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ChemicalBook >> CAS DataBase List >>[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Structure
[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate structure
CAS No.
150080-09-4
Chemical Name:
[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate
Synonyms
CS-1219;PT100 mesylate;Unii-V8zg4Y1B51;Talabostat mesylate;Talabostat Mesilate;Val-boroPro mesylate;Adrafinil Impurity 6;Talabostat (PT-100) ，S8455;Talabostat-mesylate, PT-100;methanesulfonic acid - [A83080]
CBNumber:
CB52128758
Molecular Formula:
C10H23BN2O6S
Molecular Weight:
310.17
MDL Number:
MFCD13194906
MOL File:
150080-09-4.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-07-27 17:00:41
Product description Number Pack Size Price
Val-boroPro - CAS 150080-09-4 - Calbiochem 5.31465 10mg $286
Talabostat (mesylate) ≥95% 29007 5mg $54
Talabostat (mesylate) ≥95% 29007 10mg $91
Talabostat (mesylate) ≥95% 29007 25mg $209
Talabostat (mesylate) ≥95% 29007 50mg $367
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[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Properties

Melting point >160°C (dec.)
storage temp. under inert gas (nitrogen or Argon) at 2–8 °C
solubility Soluble in DMSO (up to at least 25 mg/ml)
form solid
color White
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
InChI 1S/C9H19BN2O3.CH4O3S/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15;1-5(2,3)4/h6-8,14-15H,3-5,11H2,1-2H3;1H3,(H,2,3,4)/t7-,8-;/m0./s1
InChIKey OXYYOEIGQRXGPI-WSZWBAFRSA-N
SMILES B(O)(O)[C@H]1N(CCC1)C(=O)[C@@H]([N+H3])C(C)C.[S](=O)(=O)([O-])C
NCI Dictionary of Cancer Terms talabostat mesylate
FDA UNII V8ZG4Y1B51
NCI Drug Dictionary talabostat mesylate
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  Exclamation Mark (GHS07)
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501
WGK Germany  WGK 3
Storage Class 11 - Combustible Solids

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate price More Price(74)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 5.31465 Val-boroPro - CAS 150080-09-4 - Calbiochem 150080-09-4 10mg $286 2026-04-30 Buy
Cayman Chemical 29007 Talabostat (mesylate) ≥95% 150080-09-4 5mg $54 2026-04-30 Buy
Cayman Chemical 29007 Talabostat (mesylate) ≥95% 150080-09-4 10mg $91 2026-04-30 Buy
Cayman Chemical 29007 Talabostat (mesylate) ≥95% 150080-09-4 25mg $209 2026-04-30 Buy
Cayman Chemical 29007 Talabostat (mesylate) ≥95% 150080-09-4 50mg $367 2026-04-30 Buy
Product number Packaging Price Buy
5.31465 10mg $286 Buy
29007 5mg $54 Buy
29007 10mg $91 Buy
29007 25mg $209 Buy
29007 50mg $367 Buy

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Chemical Properties,Uses,Production

Description

Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP; IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively). It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs; IC50 = ~10 nM). Talabostat (5 μg twice per day) increases expression of a variety of cytokines, including those encoding IL-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model. It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.

Uses

Treatment of cancer; hematopoetic stimulant.

Uses

Talabostat Mesylate can be used in biological study and pharmacological activity of treatment of cancer using immunomodulation.

General Description

A prolineboronic acid-based broad-spectrum DDP IV activity and/or structural homologue (DASH) family dipeptidyl peptidases inhibitor that converts in solution between the protonated active form and a cyclized inactive form due to a reversible intramolecular B-N dative bond formation of the non-protonated Val-boroPro (kinact = 6.4 x 10--4 s- and kcyc = 6.4 x 10-5 s- at pH 7.8). Although equilibrium favors cyclization at basic pH, high affinity binding (kon & koff toward CD26 at pH 7.8 = 5.02 x 106 M-s- and 77.8 x 10-6 s-, respectively) drives the equilibrium away from cyclization and traps the active form in enzyme-bound state with prolonged incubation. Reported to inhibit DPP7/DPPII/QPP (IC50/[Substrate]/rxn time at pH 5.5 = 15 nM/500 μM Lys-Pro-MNA/1 h & 310 nM/50 μM Nle-Pro-AMC/15 min), CD26/DPPIV (IC50 = 26 nM; 500 μM Ala-Pro-MNA for 1 h at pH 7.8), fibroblast activation protein/FAP (IC50 = 40 nM; 250 μM Ala-Pro-AFC at pH 2.0), DPP8 (IC50 = 4 nM; 100 μM Ala-Pro-AFC for 15 min at pH 8.0), DDP9 (IC50 = 11 nM; 100 μM Gly-Pro-AMC for 30 min at pH 7.4) with little potency against 9 other proteases (IC50 >100 μM; aminopeptidase P, chymoptrypsin, leukocyte elastase, plasma kallikrein, plasmin, prolidase, thrombin, trypsin, tryptase), while contradictory reports regarding prolyl endopeptidase/PEP/PREP inhibition exist (e.g. IC50 = 390 nM/50 μM Z-Gly-Pro-AMC/pH 7.5/30 min vs. 25 μM/500 μM Z-Gly-Pro-MNA/pH 7.8/60 min). Shown to promote the propagation of human BM CD34+ cells by stimulating stromal cells cytokine production in vitro (min EC 0.1 nM) and display hematopoietic stimulatory effect in mice in vivo (min ED 2 μg/mouse/12 h; p.o.). Although orally available in mice and rats, caution must be taken not to exceed toxicity levels (MTD = 25 μg/mL using Sprague-Dawley rats; LD50 ~0.5 mg/mL in 24 survival test using Fisher rats; p.o.) for in vivo studies.

