2. Autophagy
  3. Atg4 Autophagy
  4. Atg4B activator-1

Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a Kd 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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Atg4B activator-1

Atg4B activator-1 Chemical Structure

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Atg4B activator-1 Related Antibodies

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Description

Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a Kd 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[1].

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 Kd 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.

Atg4B activator-1 Related Antibodies

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 T1/2 Tmax Cmax AUC0-t AUC0-∞ Vz 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.
Molecular Weight

436.91

Formula

C25H22ClFN2O2
SMILES

FC1=CC(Cl)=C(COC2=C(OC)C=C(CNCC3=CC=CC4=C3N=CC=C4)C=C2)C=C1
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
References
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Atg4B activator-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Atg4B activator-1Atg4AutophagyAutophagy-related 4triple-negative breast cancer cellsEMT markersautophagic fluxATG4BautolysosomeBALB/c nude miceautophagosomeautophagyprotease activityMDA-MB-231 cellsInhibitorinhibitorinhibit

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