Cat. No.: HY-B0134

Bestatin

(Synonyms: Ubenimex)

12 Cited Publications

Customer Review

Based on 12 publication(s) in Google Scholar

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

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

Purity: 99.98%
CAS No.: 58970-76-6
Formula: C₁₆H₂₄N₂O₄
Molecular Weight:308.37

Storage:

4°C, sealed storage, away from moisture

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

Bestatin Chemical Structure

CAS No.: 58970-76-6

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target^[1]^[2]^[3]^[4]

CD13

IAP

cIAP1

All Aminopeptidase Isoforms :

CD13
LTA4H

All Antibiotic Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	512.9 μM Compound: Bestatin	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 22901392]
A549	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 27322756]
A549	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 27670098]
A549	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 29202398]
A549	IC₅₀	15.93 μM Compound: 1	Antiproliferative activity against human A549 cells in presence of 5-FU after 48 hrs by MTT assay Antiproliferative activity against human A549 cells in presence of 5-FU after 48 hrs by MTT assay	[PMID: 29202398]
A549	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 29859750]
A549	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 30737134]
AGS	IC₅₀	>200 μM Compound: Bestatin	Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 34917257]
B16-BL6	GI₅₀	>500 μM Compound: Bestatin	Cytotoxicity against mouse B16-BL6 cells assessed as cell growth inhibition after 24 hrs by MTT assay Cytotoxicity against mouse B16-BL6 cells assessed as cell growth inhibition after 24 hrs by MTT assay	[PMID: 24900417]
ES-2	IC₅₀	>500 μM Compound: Bestatin	Cytotoxicity against human ES2 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human ES2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
HCT-116	IC₅₀	>1000 μM Compound: Bestatin	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 22901392]
HCT-116	IC₅₀	315.25 μM Compound: 1; Ube	Antiproliferative activity against human HCT-116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells after 48 hrs by MTT assay	[PMID: 27322756]
HCT-116	IC₅₀	42.54 μM Compound: Bestatin	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by WST1 assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by WST1 assay	[PMID: 28065501]
HCT-116	IC₅₀	357.61 μM Compound: 1	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 29202398]
HCT-116	IC₅₀	44.06 μM Compound: 1	Antiproliferative activity against human HCT116 cells in presence of 5-FU after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells in presence of 5-FU after 48 hrs by MTT assay	[PMID: 29202398]
HCT-116	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 29859750]
HEL	IC₅₀	416.65 μM Compound: 1; Ube	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 27322756]
HEL	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 27670098]
HeLa	IC₅₀	154.9 μM Compound: Bestatin	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	[PMID: 22901392]
HeLa	IC₅₀	>100 μM Compound: Bestatin	Inhibition of HDAC1/HDAC2 in human HeLa cells nuclear extract preincubated for 5 mins before Boc-Lys (acetyl)-AMC substrate addition for 30 mins by microplate reader analysis Inhibition of HDAC1/HDAC2 in human HeLa cells nuclear extract preincubated for 5 mins before Boc-Lys (acetyl)-AMC substrate addition for 30 mins by microplate reader analysis	[PMID: 26629857]
HeLa	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 27322756]
HeLa	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 27670098]
HepG2	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 27322756]
HepG2	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 29202398]
HepG2	IC₅₀	14.52 μM Compound: 1	Antiproliferative activity against human HepG2 cells in presence of 5-FU after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells in presence of 5-FU after 48 hrs by MTT assay	[PMID: 29202398]
HepG2	IC₅₀	>500 μM Compound: Bestatin	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
HL-60	IC₅₀	1.65 mM Compound: Bestatin	Antiproliferative activity against human HL-60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL-60 cells after 48 hrs by MTT assay	[PMID: 18996018]
HL-60	IC₅₀	0.92 mM Compound: Bestatin	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 19299146]
HL-60	IC₅₀	1.65 mM Compound: bestatin	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 19423354]
HL-60	IC₅₀	245 μM Compound: Bestatin	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 19683842]
HL-60	IC₅₀	0.92 mM Compound: bestatin	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 19782572]
