Art. -Nr.: HY-13233

Talabostat

(Synonyms: Val-boroPro; PT100)

42 Cited Publications

Kundenbewertung

Based on 42 publication(s) in Google Scholar

Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC₅₀ < 4 nM; K_i = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC₅₀ = 560 nM), inhibits DPP8/9 (IC₅₀ = 4/11 nM; K_i = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC₅₀ = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.

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CAS. Nr.: 149682-77-9
Formel: C₉H₁₉BN₂O₃
Molecular Weight:214.07

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

Talabostat Chemical Structure

CAS. Nr.: 149682-77-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (42)
Lösungsmittel & Löslichkeit
- In Vitro
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

DPP-4

Alle Dipeptidyl Peptidase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.066 μM Compound: 1, PT-100	Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry	[PMID: 24617858]
HEK293	IC₅₀	0.066 μM Compound: 1, PT-100, Val-boroPro	Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique	[PMID: 22525314]
HEK293	IC₅₀	0.07 μM Compound: 1, PT- 100, Talabostat	Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition	[PMID: 24900696]
HEK-293T	IC₅₀	6.8 μM Compound: 1, Val-boroPro	Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs	[PMID: 18783201]
U-87MG ATCC	IC₅₀	0.224 μM Compound: Talabostat	Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay	[PMID: 32527554]

In Vitro

By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat (Val-boroPro) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity^[3].
Talabostat (Val-boroPro) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site^[4].

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

In Vivo

Talabostat (Val-boroPro; PT100) can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system.
In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, Talabostat (Val-boroPro) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory.
Talabostat (Val-boroPro) treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells^[4].

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. Nr. 149682-77-9
Molecular Weight 214.07
Formel C₉H₁₉BN₂O₃
SMILES

CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O
Synonyms

Val-boroPro; PT100
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (42)

All In Vivo Efficacy StudyWBCell Imaging/StainingELISA

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Journal Impact Factor

Science

Enteroviral 3C protease activates the human NLRP1 inflammasome in airway epithelia. [Abstract]

2020 Dec 4;370(6521):eaay2002. PMID: 33093214
Cell

The CARD8 inflammasome dictates HIV/SIV pathogenesis and disease progression. [Abstract]

2024 Feb 29;187(5):1223-1237.e16. PMID: 38428396

Talabostat purchased from MedChemExpress. Usage Cited in: Cell. 2024 Feb 29;187(5):1223-1237.e16. [Abstract]

Activation of CARD8 inflammasome by HIV-1 in THP-1 cells. CARD8-KO THP-1 cells expressing wild-type or mutant CARD8 were exposed to HIV reporter virus NL4-3-ΔEnv-EGFP pseudotyped with the VSVG envelope for six hours before LDH. Talabostat mesylate (VbP, 5 μM) was used as a positive control, as it induces cell death and IL-1β secretion.
Cell

Bat ASC2 suppresses inflammasomes and ameliorates inflammatory diseases. [Abstract]

2023 May 11;186(10):2144-2159.e22. PMID: 37172565

Talabostat purchased from MedChemExpress. Usage Cited in: Cell. 2023 May 11;186(10):2144-2159.e22. [Abstract]

LDH release and IL-1b secretion by ELISA in cell-free supernatants of N/TERT-1 stably expressing mCitrine (control) or bat/human ASC2-mCitrine, treated with Talabostat mesylate (2-200 μM) for 24 h.
Cancer Commun (Lond)

Conserved immuno-collagenic subtypes predict response to immune checkpoint blockade. [Abstract]

2024 May;44(5):554-575. PMID: 38507505

Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2024 May;44(5):554-575. [Abstract]

Talabostat mesylate (20 µg/mouse; i.g.; once daily for 21 days) effectively inhibited tumor growth in BALB/c mice bearing 4T1 cells.
Cancer Res

SPP1 Drives Colorectal Cancer Liver Metastasis and Immunotherapy Resistance by Stimulating CXCL12 Production in Cancer-Associated Fibroblasts. [Abstract]

2026 Jan 2;86(1):58-79. PMID: 41051794
Cancer Res

FAP Promotes Immunosuppression by Cancer-Associated Fibroblasts in the Tumor Microenvironment via STAT3-CCL2 Signaling. [Abstract]

2016 Jul 15;76(14):4124-35. PMID: 27216177

Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]

RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Cleaved caspase-3 in the cells was detected by Western blotting. The results indicate that Talabostat mesylate can activate caspase‑3 in Gsdmd‑knockout cells.

Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]

RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Microscopic images of the cells. The results showed that Talabostat mesylate induced apoptotic morphological changes in Gsdmd‑knockout cells.
Nat Commun

Caspase-1 initiates apoptosis in the absence of gasdermin D. [Abstract]

2019 May 7;10(1):2091. PMID: 31064994
J Adv Res

Hippocampal dipeptidyl peptidase 9 bidirectionally regulates memory associated with synaptic plasticity. [Abstract]

2025 Aug:74:225-236. PMID: 39369958
Adv Sci (Weinh)

Intratumoral Collagen Deposition Supports Angiogenesis Suggesting Anti-angiogenic Therapy in Armored and Cold Tumors. [Abstract]

2025 Jan 17:e2409147. PMID: 39823457
Adv Sci (Weinh)

ANO1-Mediated Inhibition of Cancer Ferroptosis Confers Immunotherapeutic Resistance through Recruiting Cancer-Associated Fibroblasts. [Abstract]

2023 Aug;10(24):e2300881. PMID: 37341301
Int J Biol Sci

BGN/FAP/STAT3 positive feedback loop mediated mutual interaction between tumor cells and mesothelial cells contributes to peritoneal metastasis of gastric cancer. [Abstract]

2023 Jan 1;19(2):465-483. PMID: 36632455
J Allergy Clin Immunol

NLRP1 variant M1184V decreases inflammasome activation in the context of DPP9 inhibition and asthma severity. [Abstract]

2021 Jun;147(6):2134-2145.e20. PMID: 33378691
J Exp Med

Discovery of potent and selective inhibitors of human NLRP3 with a novel mechanism of action. [Abstract]

2025 Nov 3;222(11):e20242403. PMID: 40892070
J Exp Med

Viral proteases activate the CARD8 inflammasome in the human cardiovascular system. [Abstract]

2022 Oct 3;219(10):e20212117. PMID: 36129453
Proc Natl Acad Sci U S A

Activation of the NLRP1 inflammasome in human keratinocytes by the dsDNA mimetic poly(dA:dT). [Abstract]

2023 Jan 31;120(5):e2213777120. PMID: 36693106
Proc Natl Acad Sci U S A

Homozygous NLRP1 gain-of-function mutation in siblings with a syndromic form of recurrent respiratory papillomatosis. [Abstract]

2019 Sep 17;116(38):19055-19063. PMID: 31484767
Cell Rep

Peli1 facilitates NLRP3 inflammasome activation by mediating ASC ubiquitination. [Abstract]

2021 Oct 26;37(4):109904. PMID: 34706239
Anal Chem

Ultrasensitive Fluorescent Probes Reveal an Adverse Action of Dipeptide Peptidase IV and Fibroblast Activation Protein during Proliferation of Cancer Cells. [Abstract]

2016 Aug 16;88(16):8309-14. PMID: 27444320
Sci Signal

Tyrosine kinase inhibitors can activate the NLRP3 inflammasome in myeloid cells through lysosomal damage and cell lysis. [Abstract]

2023 Jan 17;16(768):eabh1083. PMID: 36649377
Neurosci Bull

Time-Dependent Transcriptional Dynamics of Contextual Fear Memory Retrieval Reveals the Function of Dipeptidyl Peptidase 9 in Reconsolidation. [Abstract]

2025 Jan;41(1):16-32. PMID: 39621238
CNS Neurosci Ther

Anti-cancer effect of targeting fibroblast activation protein alpha in glioblastoma through remodeling macrophage phenotype and suppressing tumor progression. [Abstract]

2023 Mar;29(3):878-892. PMID: 36382346
Biochem Pharmacol

Targeting the FAPα/Integrin αvβ1 complex attenuates hepatic stellate cell activation and liver fibrosis. [Abstract]

2026 May:247:117801. PMID: 41687828
Cells

DPP8 Selective Inhibitor Tominostat as a Novel and Broad-Spectrum Anticancer Agent against Hematological Malignancies. [Abstract]

2023 Apr 6;12(7):1100. PMID: 37048172
Biomolecules

DPP Inhibition Enhances the Efficacy of PD-1 Blockade by Remodeling the Tumor Microenvironment in Lewis Lung Carcinoma Model. [Abstract]

