Talabostat
Based on 42 publication(s) in Google Scholar
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 149682-77-9
- 分子式: C9H19BN2O3
- 分子量:214.07
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Talabostat
More- Science. 2020 Dec 4;370(6521):eaay2002. [Abstract]
- Cell. 2024 Feb 29;187(5):1223-1237.e16. [Abstract]
- Cell. 2023 May 11;186(10):2144-2159.e22. [Abstract]
- Cancer Commun (Lond). 2024 May;44(5):554-575. [Abstract]
- Cancer Res. 2026 Jan 2;86(1):58-79. [Abstract]
- Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]
- Nat Commun. 2019 May 7;10(1):2091. [Abstract]
- J Adv Res. 2025 Aug:74:225-236. [Abstract]
- Adv Sci (Weinh). 2025 Mar;12(10):e2409147. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(24):e2300881. [Abstract]
- Int J Biol Sci. 2023 Jan 1;19(2):465-483. [Abstract]
- J Allergy Clin Immunol. 2021 Jun;147(6):2134-2145.e20. [Abstract]
- J Exp Med. 2025 Nov 3;222(11):e20242403. [Abstract]
- J Exp Med. 2022 Oct 3;219(10):e20212117. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Jan 31;120(5):e2213777120. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Sep 17;116(38):19055-19063. [Abstract]
- Cell Rep. 2021 Oct 26;37(4):109904. [Abstract]
- Anal Chem. 2016 Aug 16;88(16):8309-14. [Abstract]
- Sci Signal. 2023 Jan 17;16(768):eabh1083. [Abstract]
- Neurosci Bull. 2025 Jan;41(1):16-32. [Abstract]
- CNS Neurosci Ther. 2023 Mar;29(3):878-892. [Abstract]
- Biochem Pharmacol. 2026 May:247:117801. [Abstract]
- Cells. 2023 Apr 6;12(7):1100. [Abstract]
- Biomolecules. 2024 Mar 25;14(4):391. [Abstract]
- Int Immunopharmacol. 2023 Jul:120:110291. [Abstract]
- Obesity. 2021 Feb;29(2):327-336. [Abstract]
- J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]
- J Immunol. 2020 Sep 15;205(6):1653-1663. [Abstract]
- Ann Surg Oncol. 2020 Oct;27(11):4337-4347. [Abstract]
- J Diabetes Investig. 2022 Jan;13(1):22-33. [Abstract]
- Iran J Allergy Asthma Immunol. 2021 Mar 17.
- bioRxiv. 2025 Aug 16.
- NPJ Dement. 2025;1(1):3. [Abstract]
- SSRN. 2025 Jan 28.
- Research Square Preprint. 2024 Apr 18.
- bioRxiv. 2023 Nov 4.
- bioRxiv. 2023 Jun 25.
- bioRxiv. 2023 Mar 19.
- bioRxiv. 2023 Jan 17.
- bioRxiv. January 25, 2022.
- Curr Protoc Immunol. 2020 Dec;131(1):e107. [Abstract]
- SSRN. 2020 Jul.
Customer Validation & Images
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ELISA
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In Vivo Efficacy Study
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ELISA
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WB
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WB
生物活性
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DPP-4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.066 μM
Compound: 1, PT-100
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Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry
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[PMID: 24617858] |
| HEK293 | IC50 |
0.066 μM
Compound: 1, PT-100, Val-boroPro
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Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
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[PMID: 22525314] |
| HEK293 | IC50 |
0.07 μM
Compound: 1, PT- 100, Talabostat
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Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
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[PMID: 24900696] |
| HEK-293T | IC50 |
6.8 μM
Compound: 1, Val-boroPro
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Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs
Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs
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[PMID: 18783201] |
| U-87MG ATCC | IC50 |
0.224 μM
Compound: Talabostat
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Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
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[PMID: 32527554] |
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[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 149682-77-9
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分子量 214.07
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分子式 C9H19BN2O3
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SMILES
CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O
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別名
Val-boroPro; PT100
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (42)
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Journal Impact Factor
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Most Recent
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Science
2020 Dec 4;370(6521):eaay2002. PMID: 33093214 -
Cell
2024 Feb 29;187(5):1223-1237.e16. PMID: 38428396
Talabostat purchased from MedChemExpress. Usage Cited in: Cell. 2024 Feb 29;187(5):1223-1237.e16. [Abstract]
Activation of CARD8 inflammasome by HIV-1 in THP-1 cells. CARD8-KO THP-1 cells expressing wild-type or mutant CARD8 were exposed to HIV reporter virus NL4-3-ΔEnv-EGFP pseudotyped with the VSVG envelope for six hours before LDH. Talabostat mesylate (VbP, 5 μM) was used as a positive control, as it induces cell death and IL-1β secretion.
