BQU57 - CAS 1637739-82-2
Catalog number: B0084-463448
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C16H13F3N4O
Molecular Weight:
334.1
COA:
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Targets:
Ras
Description:
BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-463448 50 mg $199 In stock
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Purity:
>98%
MSDS:
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InChIKey:
IJCMHHSFXFMZAI-UHFFFAOYSA-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
Canonical SMILES:
CC1=NN(C2=C1C(C(=C(O2)N)C#N)C3=CC=C(C=C3)C(F)(F)F)C
1.Discovery and characterization of small molecules that target the GTPase Ral.
Yan C;Liu D;Li L;Wempe MF;Guin S;Khanna M;Meier J;Hoffman B;Owens C;Wysoczynski CL;Nitz MD;Knabe WE;Ahmed M;Brautigan DL;Paschal BM;Schwartz MA;Jones DN;Ross D;Meroueh SO;Theodorescu D Nature. 2014 Nov 20;515(7527):443-7. doi: 10.1038/nature13713. Epub 2014 Sep 14.
The Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis. Chemicals that block Ral function would be valuable as research tools and for cancer therapeutics. Here we used protein structure analysis and virtual screening to identify drug-like molecules that bind to a site on the GDP-bound form of Ral. The compounds RBC6, RBC8 and RBC10 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 RBC8 derivative BQU57 to RalB was confirmed by isothermal titration calorimetry, surface plasmon resonance and (1)H-(15)N transverse relaxation-optimized spectroscopy (TROSY) NMR spectroscopy. RBC8 and BQU57 show selectivity for Ral relative to the GTPases Ras and RhoA and inhibit tumour xenograft growth to a similar extent to the depletion of Ral using RNA interference. Our results show the utility of structure-based discovery for the development of therapeutics for Ral-dependent cancers.
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CAS 1637739-82-2 BQU57

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