PDZ1 Domain inhibitor peptideDisrupts interaction between GluR6 and PSD-95 PDZ1 domain CAS# 1315378-73-4 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 1315378-73-4 | SDF | Download SDF |
| PubChem ID | 90488746 | Appearance | Powder |
| Formula | C38H61N9O11 | M.Wt | 819.95 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 1 mg/ml in 5% acetonitrile / water and to 4 mg/ml in DMSO | ||
| Sequence | YKKTEAV (Modifications: Ala-6 = β-Ala, Cyclized = Lys-3 - Ala-6)) | ||
| Chemical Name | (2S)-2-[[(2S)-2-[[(2S,5S,14S)-14-[[(2S)-6-amino-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-2-[(1R)-1-hydroxyethyl]-3,8,15-trioxo-1,4,9-triazacyclopentadecane-5-carbonyl]amino]propanoyl]amino]-3-methylbutanoic acid | ||
| SMILES | CC(C)C(C(=O)O)NC(=O)C(C)NC(=O)C1CCC(=O)NCCCCC(C(=O)NC(C(=O)N1)C(C)O)NC(=O)C(CCCCN)NC(=O)C(CC2=CC=C(C=C2)O)N | ||
| Standard InChIKey | XXRRADBJCXMGOW-RMLJCASOSA-N | ||
| Standard InChI | InChI=1S/C38H61N9O11/c1-20(2)30(38(57)58)46-32(51)21(3)42-34(53)28-15-16-29(50)41-18-8-6-10-27(36(55)47-31(22(4)48)37(56)45-28)44-35(54)26(9-5-7-17-39)43-33(52)25(40)19-23-11-13-24(49)14-12-23/h11-14,20-22,25-28,30-31,48-49H,5-10,15-19,39-40H2,1-4H3,(H,41,50)(H,42,53)(H,43,52)(H,44,54)(H,45,56)(H,46,51)(H,47,55)(H,57,58)/t21-,22+,25-,26-,27-,28-,30-,31-/m0/s1 | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Novel cyclic peptide that disrupts interaction between GluK2 (formerlyy GluR6) and the postsynaptic density protein 95 (PSD-95). Competes with the C-terminus of GluK2 for binding to the PDZ1 domain of PSD-95. Inhibits clustering of kainate receptors. |
PDZ1 Domain inhibitor peptide Dilution Calculator
PDZ1 Domain inhibitor peptide Molarity Calculator
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Targeting specific PDZ domains of PSD-95; structural basis for enhanced affinity and enzymatic stability of a cyclic peptide.[Pubmed:15123241]
Chem Biol. 2004 Apr;11(4):469-73.
A cyclic peptide, Tyr-Lys-c[-Lys-Thr-Glu(betaAla)-]-Val, incorporating a beta-Ala lactam side chain linker and designed to target the PDZ domains of the postsynaptic density protein 95 (PSD-95), has been synthesized and structurally characterized by NMR while free and bound to the PDZ1 domain of PSD-95. While bound, the lactam linker of the peptide makes a number of unique contacts outside the canonical PDZ binding motif, providing a novel target for PDZ-domain specificity as well as producing a 10-fold enhancement in binding affinity. Additionally, the cyclization greatly enhances the enzymatic stability, increasing the duration that the peptide inhibits the association between PSD-95 and glutamate receptors, effectively inhibiting the clustering of kainate receptors for over 14 hr after application. Highly specific regulation of kainate receptor action may provide a novel route for treatment of drug addiction and epilepsy.
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