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Chemical Structure| 587871-26-9 Chemical Structure| 587871-26-9

Structure of KU-55933
CAS No.: 587871-26-9

Chemical Structure| 587871-26-9

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KU-55933 is a potent ATM inhibitor with IC50 and Ki values of 12.9 and 2.2 nM, respectively, and is highly selective for ATM compared to DNA-PK, PI3K/PI4K, ATR, and mTOR.

Synonyms: ATM Kinase Inhibitor

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Product Details of KU-55933

CAS No. :587871-26-9
Formula : C21H17NO3S2
M.W : 395.49
SMILES Code : O=C1C=C(N2CCOCC2)OC(C3=C4SC5=C(C=CC=C5)SC4=CC=C3)=C1
Synonyms :
ATM Kinase Inhibitor
MDL No. :MFCD08276985
InChI Key :XRKYMMUGXMWDAO-UHFFFAOYSA-N
Pubchem ID :5278396

Safety of KU-55933

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of KU-55933

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • ATM

    ATM, IC50:12.9 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 10 mM 2 h Inhibition of ATM activity enhanced aescin-induced apoptosis Acta Pharmacol Sin. 2018 Dec;39(12):1874-1884.
AD-293 cells 8.3 μM 24 h KU-55933 suppressed Id-1 expression through high-throughput screening Proc Natl Acad Sci U S A. 2024 Jan 30;121(5):e2318718121.
human vascular endothelial cells 10 μM 24 h inhibited Smad1/5 activation induced by disturbed flow and BMP4, and suppressed endothelial cell proliferation and inflammation Proc Natl Acad Sci U S A. 2024 Jan 30;121(5):e2318718121.
Human podocytes 10 μM 2 h Inhibit ATM kinase activity, reduce MAD2B upregulation, and alleviate ADR-induced podocyte injury and cell cycle re-entry Int J Biol Sci. 2021 Oct 22;17(15):4396-4408.
DU145 cells 10μM 4 h KU55933 enhanced the radiosensitivity of DU145 cells, comparable to the effects of 30nM AZ12253801 at 10Gy, and similar to 60nM AZ12253801 at 1-10Gy. Oncogene. 2014 Nov 6;33(45):5262-73.
AGS human gastric epithelial cells 5 and 10 μM 6 h KU-55933 inhibited H. pylori-induced cell death and suppressed the increment of Bax/Bcl-2 ratio, caspase-3 activation, and nucleosome-bound DNA level. J Ginseng Res. 2020 Jan;44(1):79-85.
B65 Neuroblastoma Cells 10 µM 30 min KU-55933 significantly inhibited MPP?-induced pRb phosphorylation. Cell Mol Life Sci. 2010 Nov;67(22):3865-82.
Cerebellar Granule Cells (CGC) 1-10 µM 24 h KU-55933 showed neuroprotective effects against MPP?-induced neuronal apoptosis, reducing nuclear condensation and DNA fragmentation. Cell Mol Life Sci. 2010 Nov;67(22):3865-82.
Human corneal epithelial cells (hTCEpi) 10 µM 24 h Inhibition of ATM activity significantly reduced HSV-1 viral replication and cytopathic effect Invest Ophthalmol Vis Sci. 2014 Feb 3;55(2):706-15.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice A549 cell xenograft model Intraperitoneal injection 10 mg/kg Administered 1 day before radiotherapy and every other day thereafter To verify the regulatory role of ATM on tumor growth under low-dose radiation. Results showed that the ATM inhibitor alone inhibited the growth of A549 tumors, and the effect was more pronounced when combined with low-dose radiotherapy. Front Cell Dev Biol. 2021 May 12;9:650819
Apolipoprotein E-deficient mice High-fat diet-induced atherosclerosis model Tail vein injection 8 mg/kg Twice a week for 12 weeks KU-55933 inhibited atherosclerotic lesion formation and reduced endothelial cell proliferation and inflammation Proc Natl Acad Sci U S A. 2024 Jan 30;121(5):e2318718121.
Mice ADR-induced FSGS model Intraperitoneal injection 500 µg/kg Every 3 days until sacrifice Inhibit ATM kinase activity, reduce MAD2B upregulation, and alleviate ADR-induced podocyte injury and proteinuria Int J Biol Sci. 2021 Oct 22;17(15):4396-4408.
C57BL/6J Mice HSV-1 keratitis model Topical eye drops 200 µM Every 4 hours for 1 day, then every 8 hours for the remainder of the experiment KU-55933 significantly reduced the severity of stromal keratitis in mice Invest Ophthalmol Vis Sci. 2014 Feb 3;55(2):706-15.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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