[CAS NO. 58970-76-6] Bestatin

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PRODUCTS SPECIFICATIONS [58970-76-6]

Catalog

HY-B0134

Brand

MCE

CAS

58970-76-6

DESCRIPTION [58970-76-6]

Overview

MDL	MFCD00083262
Molecular Weight	308.37
Molecular Formula	C16H24N2O4
SMILES	CC(C)C[C@@H](C(O)=O)NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

Summary

Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects ^[1] ^[2] .

In Vitro

Bestatin enhances ATRA-induced differentiation and inhibits ATRA-driven phosphorylation of p38 MAPK in ATRA-sensitive APL NB4 cells. Bestatin can not reverse the differentiation block in ATRA-resistant APL MR2 cells. CD13 ligation with anti-CD13 antibody WM-15 results in phosphorylation of p38 MAPK, reduces the inhibition of Bestatin on the phosphorylation of p38 MAPK, and completely abolishes the enhancement of Bestatin on ATRA-inducing differentiation in NB4 cells ^[2] . Bestatin (600 μM)-treated cells progress slower through the cell cycle due to decreased rate of cell growth and the frequency of cell division. Bestatin inhibits the frequency of mitosis and the inherent multinuclearity in D. discoideum, and is not cytotoxic to D. discoideum cells at 0-600 μM. Bestatin inhibits aminopeptidase activity in lysates of PsaA-GFP- and GFP-expressing cells by 69.39% and 39.93% of control, respectively ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bestatin (20 μM) significantly reduces CD13 expression in diabetic mice and results a significant inhibition of MMP-9 specific gelationolytic band densities compared to diabetic vehicle-treated mice. Bestatin treatment significantly inhibits the expression of VEGF and heparanase in diabetic mice. Intravitreal bestatin treatment significantly downregulates the expression of both HIF-1α and VEGF in diabetic mice retinas. Furthermore, the upregulated expression of heparanase in diabetic mice retinas is significantly inhibited by intravitreal bestatin treatment ^[1] . Bestatin (10, 1, and 0.1mg/kg, i.p.) treatment before the antigen-potentiated humoral response to SRBC results in an increased number of splenocytes producing hemolytic anti-SRBC antibodies (PFC) and the 2-ME-resistant serum hemagglutinin titer (at a dose of 0.1 mg/kg). Bestatin (1 and 0.1 mg/kg) administered to mice five times on alternate days after cyclophosphamide injection does not change the suppressive effect of the drug regarding the number of PFC, and even causes the further decrease of the total anti-SRBC hemagglutinins at dose of 1 mg/kg on day 7 after antigen stimulation ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02736149	Eiger BioPharmaceuticals	Pulmonary Arterial Hypertension	December 2016	Phase 2
NCT02700529	Eiger BioPharmaceuticals	Lymphedema	June 2016	Phase 2
NCT02664558	Eiger BioPharmaceuticals	Pulmonary Arterial Hypertension	April 2016	Phase 2

Appearance

Solid

Source

Streptomyces olivoreticuli

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL ( 27.01 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2429 mL	16.2143 mL	32.4286 mL
5 mM	0.6486 mL	3.2429 mL	6.4857 mL
10 mM	0.3243 mL	1.6214 mL	3.2429 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.83 mg/mL (2.69 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.83 mg/mL (2.69 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 0.83 mg/mL (2.69 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

L-Leucine, N-[(2S,3R)-3-amino-2-hydroxy-1-oxo-4-phenylbutyl]-

L-Leucine, N-(3-amino-2-hydroxy-1-oxo-4-phenylbutyl)-, [S-(R*,S*)]-

N-[(2S,3R)-3-Amino-2-hydroxy-1-oxo-4-phenylbutyl]-L-leucine

Bestatin

NK 421

Ubenimex

(-)-Bestatin

NSC 265489