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Talabostat

编号: 24102
Cas号: 149682-77-9
纯度: 98% Min.

Talabostat, also known as PT-100 and BXCL701, is dipeptidyl peptidase inhibitor with antineoplastic and hematopoiesis- stimulating activities. By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell- dependent activity. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. Dipeptidyl peptidases are involved in the activation of polypeptide hormones and chemokines.

仅供研究使用。 我们不向患者出售。

化学信息

名称 Talabostat
Iupac 化学名称 ((R)-1-(L-Valyl)pyrrolidin-2-yl)boronic acid
同义词BXCL701; BXCL 701; BXCL-701; PT-100, PT100, PT 100, D05989, Val-boroPro; Talabostat
英文同义词BXCL701; BXCL 701; BXCL-701; PT-100, PT100, PT 100, D05989, Val-boroPro; Talabostat
分子式C9H19BN2O3
分子量214.07
SmileN[C@@H](C(C)C)C(N1[C@H](B(O)O)CCC1)=O
InChiKeyFKCMADOPPWWGNZ-YUMQZZPRSA-N
InChiInChI=1S/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
Cas号149682-77-9
相关CAS号

订购信息

包装价格库存纯度备货期
大货询价询价询价
Request Bulk Quote Download MSDS 电话 : +86-177 0271 9238   Email : sales@sun-shinechem.com
外观性状类白色固体
纯度98% Min.
存储 0-4℃,可保存几天到几周;-20℃,可保存 几个月。
可溶性溶于DMSO等有机溶剂
处理方式
运输条件可以在室温下进行运输。
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Weiss FD, Alvarez Y, Shakeri F, Sahu A, Leka P, Dernst A, Rollheiser J, Vasconcelos M, Geraci A, Duthie F, Stahl R, Lee HE, Gellner AK, Buness A, Latz E, Meissner F. Retention of ES cell-derived 129S genome drives NLRP1 hypersensitivity and transcriptional deregulation in Nlrp3tm1Flv mice. Cell Death Differ. 2024 Sep 17. doi: 10.1038/s41418-024-01379-2. Epub ahead of print. PMID: 39289506.


2: Pashaei M, Farhadi E, Kavosi H, Madreseh E, Enayati S, Mahmoudi M, Amirzargar A. Talabostat, fibroblast activation protein inhibitor, attenuates inflammation and fibrosis in systemic sclerosis. Inflammopharmacology. 2024 Aug 21. doi: 10.1007/s10787-024-01536-6. Epub ahead of print. PMID: 39167314.


3: Lei M, Liu J, Gao Y, Dai W, Huang H, Jiang Q, Liu Z. DPP Inhibition Enhances the Efficacy of PD-1 Blockade by Remodeling the Tumor Microenvironment in Lewis Lung Carcinoma Model. Biomolecules. 2024 Mar 25;14(4):391. doi: 10.3390/biom14040391. PMID: 38672409; PMCID: PMC11047990.


4: Yang W, Yi J, Zhu R, Guo Y, Zhang K, Cao Y, Li X, Zhang J, Zhang Z, Li Y, Chen X. Transformable prodrug nanoplatform via tumor microenvironment modulation and immune checkpoint blockade potentiates immunogenic cell death mediated cancer immunotherapy. Theranostics. 2023 Mar 21;13(6):1906-1920. doi: 10.7150/thno.83912. PMID: 37064869; PMCID: PMC10091884.


5: Moecking J, Laohamonthonkul P, Meşe K, Hagelueken G, Steiner A, Harapas CR, Sandow JJ, Graves JD, Masters SL, Geyer M. Inflammasome sensor NLRP1 disease variant M1184V promotes autoproteolysis and DPP9 complex formation by stabilizing the FIIND domain. J Biol Chem. 2022 Dec;298(12):102645. doi: 10.1016/j.jbc.2022.102645. Epub 2022 Oct 26. PMID: 36309085; PMCID: PMC9700037.


6: Henderson JM, Xiang MSW, Huang JC, Wetzel S, Jiang L, Lai JH, Wu W, Kench JG, Bachovchin WW, Roediger B, McCaughan GW, Zhang HE, Gorrell MD. Dipeptidyl Peptidase Inhibition Enhances CD8 T Cell Recruitment and Activates Intrahepatic Inflammasome in a Murine Model of Hepatocellular Carcinoma. Cancers (Basel). 2021 Nov 1;13(21):5495. doi: 10.3390/cancers13215495. PMID: 34771657; PMCID: PMC8583374.


7: Zhao R, Jin X, Li A, Xu B, Shen Y, Wang W, Huang J, Zhang Y, Li X. Precise Diabetic Wound Therapy: PLS Nanospheres Eliminate Senescent Cells via DPP4 Targeting and PARP1 Activation. Adv Sci (Weinh). 2022 Jan;9(1):e2104128. doi: 10.1002/advs.202104128. Epub 2021 Nov 5. PMID: 34738744; PMCID: PMC8728814.


