WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 201681
Description: KU-55933 is an ATM inhibitor, which blocks the phosphorylation of Akt induced by insulin and insulin-like growth factor I in cancer cells that exhibit abnormal Akt activity. Moreover, KU-55933 inhibits cancer cell proliferation by inducing G(1) cell cycle arrest. It does so through the downregulation of the synthesis of cyclin D1, a protein known to be elevated in a variety of tumors. In addition, KU-55933 treatment during serum starvation triggers apoptosis in these cancer cells. Research results suggest that KU-55933 may be a novel chemotherapeutic agent targeting cancer resistant to traditional chemotherapy or immunotherapy due to aberrant activation of Akt. Furthermore, KU-55933 completely abrogates rapamycin-induced feedback activation of Akt. Combination of KU-55933 and rapamycin not only induces apoptosis, which is not seen in cancer cells treated only with rapamycin, but also shows better efficacy in inhibiting cancer cell proliferation than each drug alone. For detail see: http://www.ncbi.nlm.nih.gov/pubmed/20053781.
MedKoo Cat#: 201681
Chemical Formula: C21H17NO3S2
Exact Mass: 395.06498
Molecular Weight: 395.49
Elemental Analysis: C, 63.77; H, 4.33; N, 3.54; O, 12.14; S, 16.22
KU-55933, purity > 98%, is in stock. The same day shipping out after order is received.
Synonym: KU 55933; KU55933; KU-55933.
IUPAC/Chemical Name: 2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one
InChi Key: XRKYMMUGXMWDAO-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: O=C1C=C(N2CCOCC2)OC(C3=C4SC5=C(C=CC=C5)SC4=CC=C3)=C1
The following data is based on the product molecular weight 395.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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2: Pizarro JG, Folch J, de la Torre AV, Junyent F, Verdaguer E, Jordan J, Pallas
M, Camins A. ATM is involved in cell-cycle control through the regulation of retinoblastoma protein phosphorylation. J Cell Biochem. 2010 May;110(1):210-8. PubMed PMID: 20213763.
3: Rakkestad KE, Skaar I, Ansteinsson VE, Solhaug A, Holme JA, Pestka JJ, Samuelsen JT, Dahlman HJ, Hongslo JK, Becher R. DNA damage and DNA damage responses in THP-1 monocytes after exposure to spores of either Stachybotrys chartarum or Aspergillus versicolor or to T-2 toxin. Toxicol Sci. 2010 May;115(1):140-55. Epub 2010 Feb 11. PubMed PMID: 20150440.
4: Li Y, Yang DQ. The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt. Mol Cancer Ther. 2010 Jan;9(1):113-25. Epub 2010 Jan 6. PubMed PMID: 20053781.
5: Chalmers AJ, Ruff EM, Martindale C, Lovegrove N, Short SC. Cytotoxic effects of temozolomide and radiation are additive- and schedule-dependent. Int J Radiat
Oncol Biol Phys. 2009 Dec 1;75(5):1511-9. PubMed PMID: 19931733.
6: Golding SE, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA, O'Connor MJ, Povirk LF, van Meter
T, Valerie K. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902. Epub 2009 Oct 6. PubMed PMID: 19808981; PubMed Central PMCID: PMC2761990.
7: Xue L, Yu D, Furusawa Y, Cao J, Okayasu R, Fan S. ATM-dependent hyper-radiosensitivity in mammalian cells irradiated by heavy ions. Int J Radiat
Oncol Biol Phys. 2009 Sep 1;75(1):235-43. PubMed PMID: 19695441.
8: Collaco RF, Bevington JM, Bhrigu V, Kalman-Maltese V, Trempe JP. Adeno-associated virus and adenovirus coinfection induces a cellular DNA damage and repair response via redundant phosphatidylinositol 3-like kinase pathways. Virology. 2009 Sep 15;392(1):24-33. Epub 2009 Jul 23. PubMed PMID: 19628243; PubMed Central PMCID: PMC2742906.
9: Wang Z, Wang M, Kar S, Carr BI. Involvement of ATM-mediated Chk1/2 and JNK kinase signaling activation in HKH40A-induced cell growth inhibition. J Cell Physiol. 2009 Oct;221(1):213-20. PubMed PMID: 19530246.
10: Kumari D, Somma V, Nakamura AJ, Bonner WM, D'Ambrosio E, Usdin K. The role of DNA damage response pathways in chromosome fragility in Fragile X syndrome. Nucleic Acids Res. 2009 Jul;37(13):4385-92. Epub 2009 May 21. PubMed PMID: 19465392; PubMed Central PMCID: PMC2715245.
11: Zhang YW, Jones TL, Martin SE, Caplen NJ, Pommier Y. Implication of checkpoint kinase-dependent up-regulation of ribonucleotide reductase R2 in DNA damage response. J Biol Chem. 2009 Jul 3;284(27):18085-95. Epub 2009 May 5. PubMed PMID: 19416980; PubMed Central PMCID: PMC2709352.