Biological Activity
CXCR4 allosteric agonist (EC50 = 194 nM). Induces chemotaxis in CXCR4-expressing cells in vitro. Mobilizes polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) from bone marrow niche in vivo. Exhibits biased signaling towards Gi proteins over G13 and β-arrestin.
Technical Data
M. Wt | 2256.82 |
Formula | C104H178N26O25S2 |
Sequence | MGYQKKLRSMTDKYRL (Modifications: Met-1 = N-terminal Palmitoyl) |
Storage | Store at -20°C |
CAS Number | 1337878-62-2 |
PubChem ID | 101961246 |
InChI Key | YMLOFEANRZSEGQ-QNHYGVTPSA-N |
Smiles | CCCCCCCCCCCCCCCC(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 2256.82. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
1 mM | 0.44 mL | 2.22 mL | 4.43 mL |
5 mM | 0.09 mL | 0.44 mL | 0.89 mL |
10 mM | 0.04 mL | 0.22 mL | 0.44 mL |
50 mM | 0.01 mL | 0.04 mL | 0.09 mL |
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References are publications that support the products\' biological activity.
Tchernychev et al (2010) Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells. Proc.Natl.Acad.Sci.U.S.A. 107 22255 PMID: 21139054
Planesas et al (2015) Studying the binding interactions of allosteric agonists and antagonists of the CXCR4 receptor. J.Mol.Graph Model. 60 1 PMID: 26080355
Quoyer et al (2013) Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein. Proc.Natl.Acad.Sci.U.S.A. 110 E5088 PMID: 24309376
Keywords: ATI 2341, supplier, CXCR4, allosteric, agonists, polymorphonuclear, neutrophils, PMNs, hematopoietic, stem, progenitor, cells, HSPCs, biased, signaling, Chemokine, CXC, Receptors, Chemokine, CXC, Receptors, Tocris Bioscience