Apolactoferrin
Apolactoferrin is an iron-binding protein and also an inhibitor of the MMP-2 catalytic domain. Apolactoferrin binds iron and anions at the N-lobe and C-lobe sites. Apolactoferrin N-lobe opening alters inter-lobe contacts/orientation, providing a structural signaling pathway. Apolactoferrin selectively inhibits the MMP-2 catalytic domain fragment, but has weaker inhibitory activity against full-length MMP-2, with a human Kd of 0.72 mM; its temperature-sensitive inhibition is not reversed by iron/calcium, and it does not act on other tested MMPs or puromycin (Puromycin) (HY-B1743)-sensitive aminopeptidases. The bactericidal effect of Apolactoferrin is independent of iron deprivation. Apolactoferrin does not inhibit the growth of fluconazole (Fluconazole) (HY-B0101)-resistant Candida albicans. Apolactoferrin can be used for research on rheumatoid arthritis.
For research use only. We do not sell to patients.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
Description
IC50 & Target
[1]|
MMP-2 |
In Vitro
Apolactoferrin (up to 20 µM; 30 minutes at 37°C) inhibits the 42 kDa catalytic domain of MMP-2, but shows weaker inhibition of the 66 kDa full-length activated MMP-2[1].
Apolactoferrin (3 mmol/L) decreases the Vmax of the MMP-2 catalytic domain for TPL and increases its KM[1].
Apolactoferrin (3 mmol/L) inhibition of the MMP-2 catalytic domain is strongly temperature-dependent, with KD decreasing from 3.3 mmol/L at 29°C to 0.16 mmol/L at 39°C[1].
Apolactoferrin (2-5 mmol/L) inhibition of the MMP-2 catalytic domain is reversed by Zn2+ but not by Fe2+ or Ca2+, consistent with removal of the catalytic zinc ion[1].
Apolactoferrin (12 mg mL-1) forms a 1-691 polypeptide with an open N-lobe (N2 rotated 54.3° relative to N1) and a closed C-lobe, refined at 2.0 Å resolution to R = 0.201/Rfree = 0.286, with two bound Cl- ions in the anion-binding sites[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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SMILES
[Apolactoferrin]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Apolactoferrin Related Classifications
HY-NP0222 Related Classifications
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