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Cell
2023 May 11;186(10):2144-2159.e22. PMID: 37172565
Talabostat purchased from MedChemExpress. Usage Cited in: Cell. 2023 May 11;186(10):2144-2159.e22. [Abstract]
LDH release and IL-1b secretion by ELISA in cell-free supernatants of N/TERT-1 stably expressing mCitrine (control) or bat/human ASC2-mCitrine, treated with Talabostat mesylate (2-200 μM) for 24 h.
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Cancer Commun (Lond)
2024 May;44(5):554-575. PMID: 38507505
Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2024 May;44(5):554-575. [Abstract]
Talabostat mesylate (20 µg/mouse; i.g.; once daily for 21 days) effectively inhibited tumor growth in BALB/c mice bearing 4T1 cells.
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Cancer Res
SPP1 Drives Colorectal Cancer Liver Metastasis and Immunotherapy Resistance by Stimulating CXCL12 Production in Cancer-Associated Fibroblasts. [Abstract]2026 Jan 2;86(1):58-79. PMID: 41051794 -
Cancer Res
FAP Promotes Immunosuppression by Cancer-Associated Fibroblasts in the Tumor Microenvironment via STAT3-CCL2 Signaling. [Abstract]2016 Jul 15;76(14):4124-35. PMID: 27216177
Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]
RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Cleaved caspase-3 in the cells was detected by Western blotting. The results indicate that Talabostat mesylate can activate caspase‑3 in Gsdmd‑knockout cells.
Talabostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Jul 15;76(14):4124-35. [Abstract]
RAW264.7 cells of the indicated genotypes were treated with 4 µM Talabostat mesylate (Val-boroPro) for the indicated times (6-12 h). Microscopic images of the cells. The results showed that Talabostat mesylate induced apoptotic morphological changes in Gsdmd‑knockout cells.
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Nat Commun
2019 May 7;10(1):2091. PMID: 31064994 -
J Adv Res
Hippocampal dipeptidyl peptidase 9 bidirectionally regulates memory associated with synaptic plasticity. [Abstract]2025 Aug:74:225-236. PMID: 39369958 -
Adv Sci (Weinh)
Intratumoral Collagen Deposition Supports Angiogenesis Suggesting Anti-angiogenic Therapy in Armored and Cold Tumors. [Abstract]2025 Mar;12(10):e2409147. PMID: 39823457 -
Adv Sci (Weinh)
ANO1-Mediated Inhibition of Cancer Ferroptosis Confers Immunotherapeutic Resistance through Recruiting Cancer-Associated Fibroblasts. [Abstract]2023 Aug;10(24):e2300881. PMID: 37341301 -
Int J Biol Sci
BGN/FAP/STAT3 positive feedback loop mediated mutual interaction between tumor cells and mesothelial cells contributes to peritoneal metastasis of gastric cancer. [Abstract]2023 Jan 1;19(2):465-483. PMID: 36632455 -
J Allergy Clin Immunol
NLRP1 variant M1184V decreases inflammasome activation in the context of DPP9 inhibition and asthma severity. [Abstract]2021 Jun;147(6):2134-2145.e20. PMID: 33378691 -
J Exp Med
Discovery of potent and selective inhibitors of human NLRP3 with a novel mechanism of action. [Abstract]2025 Nov 3;222(11):e20242403. PMID: 40892070 -
J Exp Med
2022 Oct 3;219(10):e20212117. PMID: 36129453 -
Proc Natl Acad Sci U S A
Activation of the NLRP1 inflammasome in human keratinocytes by the dsDNA mimetic poly(dA:dT). [Abstract]2023 Jan 31;120(5):e2213777120. PMID: 36693106 -
Proc Natl Acad Sci U S A
Homozygous NLRP1 gain-of-function mutation in siblings with a syndromic form of recurrent respiratory papillomatosis. [Abstract]2019 Sep 17;116(38):19055-19063. PMID: 31484767 -
Cell Rep
2021 Oct 26;37(4):109904. PMID: 34706239 -
Anal Chem
Ultrasensitive Fluorescent Probes Reveal an Adverse Action of Dipeptide Peptidase IV and Fibroblast Activation Protein during Proliferation of Cancer Cells. [Abstract]2016 Aug 16;88(16):8309-14. PMID: 27444320 -
Sci Signal
Tyrosine kinase inhibitors can activate the NLRP3 inflammasome in myeloid cells through lysosomal damage and cell lysis. [Abstract]2023 Jan 17;16(768):eabh1083. PMID: 36649377 -
Neurosci Bull
Time-Dependent Transcriptional Dynamics of Contextual Fear Memory Retrieval Reveals the Function of Dipeptidyl Peptidase 9 in Reconsolidation. [Abstract]2025 Jan;41(1):16-32. PMID: 39621238 -
CNS Neurosci Ther
