Talabostat-Val-boroPro-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETalabostatCat. No.: HY-13233CAS No.: 149682-77-9Synonyms: Val-boroPro; PT100分式: CHBNO分量: 214.07作靶點: Dipeptidyl Peptidase作通路: Metabolic Enzyme/Protease儲存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)

2、體外實驗 DMSO : 40 mg/mL (186.85 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.6714 mL 23.3568 mL 46.7137 mL5 mM 0.9343 mL 4.6714 mL 9.3427 mL10 mM 0.4671 mL 2.3357 mL 4.6714 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Talabostat

3、 (Val-boroPro)種服活性和選擇性的肽肽酶 IV (DPP-IV) 抑制劑 (IC50 4 nM; Ki = 0.18nM) 和成纖維細胞活化蛋 (FAP) 的第個臨床抑制劑 (IC50 = 560 nM)，抑制 DPP8/9 (IC50 = 4/11 nM; Ki =1.5/0.76 nM)，靜息細胞脯氨酸肽酶 (QPP) (IC50 = 310 nM)、DPP2 和些其他 DASH 家族酶。具有抗腫瘤和造刺激活性 1 2 3。IC50 & Target IC50: 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP

4、) 1Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9) 21/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 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

5、 T-cell immunityand T-cell dependent activity 3.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 4.體內(nèi)研究 Talabostat (Val-boroPro) can stimulate immune responses against tumo

6、rs involving both the innate andadaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphomamodels, Talabostat (Val-boroPro) causes regression and rejection of tumors. The antitumor effect appears toinvolve tumor-specific CTL and protective immunological memory. Talab

7、ostat (Val-boroPro) treatment ofWEHI 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 4.PROTOCOLAnimal Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostr

8、ils of male mice. TalabostatAdministration 4 (40 g/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed beforeBLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvestedfor histological and quantitative real-time po

9、lymerase chain reaction (qRT-PCR) analyses 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Nat Commun. 2019 May 7;10(1):2091. Cancer Res. 2016 Jul 15;76(14):4124-35. Anal Chem. 2016 Aug 16;88(16):8309-14. J Biol Chem. 2018 Dec 7;293(49):18

10、864-18878. bioRxiv. Feb. 7, 2018.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidylpeptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94.2

11、. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. JMed Chem. 2008 Oct 9;51(19):6005-13.3. Talabostat4. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediatedcytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80.McePdfHeight Caution: Product has