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

Atg4B activator-1 (Compound 16a) 是一种变构、选择性的、口服有效 ATG4B 激活剂，Kd 为 0.2199 μM。Atg4B activator-1 结合 ATG4B 的变构口袋，诱导构象变化。Atg4B activator-1 诱导自噬 (Autophagy)。Atg4B activator-1 可抑制三阴性乳腺癌细胞的增殖与迁移。Atg4B activator-1 可用于三阴性乳腺癌的相关研究。

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Atg4B activator-1

Atg4B activator-1 Chemical Structure

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Atg4B activator-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

Atg4B activator-1 可在体外实验中浓度依赖性地激活重组人源 ATG4B 蛋白酶的活性，Kd 为 2.199×10-7 M[1]。
Atg4B activator-1 (24 h) 可强效抑制多种三阴性乳腺癌细胞系的活力，在处理 24 小时后，其对 MDA-MB-231 细胞的活性最强 (IC50 = 1.81 ± 0.95 μM)[1]。
Atg4B activator-1 (1-2 μM; 0-48 h) 可浓度依赖性地抑制 MDA-MB-231 细胞在 48 h 内的迁移性伤口愈合[1]。
Atg4B activator-1 (1-4 μM) 在MDA-MB-231 细胞中可浓度依赖性地诱导自噬[1]。

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

Atg4B activator-1 相关抗体:

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.
药代动力学
(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 %
体内研究
(In Vivo)

Atg4B activator-1 (5-20 mg/kg；腹腔注射；每 2 天 1 次；连续 14 天) 在 BALB/c 裸鼠中呈剂量依赖性地抑制三阴性乳腺癌肿瘤生长，20 mg/kg 剂量下的肿瘤生长抑制率达 86.3%，同时可诱导自噬、调控 EMT 标志物，且不会引发明显的器官毒性[1]。

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.
分子量

436.91

Formula

C25H22ClFN2O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Atg4B activator-1 相关分类

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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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