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Cat. No.: HY-183166A

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Z-Arg-Lys-AOMK diTFA

Z-Arg-Lys-AOMK diTFA is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK diTFA reduces cytosolic cathepsin B activity in homogenates of mouse cerebral cortex and hippocampal tissues, and alleviates motor dysfunction associated with CCI-TBI. Z-Arg-Lys-AOMK diTFA can be used in the research of traumatic brain injury.

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

Formula: C₃₄H₄₄F₆N₆O₁₀
Molecular Weight:810.74

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Z-Arg-Lys-AOMK diTFA Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

All Cathepsin Isoforms :

In Vitro

Z-Arg-Lys-AOMK (1.7-5536 nM; 30 min) diTFA potently and selectively inhibits recombinant mouse cathepsin B at neutral pH 7.2 (IC₅₀ = 25 nM) with 100-fold lower potency at acidic pH 4.6, and does not inhibit other mouse cysteine cathepsins (C, H, L, X) at relevant concentrations^[1].

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

In Vivo

Z-Arg-Lys-AOMK (20 mg/kg; i.p.; once daily) diTFA reduces cathepsin B activity in the cytoplasm and homogenates of the cerebral cortex and hippocampus in mice induced by CCI-TBI, and restores motor function to 55% of the baseline level at 1 day post-injury^[1].

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

Animal Model:

C57BL/6J mice (female, adult, 4-5 months of age, traumatic brain injury CCI model)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; daily; 7 consecutive days (starting 1 day pre-CCI-TBI through day 6 post-CCI-TBI)
Result:

Reduced CCI-TBI-induced cytosolic cathepsin B activity in the ipsilateral brain cortex from ~400 pmol AMC/μg protein to ~275 pmol AMC/μg protein .
Reduced CCI-TBI-induced cytosolic cathepsin B activity in the contralateral cortex from ~200 pmol AMC/μg protein to ~220 pmol AMC/μg protein.
Reduced cathepsin B activity in ipsilateral brain cortex homogenates from ~1750 pmol AMC/μg protein to ~1000 pmol AMC/μg protein.
Reduced cathepsin B activity in ipsilateral hippocampus homogenates from ~1700 pmol AMC/μg protein to ~800 pmol AMC/μg protein.
Improved rotarod motor function on day 1 post-CCI-TBI, increasing latency from ~35% of baseline to ~55% of baseline.

Chemical Information

Molecular Weight 810.74
Formula C₃₄H₄₄F₆N₆O₁₀
SMILES

O=C(OCC1=CC=CC=C1)N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(COC(C2=C(C=CC=C2C)C)=O)=O)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Podvin S, et al. Activation of Cytosolic Cathepsin B Activity in the Brain by Traumatic Brain Injury and Inhibition by the Neutral pH Selective Inhibitor Probe Z-Arg-Lys-AOMK. ACS Chem Neurosci. 2025;16(7):1297-1308. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Z-Arg-Lys-AOMK diTFA

All Cathepsin Isoforms