Talabostat
Based on 16 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.
For research use only. We do not sell to patients.
- CAS No.: 149682-77-9
- Formula: C9H19BN2O3
- Molecular Weight:214.07
-
Storage:
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
HY-101056
Brensocatib
-
HY-13233A
Talabostat mesylate
-
HY-10285
Saxagliptin
-
HY-15408
Trelagliptin
-
HY-14806
Teneligliptin
-
HY-14877
Anagliptin
-
HY-14806A
Teneligliptin hydrobromide
-
HY-A0023
Alogliptin Benzoate
-
HY-112668
Retagliptin phosphate
-
HY-15408A
Trelagliptin succinate
-
HY-15981
Omarigliptin
-
HY-10287
Gosogliptin
Publications Citing Use of MedChemExpress (MCE) Talabostat
More- Science. 2020 Dec 4;370(6521):eaay2002. [Abstract]
- Cancer Res. 2026 Jan 2;86(1):58-79. [Abstract]
- Int J Biol Sci. 2023 Jan 1;19(2):465-483. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Sep 17;116(38):19055-19063. [Abstract]
- Sci Signal. 2023 Jan 17;16(768):eabh1083. [Abstract]
- CNS Neurosci Ther. 2023 Mar;29(3):878-892. [Abstract]
- Cells. 2023 Apr 6;12(7):1100. [Abstract]
- Int Immunopharmacol. 2023 Jul:120:110291. [Abstract]
- J Immunol. 2020 Sep 15;205(6):1653-1663. [Abstract]
- Ann Surg Oncol. 2020 Oct;27(11):4337-4347. [Abstract]
- Iran J Allergy Asthma Immunol. 2021 Mar 17.
- bioRxiv. 2025 Aug 16.
- bioRxiv. 2023 Jun 25.
- bioRxiv. 2023 Jan 17.
- bioRxiv. January 25, 2022.
- Curr Protoc Immunol. 2020 Dec;131(1):e107. [Abstract]
Biological Activity
|
DPP-4 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.066 μM
Compound: 1, PT-100
|
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
|
[PMID: 24617858] |
| HEK293 | IC50 |
0.066 μM
Compound: 1, PT-100, Val-boroPro
|
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
|
[PMID: 22525314] |
| HEK293 | IC50 |
0.07 μM
Compound: 1, PT- 100, Talabostat
|
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
|
[PMID: 24900696] |
| HEK-293T | IC50 |
6.8 μM
Compound: 1, Val-boroPro
|
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
|
[PMID: 18783201] |
| U-87MG ATCC | IC50 |
0.224 μM
Compound: Talabostat
|
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
|
[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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 149682-77-9
-
Molecular Weight 214.07
-
Formula C9H19BN2O3
-
SMILES
CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O
-
Synonyms
Val-boroPro; PT100
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (16)
-
Journal Impact Factor
-
Most Recent
-
Science
2020 Dec 4;370(6521):eaay2002. PMID: 33093214 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
-
-
-
-
-
Curr Protoc Immunol
2020 Dec;131(1):e107. PMID: 33017103
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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.
Purity & Documentation
References
[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 Related Classifications
HY-13233 Related Classifications
Powered by Bioz