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Cat. No.: HY-141702

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Cathepsin C-IN-1

Cathepsin C-IN-1 is an orally active Cathepsin C inhibitor with a human IC₅₀ of 57.4 nM. Cathepsin C-IN-1 inhibits Cat C activity and downstream neutrophil serine protease (NSP) activation. Cathepsin C-IN-1 shows anti-inflammatory activity in COPD rats, reducing pulmonary inflammation, histopathological changes, and pro-inflammatory cytokines (IFN-γ, IL-1β, IL-6, IL-17, TNF-α, GM-CSF) while increasing IL-10. Cathepsin C-IN-1 can be used for research on chronic obstructive pulmonary disease.

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

CAS No.: 2652046-41-6
Formula: C₂₁H₂₁ClF₃N₇
Molecular Weight:463.89

Storage:

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

Cathepsin C-IN-1 Chemical Structure

CAS No.: 2652046-41-6

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

hCathepsin C

57.4 nM (IC₅₀)

IL-1β

IL-6

IL-17

IL-10

TNF-α

All Cathepsin Isoforms :

All Interleukin Related Isoforms :

All TNF Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC50	24.3 nM	Inhibition of Cat C activity in human THP-1 cells using H-Gly-Phe-AFC as substrate incubated 1 hr at 37°C prior to substrate addition measured after 60 mins by fluorescence. Inhibition of Cat C activity in human THP-1 cells using H-Gly-Phe-AFC as substrate incubated 1 hr at 37°C prior to substrate addition measured after 60 mins by fluorescence.	34374541
U-937	IC50	20.9 nM	Inhibition of Cat C activity in human U937 cells using H-Gly-Phe-AFC as substrate incubated 1 hr at 37°C prior to substrate addition measured after 60 mins by fluorescence. Inhibition of Cat C activity in human U937 cells using H-Gly-Phe-AFC as substrate incubated 1 hr at 37°C prior to substrate addition measured after 60 mins by fluorescence.	34374541
L02	IC50	>100 μM	Cytotoxicity against human L02 hepatocytes assessed as viability reduction after 48 hrs incubation by CCK-8 assay with IC50 >100 μM. Cytotoxicity against human L02 hepatocytes assessed as viability reduction after 48 hrs incubation by CCK-8 assay with IC50 >100 μM.	34374541

In Vitro

Protein/Amino Acid MetabolismOthers

Protein/Amino Acid Metabolism

Cathepsin C-IN-1 (Compound 54) (1 μM; 6-48 h) time-dependently promotes the degradation of NE, Cat G, and PR3 in C57BL/6 bone marrow cells^[1].
Cathepsin C-IN-1 (1 μM; 6 days) partially inhibits Cat C activity and downstream NSP activation in HL-60 cells^[1].

Others

Cathepsin C-IN-1 (1 hour) inhibits Cat C activity in THP-1 and U937 cells with IC₅₀ values of 24.3 nM and 20.9 nM^[1].
Cathepsin C-IN-1 weakly inhibits CYP1A2 and CYP2C19 with IC₅₀ values of 13 and 7.13 μM, respectively, and shows a low potential for CYP-mediated interactions^[1].

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

Western Blot Analysis^[1]

Cell Line:

C57BL/6 bone marrow cells
Concentration:

1 μM
Incubation Time:

0, 6, 12, 48 h
Result:

Promoted degradation of NE, Cat G, and PR3 in C57BL/6 bone marrow cells, reducing them to 47.8%, 27.8%, and 19.9% of original levels at 48 h.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	MRT	C_max	AUC_0-∞	CL	F
Rat^[1]	2 mg/kg	i.v.	1.86 h	/	1.22 h	458.0 μg/L	249.2 μg/L·h	8.04 L/h/kg	/
Rat^[1]	10 mg/kg	p.o.	1.56 h	2.0 h	2.68 h	83.5 μg/L	157.5 μM/L·h	63.4 L/h/kg	16.7 %

In Vivo

Protein/Amino Acid MetabolismInnate Immunity

Protein/Amino Acid Metabolism

Cathepsin C-IN-1 (5-45 mg/kg; p.o.; twice daily; 6 days) produces dose-dependent inhibition of Cat C activity and downstream NSP activation in the bone marrow and blood of C57BL/6 mice^[1].

Innate Immunity

Cathepsin C-IN-1 (5-45 mg/kg; p.o.; twice daily) alleviates pulmonary inflammation, inflammatory cell recruitment, and systemic inflammation in a cigarette smoke combined with LPS (HY-D1056)-induced rat chronic obstructive pulmonary disease (COPD) model, and inhibits cathepsin C activity and downstream neutrophil serine protease activation in lung tissue and bronchoalveolar lavage fluid^[1].

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

Animal Model:

C57BL/6^[1]
Dosage:

5 mg/kg, 15 mg/kg, and 45 mg/kg
Administration:

p.o.; twice daily; 6 days
Result:

An obvious dose-dependent decrease in Cat C activity and downstream NSP activation was observed in both bone marrow and blood.
In the 45 mg/kg group, Cat C and NSP activities (NE, Cat G, and PR3) in the bone marrow were inhibited to 16.2%, 28.3%, 17.2%, and 30.8% of normal group levels, respectively.
Weight loss and lack of energy were not observed in mice.

Animal Model:

Cigarette smoke combined with LPS-induced rat chronic obstructive pulmonary disease (COPD) model^[1]
Dosage:

5, 15, 45 mg/kg
Administration:

p.o.; twice daily
Result:

Reduced the protein levels of cathepsin G and proteinase 3 to 32.5%, 27.6%, and 29.7% of their initial levels, respectively.
Ameliorated histopathological changes, including alveolar hemorrhage, alveolar dilation, partial alveolar fusion, inflammatory cell infiltration, and destruction of alveolar structure.
Reduced the levels of pro-inflammatory cytokines (IFN-γ, IL-1β, IL-6, IL-17, TNF-α, and GM-CSF).
Increased the concentration of the anti-inflammatory cytokine IL-10.

Related Protocols :

Chemical Information

CAS No. 2652046-41-6
Molecular Weight 463.89
Formula C₂₁H₂₁ClF₃N₇
SMILES

ClC1=CN=C(NC2=NC=C(N3CCN(C)CC3)C=C2)N=C1NC4=CC(C(F)(F)F)=CC=C4
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]. Chen X, et al. Discovery and Anti-inflammatory Activity Evaluation of a Novel Non-peptidyl Non-covalent Cathepsin C Inhibitor. Journal of medicinal chemistry. 2021 Aug 26;64(16):11857-11885. [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.

Bioz

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Cathepsin C-IN-1

All Cathepsin Isoforms

All Interleukin Related Isoforms

All TNF Receptor Isoforms