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Talabostat (PT-100) Dipeptidyl Peptidase Inhibitor

Name: Talabostat (PT-100)
Brand: Selleck Chemicals
SKU: S8455
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S8455

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.

Chemical Structure

Molecular Weight: 310.18

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: >97%

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	310.18	Formula	C₁₀H₂₃BN₂O₆S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	150080-09-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Val-boroPro			Smiles	B(C1CCCN1C(=O)C(C(C)C)N)(O)O.CS(=O)(=O)O

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (199.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 62 mg/mL

Ethanol : 62 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (16.12mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DPP-4 ^[1] (Cell-free assay) <4 nM DPP-8 ^[1] (Cell-free assay) 4 nM DPP-9 ^[1] (Cell-free assay) 11 nM DPP-2 ^[1] (Cell-free assay) 310 nM PEP ^[1] (Cell-free assay) 390 nM
In vitro	In vitro, talabostat (PT-100) upregulates cytokines/chemokines in human bone marrow stromal cells^[2]. This compound induces monocytes and macrophage cell death, and its induction of pyroptosis requires caspase-1^[4].
In vivo	Talabostat (PT-100) 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, it can directly target FAP expressed by reactive fibroblasts. This compound 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].
References	[1] https://pubmed.ncbi.nlm.nih.gov/16186403/ [2] https://cancerres.aacrjournals.org/content/67/9_Supplement/1894 [3] https://www.ncbi.nlm.nih.gov/pubmed/?term=23554941 [4] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5477230/