Bestatin
![Bestatin Structure](CAS/GIF/58970-76-6.gif)
- CAS No.
- 58970-76-6
- Chemical Name:
- Bestatin
- Synonyms
- UBENIMEX;nk421;BENIMEX;BESTATIN;NSC 265489;Bestatin D10;Bestatin, >=99%;Ubenimex Ubenimex;Bestatin Impurity;UbeniMex(Bestatin)
- CBNumber:
- CB9324019
- Molecular Formula:
- C16H24N2O4
- Molecular Weight:
- 308.37
- MOL File:
- 58970-76-6.mol
- Modify Date:
- 2024/3/16 16:45:53
Melting point | 245 °C (dec.)(lit.) |
---|---|
alpha | D20 -15.5° (c = 1.0 in 1N HCl) |
Boiling point | 448.76°C (rough estimate) |
Density | 1.0917 (rough estimate) |
refractive index | 1.5800 (estimate) |
storage temp. | Keep in dark place,Sealed in dry,Room Temperature |
solubility | Aqueous Acid (Slightly, Sonicated), DMSO (Slightly, Heated) |
pka | 8.1, 3.1(at 25℃) |
form | Powder |
color | White |
optical activity | [α]20/D 11°, c = 1 in 1 M NaOH |
Water Solubility | Soluble in water (<1 25), DMSO (2 mg/ml), methanol (5 mg/ml), 1eq. NaOH (50 mM), ethanol (<1 mg/ml at 25°C), acetic acid, aq. HCl, and alkaline solution. Insoluble in ethyl acetate, benzene, hexane, and chloroform. |
Merck | 13,9910 |
InChIKey | VGGGPCQERPFHOB-RDBSUJKOSA-N |
CAS DataBase Reference | 58970-76-6(CAS DataBase Reference) |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H315-H319-H335 | |||||||||
Precautionary statements | P264b-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P362+P364-P403+P233-P501c | |||||||||
Safety Statements | 22-24/25 | |||||||||
WGK Germany | 3 | |||||||||
RTECS | OH2915000 | |||||||||
HS Code | 29242998 | |||||||||
Toxicity | LD50 in male, female mice, male, female rats (g/kg): 1.3, 1.9, 1.9, 2.1 s.c.; 0.19, 0.19, 0.90, 0.78 i.p.; >4.0, >4.0, >2.0, >2.0 orally (Sakakibara) | |||||||||
NFPA 704 |
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Bestatin price More Price(13)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | 200484-M | Bestatin - CAS 58970-76-6 - Calbiochem Binds to cell surfaces and inhibits surface aminopeptidases, notably aminopeptidase B and leucine aminopeptidase. | 58970-76-6 | 200484-10MG | ₹16670.01 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | 200484-M | Bestatin - CAS 58970-76-6 - Calbiochem Binds to cell surfaces and inhibits surface aminopeptidases, notably aminopeptidase B and leucine aminopeptidase. | 58970-76-6 | 200484-10MG | ₹16670.01 | 2022-06-14 | Buy |
Sigma-Aldrich | 200484-M | Bestatin - CAS 58970-76-6 - Calbiochem Binds to cell surfaces and inhibits surface aminopeptidases, notably aminopeptidase B and leucine aminopeptidase. | 58970-76-6 | 200484-500MG | ₹883597.12 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | 200484-M | Bestatin - CAS 58970-76-6 - Calbiochem Binds to cell surfaces and inhibits surface aminopeptidases, notably aminopeptidase B and leucine aminopeptidase. | 58970-76-6 | 200484-500MG | ₹883597.12 | 2022-06-14 | Buy |
Sigma-Aldrich | 200484-M | Bestatin - CAS 58970-76-6 - Calbiochem Binds to cell surfaces and inhibits surface aminopeptidases, notably aminopeptidase B and leucine aminopeptidase. | 58970-76-6 | 200484-250MG | ₹1611522.08 | 2022-06-14 | Buy |
Bestatin Chemical Properties,Uses,Production
Description
Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli. It inhibits aminopeptidase B (IC50 = 0.05 μg/ml), aminopeptidase N (IC50 = 16.9 μM), leucine aminopeptidase (IC50 = 0.01 μg/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM). It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin. Bestatin inhibits the production of LTB4 in erythrocytes when used at a concentration of 70 μM. It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells. Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.
Chemical Properties
white powder, soluble in methanol, ethanol, DMSO and other organic solvents, from Streptomyces olivoreticuli.
Uses
Ubenimex (also known as bestatin) is a competitive aminopeptidase B inhibitor with an IC50 of 100 mg/ml for K562 cells. Proliferation of all the cell lines except KG1 was inhibited by bestatin. P39/TSU, HL60 and U937 were highly sensitive, with 50% growth inhibitory concentration. It is useful in the treatment of non-lymphocytic leukemia. In other types of cancers ubenimex added to radiotherapy or chemotherapy following surgery significantly inmases survival time through immunopotentiation. It is being studied for use in the treatment of acute myelocytic leukemia.
General Description
Bestatin was found in the culture broth of Streptomyces olivoreticuli in 1976by Umezawa et al. in the course of screening specific enzyme inhibitors of microbial origin. It shows inhibitory activity against specific exopeptidases, e.g., aminopeptidase B and leucine aminopeptidase. However, it does not act against aminopeptidase A, carboxypeptidases A and B, or endopeptidases. Bestatin acts as a bioresponse modifier and shows antitumor activity via stimulation of immuno response in the host. In combination with cytotoxic anticancer drugs, it is now under clinical evaluation for use in cancer therapy.
Biological Activity
Aminopeptidase inhibitor (K i = 0.001-90 mM); inhibits enkephalin metabolism and leukotriene A 4 hydrolase. Inhibits tumor cell proliferation.
Safety Profile
Poison by intraperitoneal route.Moderately toxic by subcutaneous route. Experimentalreproductive effects. When heated to decomposition itemits toxic fumes of NOx.
Bestatin Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
TCI Chemicals (India) Pvt. Ltd. | 1800 425 7889 | New Delhi, India | 6778 | 58 | Inquiry |
Alfa Aesar | 1 800 209 7001 | Maharashtra, India | 6913 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
Shivam Pharma Chemicals | 91-22-26403900 | Maharashtra, India | 656 | 58 | Inquiry |
Clearsynth Labs | 91-22-45045900 | Maharashtra, India | 3889 | 58 | Inquiry |
Chengdu Aslee Biopharmaceuticals, Inc. | 28-85305008 | CHINA | 964 | 58 | Inquiry |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21668 | 55 | Inquiry |
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