HL-60	IC₅₀	1.13 mM Compound: Bestatin	Cytotoxicity against human HL60 cells expressing aminopeptidase N after 72 hrs by MTT assay Cytotoxicity against human HL60 cells expressing aminopeptidase N after 72 hrs by MTT assay	[PMID: 20637634]
HL-60	IC₅₀	1.34 mM Compound: Bestatin	Antiproliferative activity against human HL60 cells expressing high levels of APN after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells expressing high levels of APN after 48 hrs by MTT assay	[PMID: 21802307]
HL-60	IC₅₀	22.89 μM Compound: Bestatin	Inhibition of APN in human HL60 cells assessed as hydrolysis of L-Leu-p-nitroanilide by spectrophotometry Inhibition of APN in human HL60 cells assessed as hydrolysis of L-Leu-p-nitroanilide by spectrophotometry	[PMID: 21802307]
HL-60	IC₅₀	245 μM Compound: Bestatin	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 22206607]
HL-60	IC₅₀	86.4 μM Compound: Bestatin	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 22901392]
HL-60	EC₅₀	>100 μM Compound: 2	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 28803047]
HUVEC	IC₅₀	>2000 μM Compound: 1	Antiproliferative activity against HUVEC after 48 hrs by MTT assay Antiproliferative activity against HUVEC after 48 hrs by MTT assay	[PMID: 30737134]
K562	IC₅₀	135.6 μM Compound: Bestatin	Cytotoxicity against human K562 cells after 48 hrs by MTT assay Cytotoxicity against human K562 cells after 48 hrs by MTT assay	[PMID: 22901392]
K562	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 27670098]
K562	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 29859750]
K562	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30737134]
K562	IC₅₀	>500 μM Compound: Bestatin	Cytotoxicity against human K562 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human K562 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
KG-1	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay	[PMID: 27322756]
KG-1	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay Antiproliferative activity against human KG1 cells after 48 hrs by MTT assay	[PMID: 27670098]
MCF7	IC₅₀	>1000 μM Compound: Bestatin	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 22901392]
MCF7	IC₅₀	541 μM Compound: Bestatin	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by resazurin dye-based fluorimetric analysis Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by resazurin dye-based fluorimetric analysis	[PMID: 27253989]
MCF7	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 27322756]
MCF7	IC₅₀	149.6 μM Compound: Bestatin	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 27624521]
MCF7	IC₅₀	>200 μM Compound: Bestatin	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 34917257]
MDA-MB-231	IC₅₀	8.59 mM Compound: Bestatin	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 20637634]
MDA-MB-231	IC₅₀	5.08 mM Compound: Bestatin	Antiproliferative activity against human MDA-MB-231 cells expressing low levels of APN after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells expressing low levels of APN after 48 hrs by MTT assay	[PMID: 21802307]
MDA-MB-231	IC₅₀	753.18 μM Compound: Bestatin	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 21911297]
MDA-MB-231	IC₅₀	50.6 μM Compound: Bestatin	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 22901392]
MDA-MB-231	IC₅₀	50.6 μM Compound: Bestatin	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 23510562]
MDA-MB-231	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 27322756]
MDA-MB-231	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 27670098]
MDA-MB-231	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 29859750]
MOLT-4	IC₅₀	>100 μg/mL Compound: Bestatin	Inhibitory activity against aminopeptidase N (APN) in human acute lymphoblastic leukemia MOLT-4 cell line Inhibitory activity against aminopeptidase N (APN) in human acute lymphoblastic leukemia MOLT-4 cell line	[PMID: 10098663]
MOLT-4	IC₅₀	>100 μg/mL Compound: Bestatin	Inhibitory activity against Dipeptidylpeptidase IV (DPP IV) in human acute lymphoblastic leukemia MOLT-4 cell line Inhibitory activity against Dipeptidylpeptidase IV (DPP IV) in human acute lymphoblastic leukemia MOLT-4 cell line	[PMID: 10098663]
MOLT-4	IC₅₀	>324.3 μM Compound: Bestatin	Inhibitory activity against Dipeptidylpeptidase IV (DPP IV) in human acute lymphoblastic leukemia MOLT-4 cell line Inhibitory activity against Dipeptidylpeptidase IV (DPP IV) in human acute lymphoblastic leukemia MOLT-4 cell line	[PMID: 10098663]
MOLT-4	IC₅₀	>471.6 μM Compound: Bestatin	Inhibitory activity against aminopeptidase N (APN) in human acute lymphoblastic leukemia MOLT-4 cell line Inhibitory activity against aminopeptidase N (APN) in human acute lymphoblastic leukemia MOLT-4 cell line	[PMID: 10098663]
