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Ac-Gly-BoroPro 

Cat. No.: HY-101801 Purity: >98.0%
Handling Instructions

Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.

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

Ac-Gly-BoroPro Chemical Structure

Ac-Gly-BoroPro Chemical Structure

CAS No. : 886992-99-0

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1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 528 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.

IC50 & Target

Ki: 23 nM (FAP)[1]

In Vitro

FAP has been implicated in cancer; however, its specific role remains elusive because inhibitors that distinguish FAP from other prolyl peptidases like dipeptidyl peptidase-4 (DPP-4) have not been developed. Ac-Gly-BoroPro selectively inhibits FAP relative to other prolyl peptidases. FAP reacts readily with submicromolar concentrations of Ac-Gly-BoroPro, reaching steady state inhibition levels rapidly (Ki=23±3 nM). In contrast, DPP-4 requires higher Ac-Gly-BoroPro concentrations for inhibition and a longer time to reach steady state inhibition levels (Ki=377±18 nM). Ac-Gly-BoroPro inhibits other prolyl peptidases (DPP-7, DPP-8, DPP-9, prolyl oligopeptidase, and acylpeptide hydrolase) with Ki values ranging from 9- to 5400-fold higher than that for FAP inhibition. The N-acyl-linkage in Ac-Gly-BoroPro blocks the N terminus of the inhibitor, making it less nucleophilic and therefore unlikely to cyclize[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

214.03

Formula

C₈H₁₅BN₂O₄

CAS No.

886992-99-0

Sequence

Ac-Gly-{boroPro}

Sequence Shortening

Ac-G-{boroP}

SMILES

O=C(N1[[email protected]@H](B(O)O)CCC1)CNC(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
-20°C 1 year

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (233.61 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6722 mL 23.3612 mL 46.7224 mL
5 mM 0.9344 mL 4.6722 mL 9.3445 mL
10 mM 0.4672 mL 2.3361 mL 4.6722 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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 FAP (1.0 nM) and DPP-4 (0.1 nM) in the presence of Ala-Pro-AFC (500 μM for FAP; 100 μM 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Ac-Gly-BoroProOthersInhibitorinhibitorinhibit

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Product Name:
Ac-Gly-BoroPro
Cat. No.:
HY-101801
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