| Chemical Properties | Back Directory | [Boiling point ]
1380.0±65.0 °C(Predicted) | [density ]
1.381±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C, protect from light | [solubility ]
Soluble to 1 mg/ml in 20% acetonitrile - 0.1% acetic acid | [form ]
Powder | [pka]
4.17±0.10(Predicted) | [color ]
White to off-white | [Sequence]
H-His-Ser-Asp-Val-His-Lys-NH2 |
| Hazard Information | Back Directory | [Uses]
P11 is a useful building block in the synthesis of various pharmaceuticals | [Enzyme inhibitor]
This potent PDZ motif-containing anti-angiogenic agent (FW = 720.78
g/mol; CAS 848644-86-0; Sequence: HSDVHK-NH2) targets the integrin
αvβ3-vitronectin interaction, blocking proliferation and inducing apoptosis in
human vascular endothelial cells (HUVECs). Arg-Gly-Asp (or RGD)
binding-site recognition by P11 is site-specific, showing a strong
antagonism against αvβ3-vitronectin interaction, IC50 = 26 nM. The
binding orientation of docked P11 in αvβ3 is similar to that for RGD,
suggesting a divalent metal-ion coordination is a common driving force for
the formation of both SDV·αvβ3 and RGD·αvβ3 complexes. P11 appears to
inhibit b-Fibroblast Growth Factor (or bFGF) -induced HUVEC
proliferation via mitogen-activated protein kinase kinase and extracellular-
signal regulated kinase inhibition as well as p53-mediated apoptosis related
with activation of caspases. (Note: Consisting of 80-90 amino-acids in
far-flung signaling proteins and binding to short C-terminal regions in
protein interaction partners, “PDZ” is an acronym that includes the first
letters of Post-synaptic density protein (PSD95), Drosophila Dlg1 tumor
suppressor, and Zonula occludens-1 protein (zo-1), the first proteins
discovered to share this domain.) | [IC 50]
αvβ3: 2.74 nM (IC50) | [storage]
-20°C, protect from light |
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BOC Sciences
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| Website: |
https://www.bocsci.com |
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