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Talabostat

Catalog No: 24102
CAS Number: 149682-77-9
Purity: 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.

For research use only. We do not sell to patients.

Chemical Information

NameTalabostat
Iupac Chemical Name ((R)-1-(L-Valyl)pyrrolidin-2-yl)boronic acid
SynonymsBXCL701; BXCL 701; BXCL-701; PT-100, PT100, PT 100, D05989, Val-boroPro; Talabostat
Molecular FormulaC9H19BN2O3
Molecular Weight214.07
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 Number149682-77-9
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Ordering Information

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FormulationOff-white solid
Purity98% Min.
StorageDry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
SolubilitySoluble in DMSO
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

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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.

Chemical Structure

24102 - Talabostat | CAS 149682-77-9

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