SC-514
Based on 9 publication(s) in Google Scholar
SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.97%
- CAS. Nr.: 354812-17-2
- Formel: C9H8N2OS2
- Molecular Weight:224.30
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
NF-κB Signaling Compound Library
HY-L014
-
Stem Cell Signaling Compound Library
HY-L017
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Differentiation Inducing Compound Library
HY-L038
-
Pyroptosis Compound Library
HY-L059
-
Targeted Diversity Library
HY-L099
-
Anti-Liver Cancer Compound Library
HY-L101
-
Human Metabolite Library
HY-L123
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) SC-514
More- Adv Sci (Weinh). 2025 Aug 4:e03972. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- J Ethnopharmacol. 2025 Aug 29:352:120267. [Abstract]
- Mol Ther Nucleic Acids. 2022 May 20:29:47-63. [Abstract]
- J Bone Miner Res. 2019 Oct;34(10):1880-1893. [Abstract]
- Parasit Vectors. 2020 Aug 31;13(1):435. [Abstract]
- Dig Dis Sci. 2019 May;64(5):1204-1216. [Abstract]
- bioRxiv. 2023 Apr 17.
Customer Validation & Images
-
WB
Biologische Aktivität
|
IKK-2 11.2 μM (IC50) |
CDK2/A 61 μM (IC50) |
AUR2 71 μM (IC50) |
PRAK 75 μM (IC50) |
MSK 123 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
7.9 μM
Compound: SC415
|
Inhibition of TNFalpha-induced NFkappaB activation in mouse NIH-3T3 cells expressing NFkappaB (unknown origin) preincubated for 15 mins followed by TNFalpha addition measured after 6 hrs by luciferase reporter gene assay
Inhibition of TNFalpha-induced NFkappaB activation in mouse NIH-3T3 cells expressing NFkappaB (unknown origin) preincubated for 15 mins followed by TNFalpha addition measured after 6 hrs by luciferase reporter gene assay
|
[PMID: 27352042] |
SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer with IC50s of 6.1±2.2 μM and 2.7±0.7 μM, respectively. IKK-2 inhibition by SC-514 is selective, reversible, and competitive with ATP. SC-514 inhibits transcription of NF-κB-dependent genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent manner. SC-514 inhibits all forms of recombinant human IKK-2 including rhIKK-2 homodimer, rhIKK-1/rhIKK-2 heterodimer, as well as the constitutively active form of rhIKK-2 with comparable IC50 values in the 3-12 μM range[1]. To evaluate whether the reactive oxygen species (ROS)-inducing IKKβ inhibitor increases the sensitivity of melanoma cells to nitrosourea. The responses of melanoma cells are first assessed to SC-514/Fotemustine co-treatment. Melanoma cell lines are treated with 50 μM of SC-514 and Fotemustine alone and in combination for 48 h and growth inhibition is assessed. Co-treatment with SC-514 significantly enhances Fotemustine-induced cytotoxicity in all melanoma cell lines tested[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 354812-17-2
-
Appearance Solid
-
Molecular Weight 224.30
-
Formel C9H8N2OS2
-
Color Light yellow to yellow
-
SMILES
O=C(C1=C(N)C=C(C2=CSC=C2)S1)N
-
Synonyms
GK 01140
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
Adv Sci (Weinh)
2025 Aug 4:e03972. PMID: 40755418 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
J Ethnopharmacol
Elephantopus scaber attenuates MC903-caused atopic dermatitis and decreases TNF-α/IFN-γ-induced chemokines by suppressing MKP-1-mediated AP-1 signaling in keratinocytes. [Abstract]2025 Aug 29:352:120267. PMID: 40633861 -
Mol Ther Nucleic Acids
Upregulation of miR-520c-3p via hepatitis B virus drives hepatocellular migration and invasion by the PTEN/AKT/NF-κB axis. [Abstract]2022 May 20:29:47-63. PMID: 35795482 -
J Bone Miner Res
Attenuation of NF-κB in Intestinal Epithelial Cells Is Sufficient to Mitigate the Bone Loss Comorbidity of Experimental Mouse Colitis. [Abstract]2019 Oct;34(10):1880-1893. PMID: 31107556 -
Parasit Vectors
Cryptosporidium parvum upregulates miR-942-5p expression in HCT-8 cells via TLR2/TLR4-NF-κB signaling. [Abstract]2020 Aug 31;13(1):435. PMID: 32867835 -
Dig Dis Sci
Inhibition of IκB Kinase 2 Attenuated the Proliferation and Induced Apoptosis of Gastric Cancer. [Abstract]2019 May;64(5):1204-1216. PMID: 30560335
SC-514 purchased from MedChemExpress. Usage Cited in: Dig Dis Sci. 2019 May;64(5):1204-1216. [Abstract]
The expression of BAX, Bcl2, P53, PARP, cleaved caspase 3, and cleaved caspase 9 in SGC-7901 cells is measured by western blotting in the treatment of SC-514.
