Ac-Gly-BoroPro |
| Catalog No.GC32883 |
Ac-Gly-BoroPro es un inhibidor selectivo de FAP con una Ki de 23 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 886992-99-0
Sample solution is provided at 25 µL, 10mM.
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Ac-Gly-BoroPro is a selective Fibroblast Activation Protein (FAP) inhibitor with a Ki of 23nM[1, 2]. Ac-Gly-BoroPro selectively inhibits FAP, compared to other proline peptidases[3, 4], which is an important biomarker for cancer-associated fibroblasts and activated fibroblasts. FAP reacts readily with submicromolar concentrations of Ac-Gly-BoroPro, reaching steady state inhibition levels rapidly (Ki=23±3nM)[2].
Ac-Gly-BoroPro (10μM; 24h or 48h) can inhibit Human periodontal ligament stem cells (hPDLSCs) proliferation and migration[5]. Ac-Gly-BoroPro (20μM; 7 days) can inhibit osteoclast differentiation[6].
Ac-Gly-BoroPro (500μg/kg; 35 days; intraperitoneal injection) was administered to 2-month-old unmated female mice with ovariectomized ovaries, which could alleviate osteoporosis induced by ovariectomy, promote bone formation, and inhibit bone resorption in mice[6]. Ac-Gly-BoroPro (40μg/kg; 4 weeks; intra-articular injection) could significantly improve cartilage erosion, subchondral bone thickening and osteophyte formation in destabilization of the medial meniscus (DMM) mice model[7].
References:
[1] HENDERSON J M, XIANG M S W, HUANG J C, et al. Dipeptidyl Peptidase Inhibition Enhances CD8 T Cell Recruitment and Activates Intrahepatic Inflammasome in a Murine Model of Hepatocellular Carcinoma [J]. Cancers (Basel), 2021, 13(21):
[2] HU Y, MA L, WU M, et al. Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7 [J]. Bioorg Med Chem Lett, 2005, 15(19): 4239-42.
[3] ZHAO L, CHEN J, PANG Y, et al. Fibroblast activation protein-based theranostics in cancer research: A state-of-the-art review [J]. Theranostics, 2022, 12(4): 1557-69.
[4] KIM S M, JANG Y J. Enzymatic activity of fibroblast activation protein-alpha is essential for TGF-beta1-induced fibroblastic differentiation of human periodontal ligament cells [J]. Exp Cell Res, 2024, 442(2): 114230.
[5] HE J, FANG B, SHAN S, et al. Mechanical stiffness promotes skin fibrosis through FAPalpha-AKT signaling pathway [J]. J Dermatol Sci, 2024, 113(2): 51-61.
[6] WEI H, XU Y, WANG Y, et al. Identification of Fibroblast Activation Protein as an Osteogenic Suppressor and Anti-osteoporosis Drug Target [J]. Cell Rep, 2020, 33(2): 108252.
[7] FAN A, WU G, WANG J, et al. Inhibition of fibroblast activation protein ameliorates cartilage matrix degradation and osteoarthritis progression [J]. Bone Res, 2023, 11(1): 3.
| Cell experiment [1]: | |
Cell lines | Human periodontal ligament stem cells (hPDLSCs) |
Preparation Method | For induction of PDL fibroblastic differentiation, hPDLSCs were cultured in α-MEM with 5% FBS containing 10ng/ml TGF-β1, which was treated every 2 days for 9 days For inhibition of dipeptidyl peptidase activity of FAPα, 10μM Ac-Gly-BoroPro was treated in cells. |
Reaction Conditions | 10μM; 24h or 48h |
Applications | Ac-Gly-BoroPro can inhibit cell proliferation and migration. |
| Animal experiment [2]: | |
Animal models | C57BL/6J wild-type mice |
Preparation Method | Administered daily intraperitoneal injections of 500mg/kg Ac-Gly-BoroPro in 8-week-old wild-type mice. |
Dosage form | 500mg/kg; 35 days; intraperitoneal injection |
Applications | Ac-Gly-BoroPro promotes bone formation and inhibits bone resorption in vivo. |
| Kinase experiment [3]: | |
Preparation Method | Ki values for inhibition of proteases by Ac-Gly-BoroPro are determined using the method of progress curves for analysis of tight binding competitive inhibitors. Various concentrations of Ac-Gly-BoroPro are reacted with Fibroblast Activation Protein (FAP (1.0nM) ) and Dipeptidyl Peptidase 4 (DPP-4 (0.1nM)) in the presence of Alanine-Proline-7-Amino-4-Methylcoumarin (Ala-Pro-AFC (500μM for FAP; 100μM for DPP-4 )), and time-dependent inhibition of each protease is monitored. Reactions contained inhibitor concentrations at least 20-fold greater than protease concentrations, such that the protease-inhibitor complex does not significantly deplete the free inhibitor. |
Reaction Conditions | 23nM; 150s, 300s, 450s, 600s |
Applications | Ac-Gly-BoroPro can rapidly and effectively inhibit the activity of FAP. |
References: | |
| Cas No. | 886992-99-0 | SDF | |
| Canonical SMILES | Ac-Gly-{boroPro} | ||
| Formula | C8H15BN2O4 | M.Wt | 214.03 |
| Solubility | DMSO : ≥ 50 mg/mL (233.61 mM) | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.6722 mL | 23.3612 mL | 46.7224 mL |
| 5 mM | 934.4 μL | 4.6722 mL | 9.3445 mL |
| 10 mM | 467.2 μL | 2.3361 mL | 4.6722 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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