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Cat. No.: HY-181936

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Atg4B activator-1

Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a K_d of 0.2199 μM. Atg4B activator-1 binds to the allosteric pocket of ATG4B and induces conformational changes. Atg4B activator-1 induces Autophagy. Atg4B activator-1 inhibits the proliferation and migration of triple-negative breast cancer cells. Atg4B activator-1 can be used in studies related to triple-negative breast cancer.

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CAS No.: 3126601-01-9
화학식: C₂₅H₂₂ClFN₂O₂
분자량:436.91

보관:

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

Atg4B activator-1 Chemical Structure

CAS No.: 3126601-01-9

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

ATG4B

0.2199 μM (Kd)

In Vitro

Atg4B activator-1 activates the activity of recombinant human ATG4B protease in a concentration-dependent manner in in vitro assays, with a K_d of 2.199×10^-7 M^[1].
Atg4B activator-1 (24 h) potently inhibits the viability of various triple-negative breast cancer cell lines, and exhibits the strongest activity against MDA-MB-231 cells after 24 h of treatment (IC₅₀ = 1.81 ± 0.95 μM)^[1].
Atg4B activator-1 (1-2 μM; 0-48 h) inhibits the migratory wound healing of MDA-MB-231 cells within 48 h in a concentration-dependent manner^[1].
Atg4B activator-1 (1-4 μM) induces autophagy in a concentration-dependent manner in MDA-MB-231 cells^[1].

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

Cell Autophagy Assay^[1]

Cell Line:

MDA-MB-231
Concentration:

1, 2, 4 μM
Incubation Time:

24 h for Immunofluorescence assay
Result:

Increased LC3 puncta intensity.
Increased LC3-II protein levels.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	V_z	CL	Bioavailability
Mice^[1]	1 mg/kg	i.v.	0.74 h	0.08 h	134.10 ng/mL	386.24 ng·h/mL	393.20 ng·h/mL	2715.78 mL/kg	42.39 mL/min/kg	/
Mice^[1]	10 mg/kg	p.o.	3.37 h	0.25 h	31.85 ng/mL	273.40 ng·h/mL	304.76 ng·h/mL	/	/	7.75 %

In Vivo

Atg4B activator-1 (5-20 mg/kg; i.p.; once every two days; 14 days) dose-dependently inhibits triple-negative breast tumor growth in BALB/c nude mice, with 86.3% tumor growth inhibition at the 20 mg/kg dose, and induces autophagy while modulating EMT markers without causing overt organ toxicity^[1].

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

Animal Model:

BALB/c nude (female, 5-6 weeks old, triple-negative breast cancer model via subcutaneous inoculation of MDA-MB-231 cells)^[1]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

i.p.; once every two days; 14 days
Result:

Achieved 49.2% tumor growth inhibition at 5 mg/kg, 72.2% at 10 mg/kg, and 86.3% at 20 mg/kg relative to control.
Significantly reduced tumor weight in all treatment groups, with the greatest reduction in the 20 mg/kg group.
Showed no significant changes in mouse body weight across treatment groups.
Upregulated E-cadherin, downregulated MMP-2, and increased LC3-II levels in tumor tissue.
Caused no pathological lesions in heart, liver, spleen, lung, and kidney via hematoxylin-eosin staining.
Markedly reduced Ki-67 positive nuclei in the 20 mg/kg group, indicating suppressed tumor cell proliferation.

Chemical Information

CAS No. 3126601-01-9
분자량 436.91
화학식 C₂₅H₂₂ClFN₂O₂
SMILES

FC1=CC(Cl)=C(COC2=C(OC)C=C(CNCC3=CC=CC4=C3N=CC=C4)C=C2)C=C1
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Jin W, et al. Structure-based discovery of a novel allosteric activator of ATG4B for the treatment of triple-negative breast cancer. Eur J Med Chem. 2026;308:118686. [Content Brief]

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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MOQ

Minimum order quantity

100 mg

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