-
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (222.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (11.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protokoll
IKK complexes are immunoprecipitated from IL-1β-treated RASF cell lysates (0.5-2 mg) using a NEMO antibody (3-10 μg) followed by the addition of protein A-agarose beads. Antibody complexes are pelleted by centrifugation and washed 3 times with 1 mL of cold whole-cell lysis buffer followed by 2 washes in kinase buffer (25 mM HEPES, pH 7.6, 2 mM MgCl2, 2 mM MnCl2, 10 mM NaF, 5 mM DTT, and 1 mM phenylmethylsulfonyl fluoride). 100-200 μg of immunoprecipitated IKK is analyzed for kinase activity in a reaction containing 10 μM biotinylated IκBα peptide as substrate and 1 μM [γ-33P]ATP (2500 Ci/mmol). After incubation at room temperature for 30 min, 25 μL of the reaction mixture is withdrawn and added to a SAM 96 biotin capture plate. After successive wash steps the plate was allowed to air-dry, and 25 μL of scintillation fluid is added to each well. Incorporation of [γ-33P]ATP is measured using a Top-Count NXT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For crystal violet staining assay, melanoma cell lines (1×104) are seeded in 60 mm dishes, and then untreated or pretreated with SC-514 (50 µM) and/or Fotemustine. Then, cells are formalin-fixed and stained with crystal violet. Cell numbers are measured as the optical density at 595 nm (OD595) of solubilized crystal violet from formalin-fixed cells. Cytotoxicity are also determined by the MTT reduction assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
SC-514 or vehicle (2% Me2SO in saline) is administered either by oral gavage (50 mg/kg) or intraperitoneally (10 and 50 mg/kg) to adult male Wistar rats that have been deprived of food overnight. Two hours after compound treatment, 1 mg/kg LPS (Escherichia coli) in saline is administered intraperitoneally 90 min after LPS administration; the animals are bled and serum TNFα levels analyzed by a rat-specific TNFα ELISA.
Mice[2]
Male nu/nu BALB/c mice (6 weeks old) are maintained in individual ventilated cages. A375 or G361 (5×106) cells are resuspended in 0.1 mL PBS and inoculated subcutaneously into the backs of nude mice and allowed to grow for 7 days. After that, mice are randomly assigned to 4 groups (n=6 for each group) and treated by intraperitoneal injection with 200 µL 30% PEG/5% Tween-80 solution as the vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days. Body weight and tumor volume are measured every 3 days. Tumor volumes are determined by a caliper and calculated. At the end of the experiment, mice are sacrificed and tumor xenografts are collected. Tumor tissues are stored at -80°C for Western blot analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (283 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Kishore N, et al. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71. [Content Brief]
[2]. Tse AK, et al. Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. Redox Biol. 2017 Apr;11:562-576. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4583 mL | 22.2916 mL | 44.5831 mL | 111.4579 mL |
| 5 mM | 0.8917 mL | 4.4583 mL | 8.9166 mL | 22.2916 mL | |
| 10 mM | 0.4458 mL | 2.2292 mL | 4.4583 mL | 11.1458 mL | |
| 15 mM | 0.2972 mL | 1.4861 mL | 2.9722 mL | 7.4305 mL | |
| 20 mM | 0.2229 mL | 1.1146 mL | 2.2292 mL | 5.5729 mL | |
| 25 mM | 0.1783 mL | 0.8917 mL | 1.7833 mL | 4.4583 mL | |
| 30 mM | 0.1486 mL | 0.7431 mL | 1.4861 mL | 3.7153 mL | |
| 40 mM | 0.1115 mL | 0.5573 mL | 1.1146 mL | 2.7864 mL | |
| 50 mM | 0.0892 mL | 0.4458 mL | 0.8917 mL | 2.2292 mL | |
| 60 mM | 0.0743 mL | 0.3715 mL | 0.7431 mL | 1.8576 mL | |
| 80 mM | 0.0557 mL | 0.2786 mL | 0.5573 mL | 1.3932 mL | |
| 100 mM | 0.0446 mL | 0.2229 mL | 0.4458 mL | 1.1146 mL |
SC-514 Related Classifications
HY-13802 Related Classifications
Powered by Bioz