Molecular Formula | C10H23BN2O6S |
Molar Mass | 310.175 |
Melting Point | >160°C (dec.) |
Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
Appearance | solid |
Color | White |
Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
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. |
Physical and Chemical Properties | Bioactive Talabostat (Val-boroPro, PT-100) is an inhibitor of dipeptidyl peptidase DPP with IC50 values for DPP-IV, DPP8, DPP9, QPP, FAP and PEP, respectively, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM. It has activity against tumors and stimulates hematopoiesis. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.224 ml | 16.12 ml | 32.24 ml |
5 mM | 0.645 ml | 3.224 ml | 6.448 ml |
10 mM | 0.322 ml | 1.612 ml | 3.224 ml |
5 mM | 0.064 ml | 0.322 ml | 0.645 ml |
Target
Target Value
DPP-4
(Cell-free assay) <4 nM
DPP8
(Cell-free assay) 4 nM
DPP9
(Cell-free assay) 11 nM
QPP
(Cell-free assay) 310 nM
PEP
(Cell-free assay) 390 nM
in vitro studies
talabo stat up-regulates cytokine/chemokine levels in human bone marrow stromal cells in vitro. Talabo stat (Val-boroPro) can induce the death of monocytes and macrophages, and Val-boroPro induction of apoptosis requires caspase-1 participation.
in vivo studies
Talabostat can effectively exert its anti-tumor activity in a variety of mouse tumor models. Val-boroPro complete tumor regression can be mediated by an entirely new mechanism requiring more rapid dendritic cell trafficking and subsequent acceleration of T cell priming. In the tumor stroma, talabo stat can directly target FAP expressed by reactive fibroblasts. Talabostat stimulates both endogenous and adaptive immune responses to up-regulate cytokine and chemokine transcription, and thus is anti-tumor. In tumors and tumor-draining lymph nodes, Val-boroPro stimulated transcription up-regulation of various cytokines, such as IL-1β, IL-6, G-CSF and CXCL1/KC; the serum protein levels of various cytokines in mice were also up-regulated, including G-CSF and CXCL1/KC.