1. Metabolic Enzyme/Protease Autophagy
  2. Atg4 Cathepsin Phospholipase Autophagy
  3. Atg4B-IN-2

Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition.

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

Atg4B-IN-2 Chemical Structure

Atg4B-IN-2 Chemical Structure

CAS No. : 2765008-88-4

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5 mg USD 280 In-stock
10 mg USD 460 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition[1].

IC50 & Target

IC50: 11 μM (Atg4B), 3.5 μM (PLA2)[1]
Ki: 3.1 μM (Atg4B)[1]

In Vitro

Atg4B-IN-2 (compound 21f) (1-10 μM; 2 hours) restores the p62 expression in cells treated with AF (amino acid-free) in a dose-dependent manner[1].
Atg4B-IN-2 (1 and 5 μM; 2 hours) decreases moderately autophagic vesicles at 1 μM, and almost completely inhibits autophagy at 5 μM[1].
Atg4B-IN-2 (5 μM; 2 hours) inhibits Abi-induced autophagy and significantly augments apoptotic cell death and sensitivity to Abi[1].

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

Western Blot Analysis

Cell Line: LNCaP cells (incubated in AF medium)[1]
Concentration: 1, 2, 5, 10 μM
Incubation Time: 2 hours (then incubated in AFM for 24 or 3 hours)
Result: Restored the p62 expression in cells treated with AF in a dose-dependent manner.

Cell Autophagy Assay

Cell Line: LNCaP cells (incubated in AF medium)[1]
Concentration: 1 and 5 μM
Incubation Time: 2 hours (then incubated in AFM for 24 or 3 hours)
Result: Decreased moderately autophagic vesicles at 1 μM, and almost completely inhibited autophagy at 5 μM.
Molecular Weight

330.46

Formula

C21H30O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C=C1)CCCCCCCCCCC)/C=C/C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (302.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0261 mL 15.1304 mL 30.2609 mL
5 mM 0.6052 mL 3.0261 mL 6.0522 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0261 mL 15.1304 mL 30.2608 mL 75.6521 mL
5 mM 0.6052 mL 3.0261 mL 6.0522 mL 15.1304 mL
10 mM 0.3026 mL 1.5130 mL 3.0261 mL 7.5652 mL
15 mM 0.2017 mL 1.0087 mL 2.0174 mL 5.0435 mL
20 mM 0.1513 mL 0.7565 mL 1.5130 mL 3.7826 mL
25 mM 0.1210 mL 0.6052 mL 1.2104 mL 3.0261 mL
30 mM 0.1009 mL 0.5043 mL 1.0087 mL 2.5217 mL
40 mM 0.0757 mL 0.3783 mL 0.7565 mL 1.8913 mL
50 mM 0.0605 mL 0.3026 mL 0.6052 mL 1.5130 mL
60 mM 0.0504 mL 0.2522 mL 0.5043 mL 1.2609 mL
80 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
100 mM 0.0303 mL 0.1513 mL 0.3026 mL 0.7565 mL
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  • 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.

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Product Name:
Atg4B-IN-2
Cat. No.:
HY-144636
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