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.

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CS47

CS47 構造式

CAS 番号 : 1372792-51-2

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CS47 関連抗体

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製品説明

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].

体外実験

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 関連抗体
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
体内実験

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.
分子量

595.21

分子式

C21H16AuCl2N2P
CAS 番号
SMILES

ClC1=C(Cl)[N-]([Au+][P](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)C=N1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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CS47 Related Classifications

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  • 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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