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CID-1067700

 
Catalog No.
C4819
Ras相关GTP酶核苷酸结合的竞争性抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,220.00
Ship with 10-15 days
10mg
¥ 2,762.00
Ship with 10-15 days
25mg
¥ 4,604.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt390.5
Cas No.314042-01-8
FormulaC18H18N2O4S2
SynonymsML-282
Solubility≤10mg/ml in DMSO
Chemical Name2-[[(benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-5H-thieno[2,3-c]pyran-3-carboxylic acid
SDFDownload SDF
Canonical SMILESO=C(NC(NC1=C(C(O)=O)C(CC(C)(C)OC2)=C2S1)=S)C3=CC=CC=C3
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质量控制

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化学结构

CID-1067700