CID-1067700
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.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 390.5 |
| Cas No. | 314042-01-8 |
| Formula | C18H18N2O4S2 |
| Synonyms | ML-282 |
| Solubility | ≤10mg/ml in DMSO |
| Chemical Name | 2-[[(benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-5H-thieno[2,3-c]pyran-3-carboxylic acid |
| SDF | Download SDF |
| Canonical SMILES | O=C(NC(NC1=C(C(O)=O)C(CC(C)(C)OC2)=C2S1)=S)C3=CC=CC=C3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity ≥ 95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