Biochem/physiol Actions

Cell permeable: yes

in vitro

by the cleavage of n-terminal xaa-pro or xaa-ala residues, talabostat blocks dipeptidyl peptidases, such as fibroblast activation protein (fap), resulting in inducing the production of cytokine and chemokine (besides specific t-cell immunity and t-cell-dependent activity). this agent may also induce the production of colony stimulating factors, for instance, granulocyte colony stimulating factor (g-csf), resulting in the inducement of hematopoiesis. dipeptidyl peptidases are referred to the activation of polypeptide hormones and chemokines.

IC 50

1 nm

storage

Store at -20°C

References

[1] PETERS J, MATTEI P. Dipeptidyl Peptidase IV Inhibitors for the Treatment of Type 2 Diabetes[C]. 2010: 0. DOI:10.1002/9783527630035.ch5
[2] SHARLENE ADAMS. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism.[J]. Cancer research, 2004, 64 15: 5471-5480. DOI:10.1158/0008-5472.can-04-0447
[3] MEGHAAN P WALSH. Val-boroPro accelerates T cell priming via modulation of dendritic cell trafficking resulting in complete regression of established murine tumors.[J]. PLoS ONE, 2013: e58860. DOI:10.1371/journal.pone.0058860
[4] MARIAN C OKONDO. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis[J]. Nature chemical biology, 2016, 13 1: 46-53. DOI:10.1038/nchembio.2229
[5] MARIAN C. OKONDO . Inhibition of Dpp8/9 Activates the Nlrp1b Inflammasome[J]. Cell Chemical Biology, 2018, 25 3: Pages 262-267.e5. DOI:10.1016/j.chembiol.2017.12.013

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Preparation Products And Raw materials

Raw materials

Preparation Products

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Suppliers

Global( 150)Suppliers
Supplier Tel Email Country ProdList Advantage
Adachibio Inc. 		+81-8027837258; sales@adachibio.com Japan 938 58
Capot Chemical Co.,Ltd. 		+86-（0）57185586718 +86-13336195806 sales@capot.com China 29626 60
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32998 60
CONIER CHEM AND PHARMA LIMITED 		sales@conier.com China 49906 58
career henan chemical co 		+86-0371-86658258 factory@coreychem.com China 29780 58
Guangzhou Yuheng Pharmaceutical Technology Co., Ltd 		+8613580539051 joe@yuhengpharm.com CHINA 21135 58
TargetMol Chemicals Inc. 		+1-781-999-5354; +1-00000000000 marketing@targetmol.com United States 32431 58
Win-Win chemical CO., Limited 		+86-0086-577-64498589 +86-15355981851 sales@win-winchemical.com China 14301 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1059@dideu.com China 29096 58
Baoji Guokang Healthchem Co., Ltd. 		+86-0917-3909592 +86-13892490616 gksales1@gk-bio.com China 9040 58
Supplier Advantage
Adachibio Inc. 		58
Capot Chemical Co.,Ltd. 		60
ATK CHEMICAL COMPANY LIMITED 		60
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
Guangzhou Yuheng Pharmaceutical Technology Co., Ltd 		58
TargetMol Chemicals Inc. 		58
Win-Win chemical CO., Limited 		58
Dideu Industries Group Limited 		58
Baoji Guokang Healthchem Co., Ltd. 		58

View Lastest Price from [(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Talabostat mesylate pictures 2026-07-27 Talabostat mesylate
150080-09-4
 $50.00-159.00 99.99% 10g TargetMol Chemicals Inc.
[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate pictures 2025-11-18 [(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate
150080-09-4
 $1.10 1g 99.00% 100 Tons Min Dideu Industries Group Limited
Talabostat mesylate pictures 2021-07-13 Talabostat mesylate
150080-09-4
 $10.00-15.00 1KG 99%+ HPLC Zhuozhou Wenxi import and Export Co., Ltd

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Spectrum

[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate(150080-09-4)MS[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate(150080-09-4)1HNMR

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[(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Boronic acid, ((2R)-1-((2S)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-, monomethanesulfonate Unii-V8zg4Y1B51 Methanesulfonic acid ((R)-1-((S)-2-amino-3-methyl-butanoyl)pyrrolidin-2-yl)boronic acid (1:1) Talabostat mesylate Val-boroPro mesylate CS-1219 Talabostat-mesylate, PT-100 Talabostat Mesilate [(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate Talabostat mesilate Talabostat mesylate [(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate [(2R)-1-(L-Valyl)-2-pyrrolidinyl]boronic acid methanesulfonate (1:1) B-[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid methanesulfonate PT100 mesylate (2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronicacid,methanesulfonicaci [(2R)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid mesylate ISO 9001：2015 REACH [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid,methanesulfonic acid (R)-1-[(S)-2-Amino-3-methylbutanoyl]pyrrolidine-2-boronic Acid Methanesulfonate methanesulfonic acid compound with ((R)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid (1:1) Adrafinil Impurity 6 Talabostat mesylate, 10 mM in DMSO Talabostat mesylate (Val-boroPro mesylate Talabostat (PT-100) ，S8455 methanesulfonic acid - [A83080] methanesulfonic acid compound with ((r)-1-(l-valyl)pyrrolidin-2-yl)boronic acid (1:1) 150080-09-4 C10H23BN2O6S C9H19BN2O3CH4O3S