NCI677397
Based on 1 publication(s) in Google Scholar
NCI677397 is a USP24 inhibitor. NCI677397 increases lipid ROS, activates cholesterol and fatty acid biosynthesis, degrades ABC transporters, GPX4 and DHFR through the autophagy pathway, decreases the level of P-gp and ultimately leads to ferroptosis in drug-resistant cancer cells. NCI677397 can be used for the study of lung caner and brain cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 907547-06-2
- Fòrmula: C28H31N3OS
- Peso molecular:457.63
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NCI677397
More
Actividad biológica
Descripciòn
IC50 & Target
|
GPX4 |
In Vitro
NCI677397 (0-120 nM, 24 h-7 d) effectively reverses drug resistance in multiple cancer types: Lung cancer (T24 cells) resistant to Taxol, Brain cancer (Pt3-TMZR and U87-R cells) resistant to TMZ (HY-17364), Nasopharyngeal cancer (Hone-1-CPTR cells) resistant to CPT (HY-16560) and Colorectal cancer (HCT116-OXR cells) resistant to Oxaliplatin (HY-17371)[2].
NCI677397 (10 and 20 μM, 4 days) significantly reduces the viability of TMZ-sensitive and -resistant GBM cells and there is a synergistic effect combined with TMZ[1].
NCI677397 (0-20 μM, 24 h) induces autophagy, not apoptosis in both TMZ-sensitive and TMZ-resistant GBM cells and A549 and Taxol-resistant A549 (A549-T24) cells[1].
NCI677397 (0-15 μM, 24 h) induces the biosynthesis of cholesterol and fatty acid in U87, U87R, Pt’3, Pt’3R, A549 and A549-T24 cells[1].
NCI677397 (0-25 μM, 24 h) induces ferroptosis mediated via lipid ROS in U87, U87R, Pt’3, Pt’3R and A549-T24 cells[1].
NCI677397 (0-25 μM, 24 h) degrades ABCG1/5/8 through the autophagy pathway and reduces the stability of GPX4 and DHFR in Pt’3R and A549-T24 cells[1].
NCI677397 (20 μM, 0-24 h) induces lipid peroxidation within 2 hours, upregulates cholesterol synthase 6 hours later, and completes the ferroptosis process 24 hours later in Pt’3R cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:TMZ-sensitive GBM cells (Pt’3, A172 and U87 cells) and TMZ-resistant GBM cells (Pt’3R, A172R and U87R cells)
-
Concentration:0, 10 and 20 μM
-
Incubation Time:4 days
-
Result:Significantly decreased the viability combined with TMZ treatment.
-
Cell Line:TMZ-sensitive GBM cells (Pt’3, A172 and U87 cells) and TMZ-resistant GBM cells (Pt’3R, A172R and U87R cells)
-
Concentration:0, 5, 10, 15, 20 μM
-
Incubation Time:24 h
-
Result:Increased the levels of autophagosome-associated lipidated form of LC3B (LC3B-II).
Did not increase the levels of Bax, an apoptotic marker.
Increased autophagic and apoptotic cell death with TMZ.
-
Cell Line:Pt’3R cells
-
Concentration:15 μM
-
Incubation Time:24 h
-
Result:Induced accumulation of LC3B spots.
-
Cell Line:Pt’3, Pt’3R and A549-T24cells
-
Concentration:0, 5, 10, 15, 20, 25 μM
-
Incubation Time:24 h
-
Result:Increased the levels of p-IRE1a, Bip, XBP1, p-eIF2a and CHOP in Pt’3 cells.
Increased the levels of ACSL3 and ACSL4 in brain and lung cancer cells.
Increased heme oxygenase-1 (HO-1) and p62/SQSTM1.
Induced SLC47A1 upregulation in both A549-T24 and Pt30R cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:U87R xenograft model established in male nonobese diabetic/severe combined immunodeficiency mice (8 weeks old)[1]
-
Dosage:20 mg/kg
-
Administration:Intraperitoneal injection (i.p.), twice a week for 7 weeks
-
Result:Led to smaller tumor size and lowered tumor weight.
Chemical Information
-
No. CAS 907547-06-2
-
Peso molecular 457.63
-
Fòrmula C28H31N3OS
-
SMILES
O=C(C1=CC=C2SC3=C(N(CCCCN4CCN(CC4)C)C2=C1)C=CC=C3)C5=CC=CC=C5
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Poult Sci
Ferroptosis bridges early-life oxidative stress and lifetime meat quality defects in broilers. [Abstract]2026 May 15;105(8):107133. PMID: 42184739
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (218.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
-
ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
-
Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
-
Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
-
Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
-
Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Pureza y Documentación
Referencias
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1852 mL | 10.9259 mL | 21.8517 mL | 54.6293 mL |
| 5 mM | 0.4370 mL | 2.1852 mL | 4.3703 mL | 10.9259 mL | |
| 10 mM | 0.2185 mL | 1.0926 mL | 2.1852 mL | 5.4629 mL | |
| 15 mM | 0.1457 mL | 0.7284 mL | 1.4568 mL | 3.6420 mL | |
| 20 mM | 0.1093 mL | 0.5463 mL | 1.0926 mL | 2.7315 mL | |
| 25 mM | 0.0874 mL | 0.4370 mL | 0.8741 mL | 2.1852 mL | |
| 30 mM | 0.0728 mL | 0.3642 mL | 0.7284 mL | 1.8210 mL | |
| 40 mM | 0.0546 mL | 0.2731 mL | 0.5463 mL | 1.3657 mL | |
| 50 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0926 mL | |
| 60 mM | 0.0364 mL | 0.1821 mL | 0.3642 mL | 0.9105 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2731 mL | 0.6829 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2185 mL | 0.5463 mL |
NCI677397 Related Classifications
HY-176557 Related Classifications
Powered by Bioz