Bestatin | 58970-76-6

Bestatin Properties

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

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

	0
2		0

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

Product number	Packaging	Price	Buy
200484-M	200484-10MG	₹16670.01	Buy
200484-M	200484-10MG	₹16670.01	Buy
200484-M	200484-500MG	₹883597.12	Buy
200484-M	200484-500MG	₹883597.12	Buy
200484-M	200484-250MG	₹1611522.08	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 (K_app = 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

(2S,3R)-3-(((Benzyloxy)carbonyl)aMino)-2-hydroxy-4-phenylbutanoic acid

Preparation Products

Bestatin Suppliers

Global( 402)Suppliers

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

Supplier	Advantage
A.J Chemicals	58
CLEARSYNTH LABS LTD.	58
TCI Chemicals (India) Pvt. Ltd.	58
Alfa Aesar	58
Pharmaffiliates Analytics and Synthetics P. Ltd	58
Pharma Affiliates	58
Shivam Pharma Chemicals	58
Clearsynth Labs	58
Chengdu Aslee Biopharmaceuticals, Inc.	58
Henan Tianfu Chemical Co.,Ltd.	55

Bestatin Spectrum

Bestatin(58970-76-6)¹HNMR Bestatin(58970-76-6)IR

58970-76-6(Bestatin)Related Search:

Tris(hydroxymethyl)aminomethane N-CARBOBENZOXY-DL-LEUCINE ALTRENOGEST 6-Aminocaproic acid mecysteine

CHLOROPHOSPHONAZO III Glycine L-tert-Leucine N-(2-HYDROXYETHYL)LACTAMIDE BESTATIN HYDROCHLORIDE

H-BETA-ALA-LEU-OH H-BETA-ALA-ALA-OH (-)-N-[(2S, 3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTYRYL]-L-LEUCINE METHYL ESTER THREO-(2RS)-3-ACETYLAMINO-2-HYDROXY-4-OXO-4-PHENYLBUTYRIC ACID [UBENIMEX INTERMEDIATE] Bestatin

AMINO ACIDS Ubenimex,AntitumorDrug H-BETA-ALA-DL-LEU-OH

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UbenaMix, Inobestin, NK 421 L-Leucine,N-[(2S,3R)-3-aMino-2-hydroxy-1-oxo-4-phenylbutyl]- N-[(2S,3R)-3-AMino-2-hydroxy-4-phenylbutyryl]-L-leucine 97% 3-(r)-amino-2-(s)-hydroxy-4-phenylbutanoyl-(s)-leucine n-(3-amino-2-hydroxy-1-oxo-4-phenylbutyl)-,(s-(r*,s*))-l-leucin nk421 N-[(2S,3R)-3-AMINO-2-HYDROXY-1-OXO-4-PHENYLBUTYL]-L-LEUCINE N-((2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTYRYL)-L-LEUCINE [(2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTYRYL]-L-LEUCINE [(2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTANOYL]-LEU [(2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTANOYL]-LEU-OH [(2S, 3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTANOYL]-L-LEUCINE BESTATIN BENIMEX L-Leucine, N-(3-amino-2-hydroxy-1-oxo-4-phenylbutyl)-, [S-(R*,S*)]- L-Leucine, N-[(2S,3R)-3-amino-2-hydroxy-1-oxo-4-phenylbutyl]- (9CI) NSC 265489 [S-(R*,S*)]-N-(3-Amino-2-hydroxy-1-oxo-4-phenylbuty1)-L-leucine [S-(R*,S*)]-N-(3-amino-2-hydroxy-4-phenylbutyroyl)-L-leucine N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-L-leucine N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine,97% UbeniMex(Bestatin) N-[(2S,3R)-3-AMino-2-hydroxy-4-phenylbutyryl]-L-leucine, 97% 500MG Bestatin, UbeniMex (2R)-2-[(2S,3R)-3-aMino-2-hydroxy-4-phenylbutanaMido]-4-Methylpentanoic acid (S)-2-((2S,3R)-3-aMino-2-hydroxy-4-phenylbutanaMido)-4-Methylpentanoic acid N-[(2S,3R)-3-AMino-2-hydroxy-4-phenylbutyryl]-L-leucine|(-)-N-[3(R)-AMino-2(S)-hydroxy-4-phenylbutyryl]-L-leucine [S-(R*,S*)]-N-(3-Amino-2-hydroxy-1-oxo-4-phenylbutyl)-L-leucine Bestatin, >=99% N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine≥ 98% (HPLC) Bestatin - CAS 58970-76-6 - Calbiochem Bestatin free base Bestatin-d5 (Ubenimex-d5) Ubenimex Ubenimex Bestatin USP/EP/BP Bestatin D10 UBENIMEX DIBUTYL CARBONATE 542-52-9 Bestatin Impurity 58970-76-6 C16H24N2O4 CH32CHCH2CHNHCOCHOHCHNH2CH2C6H5CO2H Leucine Derivatives Peptide Synthesis Specialty Synthesis Unnatural Amino Acid Derivatives ProteaseInhibitors Ubenimex Pepetides Active Pharmaceutical Ingredients peptides Bestatin API