MOLT-4	EC₅₀	>100 μM Compound: 2	Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay	[PMID: 28803047]
MV4-11	IC₅₀	>20 μM Compound: Bestatin	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by resazurin based microplate reader analysis Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by resazurin based microplate reader analysis	[PMID: 37647727]
NB-4	IC₅₀	220.9 μM Compound: Bestatin	Cytotoxicity against human NB4 cells after 48 hrs by MTT assay Cytotoxicity against human NB4 cells after 48 hrs by MTT assay	[PMID: 22901392]
NCI-H1975	IC₅₀	>200 μM Compound: Bestatin	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 34917257]
NIH3T3	IC₅₀	>1000 μM Compound: Bestatin	Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay	[PMID: 22901392]
PC-3	IC₅₀	399.4 μM Compound: Bestatin	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 22901392]
PC-3	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay	[PMID: 27322756]
PC-3	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay	[PMID: 27670098]
PC-3	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 29859750]
PC-3	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 30737134]
PC-3	IC₅₀	>500 μM Compound: Bestatin	Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
PLC	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human PLC cells after 48 hrs by MTT assay Antiproliferative activity against human PLC cells after 48 hrs by MTT assay	[PMID: 29859750]
PLC	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human PLC cells after 48 hrs by MTT assay Antiproliferative activity against human PLC cells after 48 hrs by MTT assay	[PMID: 30737134]
PLC-PRF-5	IC₅₀	>500 μM Compound: 1; Ube	Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay	[PMID: 27322756]
PLC-PRF-5	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay Antiproliferative activity against human PLC-PRF-5 cells after 48 hrs by MTT assay	[PMID: 27670098]
PLC-PRF-5	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human PLC/PRF/5 cells after 48 hrs by MTT assay Antiproliferative activity against human PLC/PRF/5 cells after 48 hrs by MTT assay	[PMID: 29202398]
PLC-PRF-5	IC₅₀	22.81 μM Compound: 1	Antiproliferative activity against human PLC/PRF/5 cells in presence of 5-FU after 48 hrs by MTT assay Antiproliferative activity against human PLC/PRF/5 cells in presence of 5-FU after 48 hrs by MTT assay	[PMID: 29202398]
PLC-PRF-5	IC₅₀	>500 μM Compound: Bestatin	Cytotoxicity against human PLC-PRF-5 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human PLC-PRF-5 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
SK-OV-3	IC₅₀	>1000 μM Compound: Bestatin	Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay	[PMID: 22901392]
U-266	IC₅₀	>500 μM Compound: Ubenimex	Antiproliferative activity against human U266 cells after 48 hrs by MTT assay Antiproliferative activity against human U266 cells after 48 hrs by MTT assay	[PMID: 27670098]
U-266	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human U266 cells after 48 hrs by MTT assay Antiproliferative activity against human U266 cells after 48 hrs by MTT assay	[PMID: 29202398]
U-266	IC₅₀	43.48 μM Compound: 1	Antiproliferative activity against human U266 cells in presence of 5-FU after 48 hrs by MTT assay Antiproliferative activity against human U266 cells in presence of 5-FU after 48 hrs by MTT assay	[PMID: 29202398]
U-937	IC₅₀	>1000 μM Compound: Bestatin	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay Antiproliferative activity against human U937 cells after 48 hrs by MTT assay	[PMID: 23453219]
U-937	IC₅₀	142.63 μM Compound: Ubenimex	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay Antiproliferative activity against human U937 cells after 48 hrs by MTT assay	[PMID: 27670098]
U-937	IC₅₀	142.63 μM Compound: 1	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay Antiproliferative activity against human U937 cells after 48 hrs by MTT assay	[PMID: 29202398]
U-937	IC₅₀	9.56 μM Compound: 1	Antiproliferative activity against human U937 cells in presence of 5-FU after 48 hrs by MTT assay Antiproliferative activity against human U937 cells in presence of 5-FU after 48 hrs by MTT assay	[PMID: 29202398]
U-937	IC₅₀	>500 μM Compound: 1	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay Antiproliferative activity against human U937 cells after 48 hrs by MTT assay	[PMID: 29859750]
U-937	IC₅₀	>500 μM Compound: Bestatin	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
Vero	CC₅₀	≥25 μM Compound: 2	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 28803047]
Vero	CC₅₀	25 μM Compound: 5	Cytotoxicity against African green monkey Vero cells by MTT assay Cytotoxicity against African green monkey Vero cells by MTT assay	[PMID: 38917665]

