1. Autophagy
  2. Autophagy
  3. CUR5g

CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo.

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CUR5g Chemical Structure

CUR5g Chemical Structure

CAS No. : 1370032-20-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 308 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo[1].

In Vitro

CUR5g (0-40 μM, 0-24 h) selectively induces autophagosome accumulation in cancer cells[1].
CUR5g (0-40 μM, 0-24 h) up-regulates LC3B-II and sequestosome 1 (SQSTM1) levels[1].
CUR5g (0-40 μM, 24 h) inhibits proliferation and migration of A549 cells, but dose not induce apoptosis or necrosis[1].

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

Cell Autophagy Assay[1]

Cell Line: A549 cells
Concentration: 0, 1, 5, 10, 20, and 40 μM
Incubation Time: 3, 6, 12, and 24 h
Result: Induced extensive cytoplasmic vacuolization, and GFP-LC3B signal shifted from diffuse cytosolic staining to a punctate pattern outlining autophagosomes.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0, 1, 5, 10, 20, and 40 μM
Incubation Time: 0, 1, 3, 6, 12, and 24 h
Result: Up-regulated LC3B-II and sequestosome 1 (SQSTM1) levels time- and dose-dependently. This increase was not the result of enhanced transcription, as mRNA expression of SQSTM1 and LC3B were not increased within CUR5g-exposed cells, suggesting that CUR5g might block autophagic flux rather than increase autophagosome formation.

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 0, 1, 5, 10, 20, and 40 μM
Incubation Time: 24 h
Result: Exhibited great toxicity to A549 cells at 20 μM. Slightly decreased A549 cell number at 10 µM, while decreased the number of A549 cells significantly at 20 µM. Showed no discernable activity in healthy human umbilical vein endothelial cell (HUVEC) viability at 40 µM.
In Vivo

CUR5g (40 mg/kg, Injected via caudal vein, once every 2 days for up to 15 days) exhibits synergistic anticancer effects with Cisplatin (HY-17394) (1 mg/kg) and inhibits autophagic flux in vivo[1].

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

Animal Model: BALB/c nude mice (4-week-old, A549 cells were subcutaneously injected into the right scapula of each nude mouse)[1]
Dosage: 40 mg/kg, CUR5g (40 mg/kg) and Cisplatin (1 mg/kg)
Administration: Injected via caudal vein, once every 2 days for up to 15 days
Result: Retarded the growth of xenografted tumors, whereas the combination treatment with Cisplatin almost completely inhibited tumor growth. Promoted the cisplatin sensitivity of A549 cells by inhibiting autophagic flux.
Molecular Weight

344.41

Formula

C22H20N2O2

CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C1/C(CN(C)C/C1=C\C2=CNC3=C2C=CC=C3)=C/C4=CC=C(O)C=C4

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 : 41.67 mg/mL (120.99 mM; ultrasonic and warming and heat to 60°C; 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 2.9035 mL 14.5176 mL 29.0352 mL
5 mM 0.5807 mL 2.9035 mL 5.8070 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.69%

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 2.9035 mL 14.5176 mL 29.0352 mL 72.5879 mL
5 mM 0.5807 mL 2.9035 mL 5.8070 mL 14.5176 mL
10 mM 0.2904 mL 1.4518 mL 2.9035 mL 7.2588 mL
15 mM 0.1936 mL 0.9678 mL 1.9357 mL 4.8392 mL
20 mM 0.1452 mL 0.7259 mL 1.4518 mL 3.6294 mL
25 mM 0.1161 mL 0.5807 mL 1.1614 mL 2.9035 mL
30 mM 0.0968 mL 0.4839 mL 0.9678 mL 2.4196 mL
40 mM 0.0726 mL 0.3629 mL 0.7259 mL 1.8147 mL
50 mM 0.0581 mL 0.2904 mL 0.5807 mL 1.4518 mL
60 mM 0.0484 mL 0.2420 mL 0.4839 mL 1.2098 mL
80 mM 0.0363 mL 0.1815 mL 0.3629 mL 0.9073 mL
100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7259 mL
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CUR5g Related Classifications

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.

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CUR5g
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HY-152100
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