Talabostat (PT-100)

Catalog No.S8455 Synonyms: Val-boroPro

For research use only.

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

CAS No. 150080-09-4

Selleck's Talabostat (PT-100) has been cited by 2 Publications

Purity & Quality Control

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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, 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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T M{nCVWZ2dmO2aX;uJIF{e2G7 MUXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KESSUEmg[ZhxemW|c3XkJIlvKEiHS{K5N3Qh[2WubIOsJGtqRTBwMECwO|bPxE1w Mn31QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5OEOyNFEoRjF6N{izNlAyRC:jPh?=
HEK293T MUPGeY5kfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KESSUEig[ZhxemW|c3XkJIlvKEiHS{K5N3Qh[2WubIOsJGtqRTBwMECxOe69VS5? MlvLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5OEOyNFEoRjF6N{izNlAyRC:jPh?=
HEK293 NWnBWmVMTnWwY4Tpc44h[XO|YYm= MmLBNVUhdWmwcx?= M1ntN2lvcGmkaYTpc44hd2ZibX;1d4UhemWlb33ibY5idnRiRlHQJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMheE6DIILlcIVie2ViZoLvcUBCdGFvUILvMZAudmm2cn;hcoltcWSnIIDy[U1qdmO3YnH0[YQhf2m2aDDlcpp6dWViZn;yJFE2KG2rboOgdJJqd3JidH:gd5Vje3S{YYTlJIFl\Gm2aX;uJIJ6KG[udX;y[ZNk\W6lZTD0[YNpdmmzdXWsJGlEPTB;MD6wOlbPxE1w MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV{NUOxOEc,OjJ3MkWzNVQ9N2F-
HEK293 MWHGeY5kfGmxbjDhd5NigQ>? MXqxOUBucW6| MkDOTY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCIQWCg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczD1d4lv\yCDbHGtVJJwNXBvbnn0do9idmmuaXTlJIF{KHO3YoP0doF1\SCrbnP1ZoF1\WRiZn;yJFE2KG2rboOgdJJqd3JidH:gd5Vje3S{YYTlJIFl\Gm2aX;uMEBKSzVyPUCuNFfPxE1w MnnWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2PVYoRjJ2OUCwOlk3RC:jPh?=
HEK293T NYXLNo1jTnWwY4Tpc44h[XO|YYm= NIeybI4zKGi{cx?= MnG4TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCGUGC5JIV5eHKnc4Pl[EBqdiCrboThZ5QhUEWNMkmzWEBk\WyuczDh[pRmeiB{IHjyd{whUUN3ME22MljPxE1w MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd6M{KwNUc,OTh5OEOyNFE9N2F-
PBMC NGrTfJdHfW6ldHnvckBie3OjeR?= NGLQd|lG\m[nY4Sgc44h[2WubDDk[YF1cCCrbjDy[ZN1cW6pIGDCUWN{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBidm6neHnuJHYheG:|aYTpeoUh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMUCwJJVOKFq4YXSt[o1s NWPIcG9SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUewOVUzPzFpPkG3NFU2OjdzPD;hQi=>
Assay
Methods Test Index PMID
Western blot pro-IL-1β 27820798
Growth inhibition assay Cell viability 29967349
ELISA IL-1β 27820798
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].

Protocol (from reference)

Cell Research:

[4]

  • Cell lines: THP-1 macrophages
  • Concentrations: 0.1, 1, 10 μM
  • Incubation Time: 24 h
  • Method:

    --

Animal Research:

[3]

  • Animal Models: C57BL/6 female mice
  • Dosages: 20 µg
  • Administration: by gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 310.18
Formula

C10H23BN2O6S

CAS No. 150080-09-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles B(C1CCCN1C(=O)C(C(C)C)N)(O)O.CS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

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

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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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