UA 62784 - CAS 313367-92-9
Catalog number: 313367-92-9
Category: Inhibitor
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Molecular Formula:
C23H15NO3
Molecular Weight:
353.37
COA:
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Targets:
Microtubule/Tubulin
Description:
UA 62784, under the IUPAC name 4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]fluoren-9-one, a cytotoxic microtubule inhibitor in vitro, causes reversible cell cycle arrest in mitosis before metaphase, which leads to apoptosis. It is also a novel specific inhibitor of CENP-E, which likely binds within the motor domain of CENP-E.
Brife Description:
A cytotoxic microtubule inhibitor
Appearance:
Yellow solid
Synonyms:
4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]fluoren-9-one; UA62784, UA62784, UA 62784; 313367-92-9; 4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]-9H-fluoren-9-one; AC1MPDKY; Oprea1_740865; SCHEMBL14765347; CTK8E8877; DTXSID20391982; ZINC1512677; AKOS024458074; PL053830; 4-[5-(4-Methoxyphenyl)-2-oxazolyl]-9H-Fluoren-9-one; 4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]fluoren-9-one; UA 62784|4-[5-(4-Methoxyphenyl)-2-oxazolyl]-9H-fluoren-9-one
Solubility:
Soluble to 25 mM in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -66℃ for long term (months to years).
MSDS:
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InChIKey:
SVICLWPFAQYZLX-UHFFFAOYSA-N
InChI:
1S/C23H15NO3/c1-26-15-11-9-14(10-12-15)20-13-24-23(27-20)19-8-4-7-18-21(19)16-5-2-3-6-17(16)22(18)25/h2-13H,1H3
Canonical SMILES:
COC1=CC=C(C=C1)C2=CN=C(O2)C3=C4C5=CC=CC=C5C(=O)C4=CC=C3
1.UA62784 Is a cytotoxic inhibitor of microtubules, not CENP-E.
Tcherniuk S1, Deshayes S, Sarli V, Divita G, Abrieu A. Chem Biol. 2011 May 27;18(5):631-41. doi: 10.1016/j.chembiol.2011.03.006.
A recent screen for compounds that selectively targeted pancreatic cancer cells isolated UA62784. We found that UA62784 inhibits microtubule polymerization in vitro. UA62784 interacts with tubulin dimers ten times more potently than colchicine, vinblastine, or nocodazole. Competition experiments revealed that UA62784 interacts with tubulin at or near the colchicine-binding site. Nanomolar doses of UA62784 promote the accumulation of mammalian cells in mitosis, due to aberrant mitotic spindles, as shown by immunofluorescence and live cell imaging. Treatment of cancerous cell lines with UA62784 is lethal, following activation of apoptosis signaling. By monitoring mitotic spindle perturbations and apoptosis, we found that the effects of UA62784 and of some known microtubule-depolymerizing drugs are additive. Finally, high content screening of H2B-GFP HeLa cells revealed that low doses of UA62784 and vinblastine potentiate each other to inhibit proliferation.
2.UA62784, a novel inhibitor of centromere protein E kinesin-like protein.
Henderson MC1, Shaw YJ, Wang H, Han H, Hurley LH, Flynn G, Dorr RT, Von Hoff DD. Mol Cancer Ther. 2009 Jan;8(1):36-44. doi: 10.1158/1535-7163.MCT-08-0789.
Pancreatic carcinoma is the fourth leading cause of death from cancer. Novel targets and therapeutic options are needed to aid in the treatment of pancreatic cancer. The compound UA62784 is a novel fluorenone with inhibitory activity against the centromere protein E (CENP-E) kinesin-like protein. UA62784 was isolated due to its selectivity in isogenic pancreatic carcinoma cell lines with a deletion of the DPC4 gene. UA62784 causes mitotic arrest by inhibiting chromosome congression at the metaphase plate likely through inhibition of the microtubule-associated ATPase activity of CENP-E. Furthermore, CENP-E binding to kinetochores during mitosis is not affected by UA62784, suggesting that the target lies within the motor domain of CENP-E. UA62784 is a novel specific inhibitor of CENP-E and its activity suggests a potential role for antimitotic drugs in treating pancreatic carcinomas.
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CAS 313367-92-9 UA 62784

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