Home Proteases DPP inhibitor Talabostat (PT-100) For research use only.

Talabostat (PT-100)

Synonyms: Val-boroPro

Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities.

Talabostat (PT-100) Chemical Structure

Talabostat (PT-100) Chemical Structure

CAS No. 150080-09-4

Purity & Quality Control

Talabostat (PT-100) Related Products

Signaling Pathway

DPP Signaling Pathways

DPP Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T Function assay Inhibition of human recombinant DPP9 expressed in HEK293T cells, Ki=0.00076μM. 18783201
HEK293T Function assay Inhibition of human recombinant DPP8 expressed in HEK293T cells, Ki=0.0015μM. 18783201
HEK293 Function assay 15 mins 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, IC50=0.066μM. 22525314
HEK293 Function assay 15 mins Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition, IC50=0.07μM. 24900696
HEK293T Function assay 2 hrs Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs, IC50=6.8μM. 18783201
PBMC Function assay Effect on cell death in resting PBMCs assessed as reduction of annexin V positive cells in presence of 100 uM Zvad-fmk 17055271
Click to View More Cell Line Experimental Data

Biological Activity

Description Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities.
Targets
DPP-4 [1]
(Cell-free assay)		 DPP-8 [1]
(Cell-free assay)		 DPP-9 [1]
(Cell-free assay)		 DPP-2 [1]
(Cell-free assay)		 PEP [1]
(Cell-free assay)
<4 nM 4 nM 11 nM 310 nM 390 nM
In vitro
In vitro

In vitro, talabostat upregulates cytokines/chemokines in human bone marrow stromal cells[2]. Talabostat (Val-boroPro) induces monocytes and macrophage cell death. Val-boroPro induced pyroptosis requires caspase-1[4].
Cell Research Cell lines THP-1 macrophages
Concentrations 0.1, 1, 10 μM
Incubation Time 24 h
Method

--
Experimental Result Images Methods Biomarkers Images PMID
Western blot pro-IL-1β 27820798
Growth inhibition assay Cell viability 29967349
ELISA IL-1β 27820798
In Vivo
In vivo

Talabostat has been shown to produce potent antitumor effects when administered orally in multiple mouse tumor models. Val-boroPro mediates complete tumor regression via a novel mechanism that requires more rapid DC trafficking and subsequent acceleration of T cell priming[3]. In tumor stroma, talabostat can directly target FAP expressed by reactive fibroblasts. Talabostat stimulates innate and adaptive immune responses against tumors involving transcriptional upregulation of cytokines and chemokines[2]. Val-boroPro is known to stimulate the transcriptional upregulation several cytokines, including IL-1β, IL-6, G-CSF, and CXCL1/KC, in both tumors and tumor-draining lymph nodes, and to increase the mouse serum protein levels of several of these cytokines, including G-CSF and CXCL1/KC[4].
Animal Research Animal Models C57BL/6 female mice
Dosages 20 µg
Administration by gavage

Chemical Information & Solubility

Molecular Weight 310.18 Formula

C10H23BN2O6S
CAS No. 150080-09-4 SDF --
Smiles B(C1CCCN1C(=O)C(C(C)C)N)(O)O.CS(=O)(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 62 mg/mL ( (199.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 62 mg/mL

Ethanol : 62 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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