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].

MedChemExpress (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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 58970-76-6
Appearance Solid
Molecular Weight 308.37
Formula C₁₆H₂₄N₂O₄
Color White to off-white
SMILES

CC(C)C[C@@H](C(O)=O)NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O
Synonyms

Ubenimex
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Microorganisms
Streptomyces olivoreticuli
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Publications (12)

All WBCell Proliferation/Viability AssayBio/Physico-chemical AssayHistological Imaging/Staining

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Cancer Res

tRF-21LeuTAA Promotes Oxidative Stress by Altering Glutathione Metabolic Enzymes to Support Prostate Cancer Progression. [Abstract]

2025 Aug 29. PMID: 40882020

Bestatin purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Aug 29. [Abstract]

The LAP3 dipeptidase activity inhibitor Bestatin (200-400 μM; 48 h) significantly suppressed LAP3 and AKT enzyme activities and reduced p-mTOR^S2481 and pAKT^S473 levels.

Bestatin purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Aug 29. [Abstract]

The LAP3 dipeptidase activity inhibitor Bestatin (200-400 μM; 48 h) induced a significant increase in intracellular GSH levels and a decrease in GSH degradation products Cys and Gly (resulting from Cys-Gly dipeptidase activity).
Hemasphere

Novel Peptide-drug Conjugate Melflufen Efficiently Eradicates Bortezomib-resistant Multiple Myeloma Cells Including Tumor-initiating Myeloma Progenitor Cells. [Abstract]

2021 Jun 12;5(7):e602. PMID: 34136753

Bestatin purchased from MedChemExpress. Usage Cited in: Hemasphere. 2021 Jun 12;5(7):e602. [Abstract]

Cytotoxicity of 125 and 250 nM melflufen in AMOaBTZ cells in the presence of BST (10 μM).
Cell Mol Gastroenterol Hepatol

Exercise-induced Metabolite N-lactoyl-phenylalanine Ameliorates Colitis by Inhibiting M1 Macrophage Polarization Via the Suppression of the NF-κB Signaling Pathway. [Abstract]

2025 Jun 23:101558. PMID: 40562095

Bestatin purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025 Jun 23:101558. [Abstract]

Western blot analysis of p65, p-p65, I_κB-_α, and p-I_κB-_α in RAW264.7 cells subjected to different treatment conditions. Bestatin (0.4 mM) significantly enhanced LPSinduced p65 phosphorylation, promoted I_κB-_α phosphorylation and degradation.

Bestatin purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025 Jun 23:101558. [Abstract]

Bestatin (50 mg/kg; i.p.; once daily) diminished the anti-inflammatory effects of high phenylalanine intake in mice.
J Med Chem

Discovery of Small-Molecule Degraders for Alpha-Synuclein Aggregates. [Abstract]

2023 Jun 22;66(12):7926-7942. PMID: 37267712
Int J Oncol

Metformin induces TPC-1 cell apoptosis through endoplasmic reticulum stress-associated pathways in vitro and in vivo. [Abstract]

2019 Jul;55(1):331-339. PMID: 31180536
J Med Chem

Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. [Abstract]

