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587871-26-9

KU-55933 (ATM Kinase Inhibitor)

CAS: 587871-26-9

Molecular Formula: C21H17NO3S2

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587871-26-9 - Names and Identifiers

Name KU-55933 (ATM Kinase Inhibitor)
Synonyms KV-55933
KU-55933
KU-55933 (ATM Kinase Inhibitor)
2-MORPHOLIN-4-YL-6-THIANTHREN-1-YL-PYRAN-4-ONE
2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one
2-(4-Morpholinyl)-6-(1-thianthrenyl)-4H-pyran-4-one
2-Morpholin-4-yl-6-thianthren-1-ylpyran-4-one KU-55933 (ATM Kinase Inhibitor)
CAS 587871-26-9

587871-26-9 - Physico-chemical Properties

Molecular FormulaC21H17NO3S2
Molar Mass395.49
Density1.419±0.06 g/cm3(Predicted)
Boling Point628.0±55.0 °C(Predicted)
Solubility Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 20 mg/ml)
Appearancepowder
Colorwhite to beige
pKa0.33±0.20(Predicted)
Storage Condition-20°C
StabilityStable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
In vitro studyKU-55933 is a potent specific ATM inhibitor with an IC50 of 13 nM and a Ki value of 2.2 nM. KU-55933 also inhibited DNA-PK and PI3K with IC50 of 2.5 and 16.6 μm, respectively. KU-55933 also inhibited mTOR activity with an IC50 of 9.3 μm. KU-55933 effective for ATM dependent phosphorylation. KU-55933 inhibits ATM-dependent phosphorylation in a dose-dependent manner with an IC50 of 300 nM. Below 30 μm, KU-58050 failed to inhibit the ATM-dependent phosphorylation of p53 (site serine 15). In the UV-induced H2AX (site 139 serine), NBS1 (site 343 serine), CHK1 (site 345 serine), and SMC1 (serine at position 966), the addition of KU-55933 had no significant effect. Upon UV treatment, KU-55933 cleaves the substrate of ATM phosphorylation induced by ionizing radiation. KU-55933 HeLa cells were sensitive to ionizing radiation. In cancer cells, KU-55933 inhibited growth factor-induced phosphorylation of Akt. KU-55933 inhibition of cancer cell proliferation. KU-55933 inhibition of ATM, by blocking the activation of downstream TAp63α, improve the viability.
KU-55933 is a potent specific ATM inhibitor with an IC50 of 13 nM and a K I value of 2.2 nM. KU-55933 also inhibited DNA-PK and PI3K with IC50 of 2.5 and 16.6 μm, respectively. KU-55933 also inhibited mTOR activity with an IC50 of 9.3 μm. KU-55933 effective for ATM dependent phosphorylation. KU-55933 inhibits ATM-dependent phosphorylation in a dose-dependent manner with an IC50 of 300 nM. Below 30 μm, KU-58050 failed to inhibit the ATM-dependent phosphorylation of p53 (site serine 15). In the UV-induced H2AX (site 139 serine), NBS1 (site 343 serine), CHK1 (site 345 serine), and SMC1 (serine at position 966), the addition of KU-55933 had no significant effect. Upon UV treatment, KU-55933 cleaves the substrate of ATM phosphorylation induced by ionizing radiation. KU-55933 HeLa cells were sensitive to ionizing radiation. In cancer cells, KU-55933 inhibited growth factor-induced phosphorylation of Akt. KU-55933 inhibition of cancer cell proliferation. KU-55933 inhibition of ATM, by blocking the activation of downstream TAp63α, improve the viability.
In vivo studyKU-55933 inhibits the activation of STAT3 in ATM-dependent and enhances TRAIL-regulated apoptosis by up-regulating the expression of DR5. Both inhibition of STAT3 and NF-κB are associated with down-regulation of cFLIP, accompanied by an increase in the level of apoptosis. ATM inhibitor KU-55933 had a greater effect on TRAIL-regulated apoptosis than either the JAK2 inhibitor AG490 or STAT3β overexpression.
KU-55933 inhibits ATM-dependent STAT3 activation and enhances TRAIL-regulated apoptosis by up-regulating DR5 expression. Both inhibition of STAT3 and NF-κB are associated with down-regulation of cFLIP, accompanied by increased levels of apoptosis. ATM inhibitor KU-55933 had a greater effect on TRAIL-regulated apoptosis than either the JAK2 inhibitor AG490 or STAT3β overexpression.

587871-26-9 - Risk and Safety

WGK Germany3

587871-26-9 - Reference

Reference
Show more
Liang Yan, Jia Zhen, Chen Zhong Hai, a Liang De. Effect of ATM on lung ischemia-reperfusion injury in rats SEVOFRANE (Sevoflurane) [J]. Chin J Gerol 2018 38(15):3756-3759.

