RSL-3


Catalog No. size PriceQuantity
M6495-2 2mg solid $112
M6495-10 10mg solid $452

Description

Cas:1219810-16-8

Product Information:

RSL-3 is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.

 

Chemical Formula: C23H21ClN2O5

 

Exact Mass: 440.1139

 

Molecular Weight: 440.88

 

Elemental Analysis: C, 62.66; H, 4.80; Cl, 8.04; N, 6.35; O, 18.14

 

Synonym: 

 

RSL3

RSL-3

RSL 3

 

Chemical Name: 

Methyl(1S,3R)-2-(2-chloroacetyl)-1-(4-(methoxycarbonyl)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate

 

InChi Key:

TXJZRSRTYPUYRW-NQIIRXRSSA-N

 

InChi Code: 

InChI=1S/C23H21ClN2O5/c1-30-22(28)14-9-7-13(8-10-14)21-20-16(15-5-3-4-6-17(15)25-20)11-18(23(29)31-2)26(21)19(27)12-24/h3-10,18,21,25H,11-12H2,1-2H3/t18-,21+/m1/s1

 

Smiles Code:

O=C(OC)[C@@H]1N(C(CCl)=O)[C@@H](C2=CC=C(C(OC)=O)C=C2)C3=C(C(C=CC=C4)=C4N3)C1

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC50s of 0.48 µM in HN3 and 5.8 µM in HN3-rslR cells, respectively.

RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.

 

In Vivo:

RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with trigonelline in mice bearing HN3R cells.

 

 

References

 

  1. Schott C, Graab U, Cuvelier N, Hahn H, Fulda S. Oncogenic RAS Mutants Confer Resistance of RMS13 Rhabdomyosarcoma Cells to Oxidative Stress-Induced Ferroptotic Cell Death. Front Oncol. 2015 Jun 22;5:131. doi: 10.3389/fonc.2015.00131. PubMed PMID: 26157704; PubMed Central PMCID: PMC4476278.

 

  1. Yang WS, Stockwell BR. Synthetic lethal screening identifies compounds activating iron-dependent, nonapoptotic cell death in oncogenic-RAS-harboring cancer cells. Chem Biol. 2008 Mar;15(3):234-45. doi: 10.1016/j.chembiol.2008.02.010. PubMed PMID: 18355723; PubMed Central PMCID: PMC2683762.

 

  1. Torii S, Shintoku R, Kubota C, Yaegashi M, Torii R, Sasaki M, Suzuki T, Mori M, Yoshimoto Y, Takeuchi T, Yamada K. An essential role for functional lysosomes in ferroptosis of cancer cells. Biochem J. 2016 Mar 15;473(6):769-77. doi: 10.1042/BJ20150658. PubMed PMID: 26759376.

 

  1. Schoeneberger H, Belz K, Schenk B, Fulda S. Impairment of antioxidant defense via glutathione depletion sensitizes acute lymphoblastic leukemia cells for Smac mimetic-induced cell death. Oncogene. 2015 Jul 30;34(31):4032-43. doi: 10.1038/onc.2014.338. PubMed PMID: 25381820.

 

Products are for research use only. Not for human use.

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