8: Mousavi MJ, Farhadi E, Vodjgani M, Karami J, Tahmasebi MN, Sharafat Vaziri A, Asgari M, Rezaei N, Mostafaei S, Jamshidi A, Mahmoudi M. Role of Fibroblast Activation Protein Alpha in Fibroblast-like Synoviocytes of Rheumatoid Arthritis. Iran J Allergy Asthma Immunol. 2021 Jun 6;20(3):338-349. doi: 10.18502/ijaai.v20i3.6335. PMID: 34134455.


9: Wu Y, Shi T, Wang J, He R. Talabostat Alleviates Obesity and Associated Metabolic Dysfunction via Suppression of Macrophage-Driven Adipose Inflammation. Obesity (Silver Spring). 2021 Feb;29(2):327-336. doi: 10.1002/oby.23058. Epub 2020 Dec 20. PMID: 33342076.


10: Chui AJ, Griswold AR, Taabazuing CY, Orth EL, Gai K, Rao SD, Ball DP, Hsiao JC, Bachovchin DA. Activation of the CARD8 Inflammasome Requires a Disordered Region. Cell Rep. 2020 Oct 13;33(2):108264. doi: 10.1016/j.celrep.2020.108264. PMID: 33053349; PMCID: PMC7594595.


11: Guo H, Ting JP. Inflammasome Assays In Vitro and in Mouse Models. Curr Protoc Immunol. 2020 Dec;131(1):e107. doi: 10.1002/cpim.107. PMID: 33017103; PMCID: PMC7751762.


12: Saso K, Miyoshi N, Fujino S, Sasaki M, Yasui M, Ohue M, Ogino T, Takahashi H, Uemura M, Matsuda C, Mizushima T, Doki Y, Eguchi H. Dipeptidyl Peptidase 9 Increases Chemoresistance and is an Indicator of Poor Prognosis in Colorectal Cancer. Ann Surg Oncol. 2020 Oct;27(11):4337-4347. doi: 10.1245/s10434-020-08729-7. Epub 2020 Jul 30. PMID: 32734369.


13: Fenini G, Karakaya T, Hennig P, Di Filippo M, Beer HD. The NLRP1 Inflammasome in Human Skin and Beyond. Int J Mol Sci. 2020 Jul 6;21(13):4788. doi: 10.3390/ijms21134788. PMID: 32640751; PMCID: PMC7370280.


14: Wen Z, Liu Q, Wu J, Xu B, Wang J, Liang L, Guo Y, Peng M, Zhao Y, Liao Q. Fibroblast activation protein α-positive pancreatic stellate cells promote the migration and invasion of pancreatic cancer by CXCL1-mediated Akt phosphorylation. Ann Transl Med. 2019 Oct;7(20):532. doi: 10.21037/atm.2019.09.164. Erratum in: Ann Transl Med. 2021 Oct;9(19):1511. doi: 10.21037/atm-2021-29. PMID: 31807514; PMCID: PMC6861799.


15: Panaro BL, Coppage AL, Beaudry JL, Varin EM, Kaur K, Lai JH, Wu W, Liu Y, Bachovchin WW, Drucker DJ. Fibroblast activation protein is dispensable for control of glucose homeostasis and body weight in mice. Mol Metab. 2019 Jan;19:65-74. doi: 10.1016/j.molmet.2018.10.011. Epub 2018 Nov 5. PMID: 30477988; PMCID: PMC6323180.


16: Zhong FL, Robinson K, Teo DET, Tan KY, Lim C, Harapas CR, Yu CH, Xie WH, Sobota RM, Au VB, Hopkins R, D'Osualdo A, Reed JC, Connolly JE, Masters SL, Reversade B. Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. J Biol Chem. 2018 Dec 7;293(49):18864-18878. doi: 10.1074/jbc.RA118.004350. Epub 2018 Oct 5. PMID: 30291141; PMCID: PMC6295727.


17: Okondo MC, Rao SD, Taabazuing CY, Chui AJ, Poplawski SE, Johnson DC, Bachovchin DA. Inhibition of Dpp8/9 Activates the Nlrp1b Inflammasome. Cell Chem Biol. 2018 Mar 15;25(3):262-267.e5. doi: 10.1016/j.chembiol.2017.12.013. Epub 2018 Jan 27. PMID: 29396289; PMCID: PMC5856610.


18: Xu Y, Zhou X, Mei M, Ren Y. Reprograming Carcinoma Associated Fibroblasts by microRNAs. Curr Mol Med. 2017;17(5):341-349. doi: 10.2174/1566524018666171205113959. PMID: 29210650.


19: Egger C, Cannet C, Gérard C, Suply T, Ksiazek I, Jarman E, Beckmann N. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72. doi: 10.1016/j.ejphar.2017.05.022. Epub 2017 May 12. PMID: 28506908.


20: Okondo MC, Johnson DC, Sridharan R, Go EB, Chui AJ, Wang MS, Poplawski SE, Wu W, Liu Y, Lai JH, Sanford DG, Arciprete MO, Golub TR, Bachovchin WW, Bachovchin DA. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. doi: 10.1038/nchembio.2229. Epub 2016 Nov 7. PMID: 27820798; PMCID: PMC5477230.

化学结构

24102 -  Talabostat | CAS 149682-77-9

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