Name | VAL-BORO-PRO |
Synonyms | Pt 100 talabostat VAL-BORO-PRO Unii-kz1o2sh88z Talabostat (PT100) [(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid Boronic acid, ((2R)-1-((2S)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)- Boronic acid, (1-(2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-, (R-(R*,S*))- |
CAS | 149682-77-9 |
InChI | InChI=1/C9H19BN2O3/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15/h6-8,14-15H,3-5,11H2,1-2H3/t7-,8-/m0/s1 |
Molecular Formula | C9H19BN2O3 |
Molar Mass | 214.07 |
Density | 1.15 |
Boling Point | 421.4±55.0 °C(Predicted) |
pKa | 9.71±0.20(Predicted) |
Storage Condition | Room Temprature |
In vitro study | 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. 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. |
In vivo study | 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. |
biological activity | Talabostat (Val-boroPro; PT100) is an oral active and non-selective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 |
target | IC50: < 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP) Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9) |