Bu-2743E
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| Category | Enzyme inhibitors |
| Catalog number | BBF-02754 |
| CAS | 88167-28-6 |
| Molecular Weight | 326.30 |
| Molecular Formula | C14H18N2O7 |
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Description
Bu-2743E is a leucine aminopeptidase (LAP) inhibitor originally isolated from Bacillus circulans J725-B93. It inhibits the LAP with an IC50 of 0.51 μg/mL.
Specification
| Synonyms | (2,3-Dihydroxybenzoyl)-L-alanyl-L-threonine |
| IUPAC Name | (2S,3R)-2-[[(2S)-2-[(2,3-dihydroxybenzoyl)amino]propanoyl]amino]-3-hydroxybutanoic acid |
| Canonical SMILES | CC(C(C(=O)O)NC(=O)C(C)NC(=O)C1=C(C(=CC=C1)O)O)O |
| InChI | InChI=1S/C14H18N2O7/c1-6(12(20)16-10(7(2)17)14(22)23)15-13(21)8-4-3-5-9(18)11(8)19/h3-7,10,17-19H,1-2H3,(H,15,21)(H,16,20)(H,22,23)/t6-,7+,10-/m0/s1 |
| InChI Key | XVYSGUYPIMZAAK-PJKMHFRUSA-N |
Properties
| Appearance | White Amorphous Solid |
| Boiling Point | 680.4°C at 760 mmHg |
| Melting Point | 147-152°C |
| Density | 1.451 g/cm3 |
Reference Reading
1. Mitogenic potentials of bestatin, amastatin, arphamenines A and B, FK-156 and FK-565 on spleen lymphocytes
N Weissmann, G Leyhausen, A Maidhof, W Tanaka, H Umezawa, W E Müller J Antibiot (Tokyo). 1985 Jun;38(6):772-8. doi: 10.7164/antibiotics.38.772.
The following aminopeptidase (AP) activities were found to be associated with the surface of mouse spleen cells: Leu-AP (138 pmol/10(5) cells X minute) and AP-B (16 pmol/10(5) cells X minute with Lys-beta-naphthylamide as substrate and 21 pmol/10(5) cells X minute with Arg-beta-naphthylamide substrate); AP-A activity was not detected by the assay system applied. The immunoactive peptide bestatin inhibited the Leu-AP, while AP-B activity decreased in the presence of both arphamenines A and B and bestatin. No effects on these enzymes were caused by amastatin (an AP-A inhibitor), FK-156, FK-565 and Bu-2743E; the latter peptide turned out to be not an inhibitor of cell surface associated microsomal Leu-AP but an inhibitor of cytosolic Leu-AP. The immunoactive peptides bestatin, arphamenines A and B, and amastatin increased [3H]thymidine incorporation into spleen cells containing lymphocytes and macrophages. These mitogenic actions were not observed when macrophages were removed from the cultures or the cells had been stimulated with ConA or LPS. The lactoyl- and heptanoyl peptides FK-156 and FK-565 caused a mitogenic action on lymphocytes independently of the presence of macrophages. The inhibitor of cytosolic Leu-AP did not change the incorporation into lymphocytes.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
