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RSL3
RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.
Catalog No. T3646Cas No. 1219810-16-8
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Purity:99.96%
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RSL3
Catalog No. T3646Alias RSL3 1S, 1S,3R-RSL3Cas No. 1219810-16-8
RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $33 | In Stock | |
| 2 mg | $47 | In Stock | |
| 5 mg | $72 | In Stock | |
| 10 mg | $128 | In Stock | |
| 25 mg | $271 | In Stock | |
| 50 mg | $368 | In Stock | |
| 100 mg | $483 | In Stock | |
| 500 mg | $1,080 | In Stock | |
| 1 g | $1,430 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $68 | In Stock |
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CitedProduct Introduction
Bioactivity
Chemical Properties
| Description | RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS. |
| Targets&IC50 | GSH:100 nM |
| In vitro | METHODS: Human hepatocellular carcinoma cells HepG2, HA22T/VGH were treated with RSL3 (0.1-10 μM) for 72 h, and cell growth inhibition was detected by MTT.
RESULTS: RSL3 dose-dependently inhibited the growth of HepG2 and HA22T/VGH cells, with an IC50 of about 0.07 μM for HepG2 cells and 0.3 μM for HA22T/VGH cells. [1] METHODS: Human glioblastoma cells U87 and U251 were treated with RSL3 (0.25 μM and 0.5 μM) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: RSL3 treatment induced a decrease in the expression of ferroptosis-related proteins GPX4, ATF4 and xCT, and an up-regulation in the expression of HO-1 in U87 and U251 cells. [2] METHODS: Human colorectal cancer cells HCT116 and LoVo were treated with RSL3 (3 μM) for 24 h. Labile iron pool (LIP) and ROS intracellular levels were analyzed by Flow Cytometry. RESULTS: RSL3 promoted the increase of LIP and accumulation of ROS associated with ferroptosis. [3] |
| In vivo | METHODS: To test the antitumor activity in vivo, RSL3 (100 mg/kg in 20 μL DMSO plus 80 μL corn oil) was intraperitoneally injected into NSG mice bearing human prostate cancer tumors DU145 or PC3 twice a week for sixteen days.
RESULTS: RSL3 treatment significantly inhibited the growth of human prostate cancer tumors, indicating antitumor activity in vivo. [4] METHODS: To detect anti-tumor activity in vivo, RSL3 (1 mg/kg) and cetuximab (13 mg/kg) were intraperitoneally injected once a week for sixteen days into BALB/c nude mice harboring KRAS-mutant human colorectal cancer tumor DLD-1. RESULTS: RSL3 treatment significantly inhibited the growth of KRAS-mutant tumors. Cetuximab enhanced RSL3-induced ferroptosisby activating p38 MAPK and inhibiting the Nrf2/HO-1 axis, which further inhibited tumor growth. [5] |
| Cell Research | TERT/LT/ST/RASV12 cells are seeded in 10 cm dishes and treated with 1 µM staurosporine, 10 µg/ml erastin, 20 µg/ml RSL5, and 1 µg/ml RSL3 for 16 hr. Both dying cells and live cells in each 10 cm dish are harvested and collected in the same 15 ml tubes by centrifuging cell suspension at 1000 rpm for 5 min. (Only for Reference) |
| Alias | RSL3 1S, 1S,3R-RSL3 |
| Molecular Weight | 440.88 |
| Formula | C23H21ClN2O5 |
| Cas No. | 1219810-16-8 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.41 mg/mL (10 mM), Working solution is recommended to be prepared and used immediately.  DMSO: 45 mg/mL (102.07 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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