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CID-1067700
competitive inhibitor of nucleotide binding by Ras-related GTPases

Catalog No.C4819
Size Price Stock Qty
5mg
$80.00
In stock
10mg
$144.00
In stock
25mg
$319.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

CID-1067700

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Chemical Properties

Cas No. 314042-01-8 SDF Download SDF
Synonyms ML-282
Chemical Name 2-[[(benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-5H-thieno[2,3-c]pyran-3-carboxylic acid
Canonical SMILES O=C(NC(NC1=C(C(O)=O)C(CC(C)(C)OC2)=C2S1)=S)C3=CC=CC=C3
Formula C18H18N2O4S2 M.Wt 390.5
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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.