2024 Mar 25;14(4):391. PMID: 38672409
Int Immunopharmacol

Cisatracurium besylate rescues Mycobacterium Tuberculosis-infected macrophages from necroptosis and enhances the bactericidal effect of isoniazid. [Abstract]

2023 Jul:120:110291. PMID: 37182451
Obesity

Talabostat Alleviates Obesity and Associated Metabolic Dysfunction via Suppression of Macrophage-Driven Adipose Inflammation. [Abstract]

2021 Feb;29(2):327-336. PMID: 33342076
J Biol Chem

Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. [Abstract]

2018 Dec 7;293(49):18864-18878. PMID: 30291141

Talabostat purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]

Lack of evidence for directly binding to NLRP1 by Talabostat. 293T-ASC-GFPNLRP1 cells are treated with 2 μM Talabostat for 16 hours and lysed by 3 rounds of freezing and thawing. 20 μL (2 μg/uL) clarified lysates are heated at a temperature gradient for 10 minutes, centrifuged at 16,000g for 10mins at room temperature.
J Immunol

RIPK3-MLKL-Mediated Neutrophil Death Requires Concurrent Activation of Fibroblast Activation Protein-α. [Abstract]

2020 Sep 15;205(6):1653-1663. PMID: 32796025
Ann Surg Oncol

Dipeptidyl Peptidase 9 Increases Chemoresistance and is an Indicator of Poor Prognosis in Colorectal Cancer. [Abstract]

2020 Oct;27(11):4337-4347. PMID: 32734369
J Diabetes Investig

VX-765 ameliorates renal injury and fibrosis in diabetes by regulating caspase-1-mediated pyroptosis and inflammation. [Abstract]

2022 Jan;13(1):22-33. PMID: 34494385
Iran J Allergy Asthma Immunol

2021 Mar 17.
bioRxiv

2025 Aug 16.
NPJ Dement

Post-symptomatic NLRP3 inhibition rescues cognitive impairment and mitigates amyloid and tau driven neurodegeneration. [Abstract]

2025;1(1):3. PMID: 40343261
SSRN

2025 Jan 28.
Research Square Preprint

2024 Apr 18.
bioRxiv

2023 Nov 4.
bioRxiv

2023 Jun 25.
bioRxiv

2023 Mar 19.
bioRxiv

2023 Jan 17.
bioRxiv

January 25, 2022.
Curr Protoc Immunol

Inflammasome Assays In Vitro and in Mouse Models. [Abstract]

2020 Dec;131(1):e107. PMID: 33017103
SSRN

2020 Jul.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 40 mg/mL (186.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

4.6714 mL

23.3568 mL

46.7137 mL

5 mM

0.9343 mL

4.6714 mL

9.3427 mL

10 mM

0.4671 mL

2.3357 mL

4.6714 mL

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Protokoll

Animal Administration^[4]

Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. Talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed before BLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvested for histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses^[4].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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)

Verweise

[1]. Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94. [Content Brief]

[2]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [Content Brief]

[3]. Talabostat

[4]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [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	4.6714 mL	23.3568 mL	46.7137 mL	116.7842 mL
	5 mM	0.9343 mL	4.6714 mL	9.3427 mL	23.3568 mL
	10 mM	0.4671 mL	2.3357 mL	4.6714 mL	11.6784 mL
	15 mM	0.3114 mL	1.5571 mL	3.1142 mL	7.7856 mL
	20 mM	0.2336 mL	1.1678 mL	2.3357 mL	5.8392 mL
	25 mM	0.1869 mL	0.9343 mL	1.8685 mL	4.6714 mL
	30 mM	0.1557 mL	0.7786 mL	1.5571 mL	3.8928 mL
	40 mM	0.1168 mL	0.5839 mL	1.1678 mL	2.9196 mL
	50 mM	0.0934 mL	0.4671 mL	0.9343 mL	2.3357 mL
	60 mM	0.0779 mL	0.3893 mL	0.7786 mL	1.9464 mL
	80 mM	0.0584 mL	0.2920 mL	0.5839 mL	1.4598 mL
	100 mM	0.0467 mL	0.2336 mL	0.4671 mL	1.1678 mL

Keywords

Talabostat

42 Cited Publications

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Talabostat

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Talabostat

Alle Dipeptidyl Peptidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (42)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Talabostat

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Talabostat

Alle Dipeptidyl Peptidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (42)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Talabostat Related Classifications

HY-13233 Related Classifications