2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis
  3. TrxR Reactive Oxygen Species (ROS) Ferroptosis
  4. CS47

CS47 is a Thioredoxin Reductase 1 (TRXR1) inhibitor and ferroptosis inducer. CS47 binds non-covalently to sites between the FAD and NADPH pockets of TRXR1. CS47 drives glutathione depletion, lipid reactive oxygen species accumulation, HMOX1-dependent iron overload, and selective cytotoxicity in lung cancer cells. CS47 can be used for the research of lung cancer.

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

CS47

CS47 Chemical Structure

CAS No. : 1372792-51-2

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CS47 Related Antibodies

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Description

CS47 is a Thioredoxin Reductase 1 (TRXR1) inhibitor and ferroptosis inducer. CS47 binds non-covalently to sites between the FAD and NADPH pockets of TRXR1. CS47 drives glutathione depletion, lipid reactive oxygen species accumulation, HMOX1-dependent iron overload, and selective cytotoxicity in lung cancer cells. CS47 can be used for the research of lung cancer[1].

In Vitro

CS47 (48 h) selectively reduces viability of KRAS-WT and EGFR-MUT human lung cancer cells in 2D culture with IC50 values of 6.74 µM and 6.78 µM, respectively, while showing much lower potency against KM lung cancer cells (IC50 = 24.22 µM) and normal IMR90 fibroblasts (IC50 = 54.85 µM)[1].
CS47 (48 h) induces potent cell death in 3D spheroids of KRAS-WT (H661, H522) and EGFR-MUT (HCC827) human lung cancer cells, but not in KM (H460) or KRAS-WT H522 cells with KM overexpression[1].
CS47 (2 μM; 24 h) induces significant lipid peroxidation in KRAS-WT human lung cancer cells (H1993, H1395), but not in KRASG12C human lung cancer cells (H157, A549)[1].
CS47 (2 μM; 24 h) alters lipid homeostasis in KRAS-WT H522 human lung cancer cells, inducing enrichment of ferroptosis-associated PUFA-containing phospholipids and accumulation of LPC and PUFA-containing TG[1].
CS47 (24 h) induces transcriptomic reprogramming in KRAS-WT and EGFR-MUT human lung cancer cells, downregulating lipid biosynthesis and selenoprotein genes while upregulating ferroptosis-related genes involved in antioxidant response, iron metabolism, and GSH homeostasis; HMOX1 is universally upregulated across all genotypes[1].

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

CS47 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUClast Vz/F CL/F MRT
Mice[1] 10 mg/kg i.p. 20.33 μg/mL 90 min 3803 min 23737567 min·ng/mL 538 mL/kg 0.098 mL/min/kg 686 min
In Vivo

CS47 (3 mg/kg; i.p.; every 3 days; 25 days) inhibits yumor growth in mouse H661 and H661-HMOX1 xenografts[1].

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

Animal Model: NCG (Nod Scid IL-2Rγ-/-) mice (9 weeks) injected with H661 and H661-HMOX1 cells[1]
Dosage: 3 mg/kg
Administration: i.p.; every 3 days; 25 days
Result: Produced a significant anti-tumor effect, with tumor volumes remaining far lower than vehicle controls throughout the 25-day treatment period.
Increased intratumoral C11-BODIPY oxidation, a marker of lipid peroxidation.
Induced accumulation of polyunsaturated fatty acid-containing phospholipids and triacylglycerols, consistent with ferroptosis.
Did not cause significant weight loss in mice.
Exhibited no marked leukopenia or neutropenia observed.
Exhibited even more pronounced anti-tumor effect in H661-HMOX1-GFPlo xenografts.
Increased intratumoral accumulation of 4-Hydroxynonenal, a marker of ferroptosis, in both parental and HMOX1-overexpressing xenografts.
Molecular Weight

595.21

Formula

C21H16AuCl2N2P
CAS No.
SMILES

ClC1=C(Cl)[N-]([Au+][P](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)C=N1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CS47 Related Classifications

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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.

Keywords:

CS471372792-51-2CS 47CS-47TrxRReactive Oxygen Species (ROS)FerroptosisThioredoxin ReductaseKRAS-WTferroptosisThioredoxin Reductase 1TRXR1HMOX1H661IMR90 fibroblastslung cancer cellsEGFR-MUTHCC827Inhibitorinhibitorinhibit

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