2017 Mar 9;60(5):1817-1828. PMID: 28218840
Biochim Biophys Acta Mol Basis Dis

CNDP2 drives renal tubular fibrosis in diabetic kidney disease via a sulfur-containing amino acids-mTOR signaling axis. [Abstract]

2026 Oct;1872(7):168312. PMID: 42276307
J Pharmacol Exp Ther

Thymidine Kinase 1 Mediates the Synergistic Antitumor Activity of Ubenimex and Celecoxib via Regulation of Cell Cycle in Colorectal Cancer. [Abstract]

2022 Aug;382(2):188-198. PMID: 35868865
Toxicol Appl Pharmacol

OAT1/3 regulate the absorption of CP-25 in the rat synovium. [Abstract]

2025 May 4:500:117371. PMID: 40328338
Discov Oncol

Bestatin attenuates breast cancer stemness by targeting puromycin-sensitive aminopeptidase. [Abstract]

2024 May 30;15(1):197. PMID: 38814491
Dis Markers

LTB4 Promotes Acute Lung Injury via Upregulating the PLC ε-1/TLR4/NF- κ B Pathway in One-Lung Ventilation. [Abstract]

2022 Jan 11:2022:1839341. PMID: 35059042

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL (27.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[4]

Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl₂ for 20 min before the fluorometric aminopeptidase assay.

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

Cell Assay^[4]

Growing cells (1×10⁶ to 2×10⁶ cells/mL) are diluted to 1.0×10³ cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h.

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

Animal Administration^[3]

Bestatin is dissolved in PBS. The agent (doses of 10, 1, and 0.1 mg/kg) is injected i.p. to non-cyclophosphamide-treated mice, 5 or 10 times at 24-h intervals before SRBC immunization. The mice are immunized 24 h after the last dose of bestatin. Pharmacological immunosuppression is induced by a single intraperitoneal injection of cyclophosphamide administered at a dose of 350 mg/kg, 12 days before SRBC immunization. Bestatin at the doses of 1 and 0.1 mg/kg is injected to cyclophosphamide-immunosuppressed mice i.p. five times at 48-h intervals or 10 times at 24-h intervals before SRBC immunization. The first dose of bestatin is administered 24 h after cyclophosphamide, while the last dose of the drug is injected 24h before SRBC immunization.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hossain A, et al. Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice. Exp Eye Res. 2016 Aug;149:100-6 [Content Brief]

[2]. Qian X, et al. Inhibition of p38 MAPK Phosphorylation Is Critical for Bestatin to Enhance ATRA-Induced Cell Differentiation in Acute Promyelocytic Leukemia NB4 Cells. Am J Ther. 2016 May-Jun;23(3):e680-9. [Content Brief]

[3]. Lis M, et al. The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice. Immunopharmacol Immunotoxicol. 2013 Feb;35(1):133-8 [Content Brief]

[4]. Poloz Y, et al. Bestatin inhibits cell growth, cell division, and spore cell differentiation in Dictyostelium discoideum. Eukaryot Cell. 2012 Apr;11(4):545-57 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2429 mL	16.2143 mL	32.4286 mL	81.0714 mL
	5 mM	0.6486 mL	3.2429 mL	6.4857 mL	16.2143 mL
	10 mM	0.3243 mL	1.6214 mL	3.2429 mL	8.1071 mL
	15 mM	0.2162 mL	1.0810 mL	2.1619 mL	5.4048 mL
	20 mM	0.1621 mL	0.8107 mL	1.6214 mL	4.0536 mL
	25 mM	0.1297 mL	0.6486 mL	1.2971 mL	3.2429 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Bestatin

Anti-Infection Compound Library

Metabolism/Protease Compound Library

Natural Product Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Peptidomimetic Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Antibacterial Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Microbial Metabolite Library

Rare Diseases Drug Library

Anti-Cancer Natural Product Library

FDA-Approved Anticancer Drug Library

Cancer Stem Cells Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

RO5 Drug-like Natural Product Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Bacteria-Sourced Compound Library

Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Bestatin

All Aminopeptidase Isoforms

All Antibiotic Isoforms

Biological Activity

Chemical Information

Publications (12)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bestatin Related Classifications

HY-B0134 Related Classifications