1. Autophagy
  2. Autophagy
  3. ROC-325

ROC-325 

Cat. No.: HY-103706 Purity: >98.0%
Handling Instructions

ROC-325 is a novel inhibitor of autophagy.

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

ROC-325 Chemical Structure

ROC-325 Chemical Structure

CAS No. : 1859141-26-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 146 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Estimated Time of Arrival: December 31
25 mg USD 408 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ROC-325 is a novel inhibitor of autophagy.

IC50 & Target

Autophagy[1]

In Vitro

ROC-325 is a novel inhibitor of autophagy. Treatment with ROC-325 results in a significant loss of acridine orange fluorescence. ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. ROC-325 treatment yields pharmacodynamic effects that are consistent with inhibition of autophagy. Treatment with 5 μM ROC-325 for 24 hours leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. Immunoblotting analysis conducted in both A498 and 786-0 cells demonstrates that ROC-325 promotes a dose-dependent increase in LC3B expression in a manner that correlated with a corresponding increase in the levels of p62 and cathepsin D[1].

In Vivo

ROC-325 treatment leads to significant, dose-dependent inhibition of disease progression. ROC-325 is well tolerated and no notable toxicities are observed other than a very modest, nonsignificant reduction in mean body weight at the highest dose. Immunohistochemical analysis of specimens collected from animals treated with ROC-325 demonstrates significant, dose-dependent increases in the autophagic markers LC3B and p62 and increases apoptosis[1].

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 : 32 mg/mL (63.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9878 mL 9.9392 mL 19.8783 mL
5 mM 0.3976 mL 1.9878 mL 3.9757 mL
10 mM 0.1988 mL 0.9939 mL 1.9878 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Renal cancer cells are incubated with ROC-325 for 24 hours. Cells are harvested and then lysed. Approximately 50 μg of total cellular protein from each sample are subjected to SDS-PAGE, proteins are transferred to nitrocellulose membranes, and the membranes are blocked with 5% nonfat milk in a Tris-buffered saline solution containing 0.1% Tween-20 for 1 hour. The blots are then probed overnight at 4°C with primary antibodies, washed, and probed with species-specific secondary antibodies coupled to horseradish peroxidase. Immunoreactive material is detected by enhanced chemiluminescence[1].

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

Cell Assay
[1]

Cell viability is estimated by the MTT assay. Cells are seeded into 96-well microcultureplates at 10,000 cells per well and allowed to attach for 24 hours. Cells are then treated with ROC-325 for 72 hours. Following ROC-325 treatment, MTT is added and formazan absorbance is quantified using a microplate reader. The estimated cell viability under each experimental condition is calculated by normalizing the respective formazan optical density to the density of control cells. Proapoptotic effects following in vitro ROC-325 exposure are quantified by propidium iodide (PI) staining and fluorescence-activated cell sorting (FACS) analysis of sub-G0/G1 DNA content and by measurement of active caspase-3 by flow cytometry using a commercial kit[1].

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

Animal Administration
[1]

786-0 renal cancer cells (5×106) are suspended in a mixture of HBSS and Matrigel and subcutaneously implanted into female nude mice. Tumor-bearing animals from each cell line xenograft are randomized into treatment groups. Mice are treated with vehicle (water), ROC-325 (25, 40, and 50 mg/kg PO) QD×5 for 6 weeks. Mice are monitored daily and tumor volumes are measured twice weekly. At study completion, tumors from representative animals are excised from each group, formalin-fixed, and paraffin-embedded for immunohistochemical analysis[1].

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

References
Molecular Weight

503.06

Formula

C₂₈H₂₇ClN₄OS

CAS No.

1859141-26-6

SMILES

O=C1C2=C(SC3=C1C=CC=C3)C(C)=CC=C2NCCN(CCNC4=CC=NC5=CC(Cl)=CC=C45)C

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ROC-325
Cat. No.:
HY-103706
Quantity:

ROC-325

Cat. No.: HY-103706