T)突变(ATM)激酶特异性抑制剂(IC50 = 13 nM)。KU-22933 可使癌细胞对电离辐射和细胞毒性 drμgs 敏感。化合物 KU-22933 可阻断 ATM 介导的 p53、gH2AX、NBS1 和 SMC1 磷酸化。IC 50 值分别为 12.9(ATM)、2000(DNA-PK)、9300(mTOR)、16600(PI3K)、>100000(ATR)和 >100000 nM(PI4K)。使细胞对电离辐射和化疗药物敏感。
应用 A cell-permeable, potent, selective and ATP-competitive ATM inhibitor
储存温度 -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 ATM 丝氨酸/苏氨酸激酶抑制剂
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产品介绍

KU-55933是ATM抑制剂,IC50和Ki分别为13和2.2 nM,对DNA-PK,PI3K/PI4K,ATR和mTOR的活性较低。A cell-permeable, potent, selective and ATP-competitive ATM inhibitor

KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
A cell-permeable, potent, selective and ATP-competitive ATM inhibitor

AI解读

关联靶点(人)

ATM Tchem 丝氨酸蛋白激酶 ATM(Serine-protein kinase ATM) (9 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal 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 Journal PubMed Id doi Assay Aladdin ID
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
Fgfr4 Fibroblast growth factor receptor 4 (138 活性数据)
活性类型 Relation Activity value Units Action Type Journal 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 Journal 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 Journal 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 Journal PubMed Id doi Assay Aladdin ID
Toxoplasma gondii (4585 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MDCK (10148 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
H4 (48 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
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 2-morpholin-4-yl-6-thianthren-1-ylpyran-4-one
INCHI InChI=1S/C21H17NO3S2/c23-14-12-16(25-20(13-14)22-8-10-24-11-9-22)15-4-3-7-19-21(15)27-18-6-2-1-5-17(18)26-19/h1-7,12-13H,8-11H2
InChi Key XRKYMMUGXMWDAO-UHFFFAOYSA-N
Canonical SMILES C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4
Isomeric SMILES C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4
WGK Germany 3
PubChem CID 5278396
分子量 395.49

化学和物理性质

溶解性 DMSO 33 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
密度 1.42
折光率 1.71
沸点 628.01° C at 760 mmHg
熔点 229.98°C
分子量 395.500 g/mol
XLogP3 3.900
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 395.065 Da
单同位素质量Monoisotopic Mass 395.065 Da
拓扑极表面积Topological Polar Surface Area 89.400 Ų
重原子数Heavy Atom Count 27
形式电荷Formal Charge 0
复杂度Complexity 643.000
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)

WGK Germany 3

技术规格说明书

Purity(HPLC) 98-100(%)
Appearance(K126884) White to Beige Powder,Solid,Crystals or Chunks
NMR spectrum Conforms to Structure

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批号(Lot Number) 证书类型 日期 货号
C1706025 分析证书 24-07-08 K126884

此产品的引用文献

1. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu.  (2023)  PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma.  CANCER RESEARCH,  83  (7): (1094-1110).  [PMID:36696363] [10.1158/0008-5472.CAN-22-3083]

参考文献

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2. Kubota S et al..  (2014)  Activation of the prereplication complex is blocked by mimosine through reactive oxygen species-activated ataxia telangiectasia mutated (ATM) protein without DNA damage..  J Biol Chem,  289  (9): (5730-46).  [PMID:24421316]
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19. Huang J et al..  (2020)  Tandem Deubiquitination and Acetylation of SPRTN Promotes DNA-Protein Crosslink Repair and Protects against Aging..  Mol Cell,  79  (5): (824-835.e5).  [PMID:32649882]
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21. Okumoto K et al..  (2020)  The peroxisome counteracts oxidative stresses by suppressing catalase import via Pex14 phosphorylation..  Elife,  [PMID:32831175]
22. Meng Y et al..  (2019)  TRAF6 mediates human DNA2 polyubiquitination and nuclear localization to maintain nuclear genome integrity..  Nucleic Acids Res,  47  (14): (7564-7579).  [PMID:31216032]
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24. Kim W et al..  (2019)  ZFP161 regulates replication fork stability and maintenance of genomic stability by recruiting the ATR/ATRIP complex..  Nat Commun,  10  (5304).  [PMID:31757956]
25. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu.  (2023)  PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma.  CANCER RESEARCH,  83  (7): (1094-1110).  [PMID:36696363] [10.1158/0008-5472.CAN-22-3083]

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