KU-55933 (ATM Kinase Inhibitor) - Moligand™, 10mM in DMSO , Inhibitor of ATM serine/threonine kinase, CAS No.587871-26-9, Inhibitor of ATM serine/threonine kinase

CAS: 587871-26-9 Cat. No.: K408000 Peso molecular: 395.49

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

KU-55933 (ATM Kinase Inhibitor) is a potent and specificATMinhibitor withIC50/Kiof 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. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation
In vitro

KU-55933 inhibits DNA-PK and PI3K with IC50 of 2.5 μM and 16.6 μM, respectively. Besides, KU-55933 also prevents the activity of mTOR with IC50 of 9.3 μM. KU-55933 is active at the cellular level in ablating a well-characterized ATM-dependent phosphorylation event. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with IC50 of 300 nM. KU-58050 does not prevent the ATM-dependent phosphorylation of p53 serine 15 until a dose of 30 μM. Addition of KU-55933 has no appreciable effects on UV-induced phosphorylation of H2AX on serine 139, NBS1 on serine 343, CHK1 on serine 345, and SMC1 on serine 966. In stark contrast to the UV responses, KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 sensitizes HeLa cells to a range of ionizing radiation doses. KU-55933 inhibits the phosphorylation of Akt induced by growth factors in cancer cells. KU-55933 suppresses the proliferation of cancer cells. Furthermore, suppression of ATM by KU-55933 improves survival, probably via prevention of downstream activation of TAp63α.

In vivo

Suppression of ATM-dependent STAT3 activation by KU-55933 enhances TRAIL-mediated apoptosis through up-regulation of surface DR5 expression, whereas suppression of both STAT3 and NF-κB appeares to be involved in down-regulation of cFLIP accompanied by an additional increase in apoptotic levels. The ATM inhibitor KU-55933 affectes TRAIL-mediated apoptosis more strongly than the JAK2 inhibitor, AG490, or overexpression of STAT3β.
Cell Data

cell lines：

Concentrations：10 μM

Incubation Time：2 hours

Powder Purity:≥99%

Specifications

Sinónimos

2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/K_i 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. KU‑55933 (ATM Kinase Inhibitor) inhibits

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of ATM serine/threonine kinase

Nombres e identificadores

• Isómeros SMILES: C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4
• WGK Alemania: 3
• Peso molecular: 395.49
• Reaxy-Rn: 10197588
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10197588&ln=

Objetivos asociados (humanos)

ATM Tchem Serine-protein kinase ATM (9 Activities)

Discover Target: ATM

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 56 mg/mL (201.18 mM); Ethanol: 56 mg/mL (201.18 mM); Water: Insoluble
• Índice de refracción: 1.71
• Punto de ebullición (°C): 628.01° C at 760 mmHg
• Punto de fusión (°C): 229.98°C

Referencias

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]