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Synonyms | Val-boroPro | Storage (From the date of receipt) |
3 years -20°C powder | ||||
化学式 | C10H23BN2O6S |
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分子量 | 310.18 | CAS No. | 150080-09-4 | ||||
Solubility (25°C)* | 体外 | DMSO | 62 mg/mL (199.88 mM) | ||||
Water | 62 mg/mL (199.88 mM) | ||||||
Ethanol | 62 mg/mL (199.88 mM) | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 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. |
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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]. |
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]. |
細胞アッセイ | 細胞株 | THP-1 macrophages |
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濃度 | 0.1, 1, 10 μM | |
反応時間 | 24 h | |
実験の流れ | -- |
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動物実験 | 動物モデル | C57BL/6 female mice |
投薬量 | 20 µg | |
投与方法 | by gavage |
Chemical inhibition of DPP9 sensitizes the CARD8 inflammasome in HIV-1-infected cells [ Nat Chem Biol, 2023, 19(4):431-439] | PubMed: 36357533 |
FAP is critical for ovarian cancer cell survival by sustaining NF-κB activation through recruitment of PRKDC in lipid rafts [ Cancer Gene Ther, 2023, 30(4):608-621] | PubMed: 36494579 |
The FAP α -activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway [ Acta Pharm Sin B, 2022, 12(3):1288-1304] | PubMed: 35530139 |
The FAPα-activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway [ Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.08.015] | PubMed: None |
Inactivation of the cytoprotective major vault protein by caspase-1 and -9 in epithelial cells during apoptosis: caspase-1 and -9 inactivate the major vault protein. [ J Invest Dermatol, 2019, S0022-202X(19)33499-2] | PubMed: 31877317 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。