CID-1067700 (Synonyms: ML-282) |
| Katalog-Nr.GC12948 |
CID-1067700 (ML282) ist ein Pan-GTPase-Inhibitor und hemmt kompetitiv Ras-verwandtes in Gehirn 7 (Rab7) mit einem Ki von 13 nM.
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Cas No.: 314042-01-8
Sample solution is provided at 25 µL, 10mM.
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CID-1067700 is the first competitive inhibitor of nucleotide binding by Ras-related GTPases [1].
The Ras superfamily of GTPases, which includes Arf, Rho, Ras and Rab GTPase subfamilies, regulate many cellular processes ranging from membrane trafficking to the control of cell proliferation. Alteration of small GTPase functions is a hallmark of genetic and sporadic human diseases, making GTPase family members attractive targets [1].
CID-1067700 is a competitive inhibitor of nucleotide binding by Ras-related GTPases. CID-1067700 exhibited EC50 values of 20-500 nM and at least 40% inhibitory activity against all tested GTPases. CID-1067700 significantly inhibited Rab GTPases (Rab2 and Rab7). CID 1067700 inhibited Rab7 binding of the BODIPY-linked nucleotides with EC50 values and Ki values of 11.22 ± 1.34 nM and 12.89 nM for BODIPY-GTP, and 20.96 ± 1.34 nM and 19.70 nM for BODIPY-GDP, respectively. The maximal inhibitory response was ≥97% for both nucleotides [1].
Reference:
[1]. Agola JO, Hong L, Surviladze Z, et al. A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition. ACS Chem Biol. 2012 Jun 15;7(6):1095-108.
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