587871-26-9 - Preparation solution concentration reference

 1mg5mg10mg
1 mM2.529 ml12.643 ml25.285 ml
5 mM0.506 ml2.529 ml5.057 ml
10 mM0.253 ml1.264 ml2.529 ml
5 mM0.051 ml0.253 ml0.506 ml
Last Update:2024-01-02 23:10:35

587871-26-9 - Reference Information

biological activity KU-55933 (ATM Kinase Inhibitor) is an effective, specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM. Compared with DNA-PK, PI3K/PI4K, ATR and mTOR, ATM is highly selective.
KU-55933 (ATM Kinase Inhibitor) is an effective and specific ATM inhibitor. IC50/Ki is 12.9 nM/2.2 nM in cell-free test. Compared with DNA-PK, PI3K/PI4K, ATR and mTOR, it is highly selective for ATM. KU -55933 (ATM Kinase Inhibitor) can inhibit the activation of autophagy-initiating kinase ULK1, resulting in a significant reduction in autophagy.
in vitro studies KU-55933 are effective specific ATM inhibitors with IC50 of 13 nM and Ki value of 2.2 nM. KU-55933 also inhibited DNA-PK and PI3K with IC50 of 2.5 and 16.6 μM, respectively. KU-55933 also inhibited mTOR activity with IC50 of 9.3 μM. KU-55933 effectively acts on ATM-dependent phosphorylation. KU-55933 inhibited ATM-dependent phosphorylation in a dose-dependent manner with an IC50 of 300 nM. At less than 30 μM, KU-58050 cannot inhibit ATM-dependent phosphorylation of p53 (serine at position 15). In UV-induced H2AX (serine at site 139), NBS1 (serine at site 343), CHK1 (serine at site 345), and SMC1 (serine at site 966), the addition of KU-55933 had no obvious effect. During UV treatment, ATM phosphorylated substrates induced by ionizing radiation were KU-55933 excised. KU-55933 sensitize HeLa cells to ionizing radiation. In cancer cells, KU-55933 inhibits the phosphorylation of Akt induced by growth factors. KU-55933 inhibit the proliferation of cancer cells. KU-55933 inhibit ATM and improve the viability by blocking the activation of downstream TAp63α.
KU-55933 is an effective specific ATM inhibitor with IC50 of 13 nM and K I value of 2.2 nM. KU-55933 also inhibited DNA-PK and PI3K with IC50 of 2.5 and 16.6 μM, respectively. KU-55933 also inhibited mTOR activity with IC50 of 9.3 μM. KU-55933 effectively acts on ATM-dependent phosphorylation. KU-55933 inhibited ATM-dependent phosphorylation in a dose-dependent manner with an IC50 of 300 nM. At less than 30 μM, KU-58050 cannot inhibit ATM-dependent phosphorylation of p53 (serine at position 15). In UV-induced H2AX (serine at site 139), NBS1 (serine at site 343), CHK1 (serine at site 345), and SMC1 (serine at site 966), the addition of KU-55933 had no obvious effect. During UV treatment, ATM phosphorylated substrates induced by ionizing radiation were KU-55933 excised. KU-55933 sensitize HeLa cells to ionizing radiation. In cancer cells, KU-55933 inhibits the phosphorylation of Akt induced by growth factors. KU-55933 inhibit the proliferation of cancer cells. KU-55933 inhibit ATM and improve the viability by blocking the activation of downstream TAp63α.
in vivo studies KU-55933 inhibit ATM-dependent STAT3 activation, enhance TRAIL-regulated apoptosis by up-regulating DR5 expression, and inhibit STAT3 and NF-κB both related to down-regulating cFLIP, accompanied by an increase in apoptosis level. ATM inhibitors KU-55933 affect TRAIL-regulated apoptosis than JAK2 inhibitors AG490 or STAT3β overexpression.
KU-55933 inhibits ATM-dependent STAT3 activation, enhances TRAIL-regulated apoptosis by up-regulating DR5 expression, and inhibits STAT3 and NF-κB both related to down-regulating cFLIP, accompanied by an increase in apoptosis level. ATM inhibitors KU-55933 affect TRAIL-regulated apoptosis than JAK2 inhibitors AG490 or STAT3β overexpression.
target TargetValue ATM (Cell-free say) 12.9 nM
TargetValue
ATM (Cell-free assay) 12.9 nM
Last Update:2024-04-10 22:29:15
587871-26-9
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Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: KU-55933 (ATM Kinase Inhibitor) Visit Supplier Webpage Request for quotation
CAS: 587871-26-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: KU-55933 Request for quotation
CAS: 587871-26-9
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: KU-55933 (ATM Kinase Inhibitor) Visit Supplier Webpage Request for quotation
CAS: 587871-26-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: KU-55933 Visit Supplier Webpage Request for quotation
CAS: 587871-26-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: KU-55933 (ATM Kinase Inhibitor) Visit Supplier Webpage Request for quotation
CAS: 587871-26-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
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