RSL3

Catalog No.S8155 Batch:S815504

Technical Data

Formula	C₂₃H₂₁ClN₂O₅
Molecular Weight	440.88	CAS No.	1219810-16-8
Solubility (25°C)*	In vitro	DMSO	88 mg/mL (199.6 mM)
		Ethanol	15 mg/mL (34.02 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

RSL3 ((1S,3R)-RSL3) is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis.

Targets

Gpx4 ^[1]
(In Calu-1 cells)

In vitro

Ferroptosis-inducing compounds inactivate GPX4 by direct binding or by depleting glutathione.After binding to GPX4, RSL3 inactivates GPX4 to induce ROS production from lipid peroxidation. RSL3's ability to induce synthetic lethality with oncogenic RAS is rapid and quite potent. This compound inhibits the growth of BJ-TERT/LT/ST/RASV12 and DRD cells as low as 10 ng/mland started to kill sensitive cells as early as 8 hr after treatment^[1]^[2].

In vivo

Prostaglandin-endoperoxide synthase (PTGS) is the key enzyme in prostaglandin biosynthesis. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2. PTGS2 encoding cyclooxygenase-2 (COX-2) is significantly upregulated after treatment with RSL3 and erastin in mice^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines TERT/LT/ST/RASV12 cells Concentrations 1 µg/ml Incubation Time 16hrs Method 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.
Animal Study:^{^[1]}	Animal Models athymic nude mice(8 weeks)implanted with subcutaneous xenograft tumors derived from BJeLR cells Dosages 100 mg/kg Administration s.c. injection

Cell Assay:^{^[1]}

Cell lines
TERT/LT/ST/RASV12 cells
Concentrations
1 µg/ml
Incubation Time
16hrs
Method
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.

Animal Study:^{^[1]}

Animal Models
athymic nude mice(8 weeks)implanted with subcutaneous xenograft tumors derived from BJeLR cells
Dosages
100 mg/kg
Administration
s.c. injection

References

Customer Product Validation

: , , Am J Physiol Renal Physiol, 2017, doi: 10.1152/ajprenal.00044.2017

: Data from [Data independently produced by , , Nature, 2017, 547(7664):453-457]

: Data from [Data independently produced by , , Cell, 2017, 171(3):628-641]

: Data from [Data independently produced by , , Cell Res, 2016, 26(9):1021-32]

Selleck's RSL3 has been cited by 396 publications

7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.]	PubMed: 38297130
7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.]	PubMed: 38297130
Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39]	PubMed: 38594259
ROS-responsive nanoparticle delivery of ferroptosis inhibitor prodrug to facilitate mesenchymal stem cell-mediated spinal cord injury repair [ Bioact Mater, 2024, 38:438-454]	PubMed: 38770428
PRDX6 augments selenium utilization to limit iron toxicity and ferroptosis [ Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01329-z]	PubMed: 38867112
Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429]	PubMed: 38365899
Intrinsic temperature increase drives lipid metabolism towards ferroptosis evasion and chemotherapy resistance in pancreatic cancer [ Nat Commun, 2024, 15(1):8540]	PubMed: 39358362
Inhibition of GPX4 enhances CDK4/6 inhibitor and endocrine therapy activity in breast cancer [ Nat Commun, 2024, 15(1):9550]	PubMed: 39500869
Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471]	PubMed: 38508142
A novel ferroptosis inhibitor, Thonningianin A, improves Alzheimer's disease by activating GPX4 [ Theranostics, 2024, 14(16):6161-6184]	PubMed: 39431016

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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