Basic Information |
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Product Name: | BQU57 |
CAS: | 1637739-82-2 |
English Synonyms: | 6-AMINO-1,3-DIMETHYL-4-(4-(TRIFLUOROMETHYL)PHENYL)-1,4-DIHYDROPYRANO[2,3-C]PYRAZOLE-5-CARBONITRILE ; BQU57 |
H bond acceptor: | 0 |
H bond donor: | 0 |
Smile: | NC1=C(C(C2=C(N(N=C2C)C)O1)C1=CC=C(C=C1)C(F)(F)F)C#N |
InChi: | InChI=1S/C16H13F3N4O/c1-8-12-13(9-3-5-10(6-4-9)16(17,18)19)11(7-20)14(21)24-15(12)23(2)22-8/h3-6,13H,21H2,1-2H3 |
InChiKey: | InChIKey=IJCMHHSFXFMZAI-UHFFFAOYSA-N |
Property |
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Comments: | BQU57 is a potent and selective GTPase Ral Inhibitor. It showed selectivity for Ral relative to the GTPases Ras and RhoA and inhibited tumour xenograft growth to a similar extent to the depletion of Ral using RNA interference. It inhibited the binding of Ral to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines. The binding of the BQU57 to RalB was confirmed by isothermal titration calorimetry, surface plasmon resonance and 1H-15N transverse relaxation-optimized spectroscopy (TROSY) NMR spectroscopy. The Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis. BQU57 that blocks Ral function would be valuable as research tools and for cancer therapeutics. |
Information: | Products for research use only, not for human use |
Safety information |
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