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Bestatin (Ubenimex) Immunology & Inflammation related inhibitor

Name: Bestatin (Ubenimex)
Brand: Selleck Chemicals
SKU: S1591
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S1591

Bestatin (Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.

Chemical Structure

Molecular Weight: 308.37

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Quality Control

Batch: Purity: 99.87%

99.87

Related Targets	PD-1/PD-L1 CXCR STING AhR CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor
Other Immunology & Inflammation related Inhibitors	Cl-amidine Tempol Tranilast Sinomenine Geniposidic acid GI254023X (GI4023) CORM-3 Acacetin Germacrone Oxymatrine

Solubility

In vitro
Batch:

DMSO : 7 mg/mL (22.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (1.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (1.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	308.37	Formula	C₁₆H₂₄N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	58970-76-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NK421			Smiles	CC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O

Mechanism of Action

Targets/IC₅₀/Ki	Aminopeptidase-N
In vitro	Bestatin (Ubenimex) inhibits proliferation of all the human leukemic cell lines except KG1. It induces DNA fragmentation quantitatively and DNA ladder and enhances caspase-3 activity in U937 cells. This compound dose-dependently induces DNA fragmentation in human leukemic cell lines. It also dose-dependently inhibits the invasion of SN12M cells into reconstituted basement membrane (Matrigel). Bestatin inhibits the degradation of type IV collagen by tumor cells, but not by tumor-conditioned medium (TCM), in a concentration-dependent manner. It inhibits hydrolysing activities towards substrates of aminopeptidases in SN12M cells. The compound inhibits the tube-like formation of human umbilical vein endothelial cells (HUVECs) in vitro. It exerts a direct stimulating effect on lymphocytes (and monocytes) via its fixation on cell surface leucine-aminopeptidase, and an indirect effect on monocytes (and lymphocytes) via aminopeptidase B inhibition of tuftsin catabolism.
In vivo	Bestatin (Ubenimex) significantly inhibits melanoma cell-induced angiogenesis in a mouse dorsal air sac assay and reduces the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice implanted with B16-BL6 melanoma cells. It also statistically significantly inhibits leukotriene B4 biosynthesis in the esophageal tissues of EGDA rats and reduces the incidence of EAC from 57.7% (15 of 26 rats) to 26.1% (6 of 23 rats).
References	[1] https://pubmed.ncbi.nlm.nih.gov/10374877/ [2] https://pubmed.ncbi.nlm.nih.gov/1733647/ [3] https://pubmed.ncbi.nlm.nih.gov/15500947/ [4] https://pubmed.ncbi.nlm.nih.gov/1912369/ [5] https://pubmed.ncbi.nlm.nih.gov/12865451/ [6] https://pubmed.ncbi.nlm.nih.gov/7913090/

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Handling Instructions

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