Anti-cancer effect of targeting fibroblast activation protein alpha in glioblastoma through remodeling macrophage phenotype and suppressing tumor progression. [Abstract]2023 Mar;29(3):878-892. PMID: 36382346 -
Biochem Pharmacol
Targeting the FAPα/Integrin αvβ1 complex attenuates hepatic stellate cell activation and liver fibrosis. [Abstract]2026 May:247:117801. PMID: 41687828 -
Cells
DPP8 Selective Inhibitor Tominostat as a Novel and Broad-Spectrum Anticancer Agent against Hematological Malignancies. [Abstract]2023 Apr 6;12(7):1100. PMID: 37048172 -
Biomolecules
DPP Inhibition Enhances the Efficacy of PD-1 Blockade by Remodeling the Tumor Microenvironment in Lewis Lung Carcinoma Model. [Abstract]2024 Mar 25;14(4):391. PMID: 38672409 -
Int Immunopharmacol
Cisatracurium besylate rescues Mycobacterium Tuberculosis-infected macrophages from necroptosis and enhances the bactericidal effect of isoniazid. [Abstract]2023 Jul:120:110291. PMID: 37182451 -
Obesity
Talabostat Alleviates Obesity and Associated Metabolic Dysfunction via Suppression of Macrophage-Driven Adipose Inflammation. [Abstract]2021 Feb;29(2):327-336. PMID: 33342076 -
J Biol Chem
Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. [Abstract]2018 Dec 7;293(49):18864-18878. PMID: 30291141
Talabostat purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Abstract]
Lack of evidence for directly binding to NLRP1 by Talabostat. 293T-ASC-GFPNLRP1 cells are treated with 2 μM Talabostat for 16 hours and lysed by 3 rounds of freezing and thawing. 20 μL (2 μg/uL) clarified lysates are heated at a temperature gradient for 10 minutes, centrifuged at 16,000g for 10mins at room temperature.
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J Immunol
RIPK3-MLKL-Mediated Neutrophil Death Requires Concurrent Activation of Fibroblast Activation Protein-α. [Abstract]2020 Sep 15;205(6):1653-1663. PMID: 32796025 -
Ann Surg Oncol
Dipeptidyl Peptidase 9 Increases Chemoresistance and is an Indicator of Poor Prognosis in Colorectal Cancer. [Abstract]2020 Oct;27(11):4337-4347. PMID: 32734369 -
J Diabetes Investig
VX-765 ameliorates renal injury and fibrosis in diabetes by regulating caspase-1-mediated pyroptosis and inflammation. [Abstract]2022 Jan;13(1):22-33. PMID: 34494385 -
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NPJ Dement
Post-symptomatic NLRP3 inhibition rescues cognitive impairment and mitigates amyloid and tau driven neurodegeneration. [Abstract]2025;1(1):3. PMID: 40343261 -
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Curr Protoc Immunol
2020 Dec;131(1):e107. PMID: 33017103 -
溶剤 & 溶解度
DMSO : ≥ 40 mg/mL (186.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Mice: BLM (0.5mg/kg/day) is administered on days -7, -6, -5, -2, -1, 0 in the nostrils of male mice. Talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed per os twice daily from day 1-14. MRI is performed before BLM and at days 0, 7 and 14. After the last MRI acquisition, animals are euthanised and the lungs harvested for histological and quantitative real-time polymerase chain reaction (qRT-PCR) analyses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
[1]. Lankas GR, et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005 Oct;54(10):2988-94. [Content Brief]
[2]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [Content Brief]
[3]. Talabostat
[4]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6714 mL | 23.3568 mL | 46.7137 mL | 116.7842 mL |
| 5 mM | 0.9343 mL | 4.6714 mL | 9.3427 mL | 23.3568 mL | |
| 10 mM | 0.4671 mL | 2.3357 mL | 4.6714 mL | 11.6784 mL | |
| 15 mM | 0.3114 mL | 1.5571 mL | 3.1142 mL | 7.7856 mL | |
| 20 mM | 0.2336 mL | 1.1678 mL | 2.3357 mL | 5.8392 mL | |
| 25 mM | 0.1869 mL | 0.9343 mL | 1.8685 mL | 4.6714 mL | |
| 30 mM | 0.1557 mL | 0.7786 mL | 1.5571 mL | 3.8928 mL | |
| 40 mM | 0.1168 mL | 0.5839 mL | 1.1678 mL | 2.9196 mL | |
| 50 mM | 0.0934 mL | 0.4671 mL | 0.9343 mL | 2.3357 mL | |
| 60 mM | 0.0779 mL | 0.3893 mL | 0.7786 mL | 1.9464 mL | |
| 80 mM | 0.0584 mL | 0.2920 mL | 0.5839 mL | 1.4598 mL | |
| 100 mM | 0.0467 mL | 0.2336 mL | 0.4671 mL | 1.1678 mL |
Talabostat 関連分類
HY-13233 関連分類
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