| Field | Specification |
|---|---|
| Target | |
| Alternative names | GK 01140 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C9H8N2OS2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
SC-514, also known as GK 01140, is a selective IKK-2 inhibitor (IC50 = 11.2 μM) that does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases. It is supplied as a light yellow to yellow solid (C9H8N2OS2, MW 224.30) at 99.97% purity.
Physical & Chemical Properties
| CAS Number | 354812-17-2 |
|---|---|
| Molecular Formula | C9H8N2OS2 |
| Molecular Weight | 224.30 g/mol |
| Purity | 99.97% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C(C1=C(N)C=C(C2=CSC=C2)S1)N |
| Target | IKK-2, CDK2/A, AUR2, PRAK, MSK |
| Signaling Pathway | NF-κB |
| Solubility | In Vitro: DMSO: 50 mg/mL (222.92 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
IKK-2 11.2 μM (IC50) |
CDK2/A 61 μM (IC50) |
AUR2 71 μM (IC50) |
PRAK 75 μM (IC50) |
MSK 123 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (222.92 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (11.15 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (11.15 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (11.15 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
SC-514 inhibits the native IKK complex and the recombinant human IKK-1/IKK-2 heterodimer, with IC50s of 6.1±2.2 μM and 2.7±0.7 μM, respectively. The inhibition of IKK-2 by SC-514 is selective, reversible, and ATP-competitive. In IL-1β-induced synovial fibroblasts derived from rheumatoid arthritis, SC-514 suppresses transcription of NF-κB-dependent genes in a dose-dependent manner. SC-514 also inhibits every recombinant human IKK-2 form tested, including rhIKK-2 homodimer, rhIKK-1/rhIKK-2 heterodimer, and the constitutively active form of rhIKK-2, with comparable IC50 values spanning 3-12 μM[1]. To test whether the reactive oxygen species (ROS)-inducing IKKβ inhibitor raises the sensitivity of melanoma cells to nitrosourea, responses to SC-514/Fotemustine co-treatment are assessed first. Melanoma cell lines receive 50 μM SC-514 and Fotemustine, alone or combined, for 48 h, and growth inhibition is measured. Co-treatment with SC-514 significantly increases Fotemustine-induced cytotoxicity in all melanoma cell lines tested[2].
In Vivo
SC-514 is effective in an acute inflammation model, LPS-induced serum TNFα production in the rat. It inhibits TNFα production in a dose-dependent manner, thereby validating IKK-2 as a potential in vivo anti-inflammatory drug target[1]. To gather in vivo evidence on the role of SC-514 in the response of cancer cells to Fotemustine, a melanoma xenograft mouse model is used. Nude mice engrafted with A375 or G361 tumors receive vehicle control, 25 mg/kg SC-514, and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days while tumor behavior is monitored. Fotemustine given with SC-514 shows a clear combined effect and reduces tumor size in mice[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[2]
For the crystal violet staining assay, seed melanoma cell lines (1×104) in 60 mm dishes, then leave untreated or pretreat with SC-514 (50 μM) and/or Fotemustine. Fix the cells with formalin and stain with crystal violet. Measure cell numbers as optical density at 595 nm (OD595), reading solubilized crystal violet from the formalin-fixed cells. Also determine cytotoxicity by the MTT reduction assay[2].
Animal Administration[1][2]
Rats[1] Administer SC-514 or vehicle (2% Me2SO in saline) by oral gavage at 50 mg/kg or intraperitoneally at 10 and 50 mg/kg to adult male Wistar rats fasted overnight. Two hours after compound treatment, give 1 mg/kg LPS (Escherichia coli) in saline intraperitoneally. At 90 min after LPS administration, bleed the animals and analyze serum TNFα levels by a rat-specific TNFα ELISA. Mice[2] House male nu/nu BALB/c mice (6 weeks old) in individual ventilated cages. Resuspend A375 or G361 (5×106) cells in 0.1 mL PBS, inoculate subcutaneously into the backs of nude mice, and allow growth for 7 days. Then randomly assign mice to 4 groups (n=6 for each group) and treat by intraperitoneal injection with 25 mg/kg SC-514 and/or Fotemustine (25 mg/kg), daily for 13-15 consecutive days, using 200 μL 30% PEG/5% Tween-80 solution as the vehicle control. Measure body weight and tumor volume every 3 days. Determine tumor volumes with a caliper and calculate them. At the end of the experiment, sacrifice the mice and collect tumor xenografts. Store tumor tissues at -80°C for Western blot analysis.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Regulation of Neuroinflammation by Microglial DUBA-IRAK1-IKKβ Signaling Loop. Adv Sci (Weinh) 2025 Aug 4:e03972. PMID: 40755418
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. ACS Environ Au 2025 Aug 5;5(6):573-582. PMID: 41277996
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. Anal Chem 2025 Jun 3;97(21):11099-11109. PMID: 40401576
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. J Ethnopharmacol 2025 Aug 29:352:120267. PMID: 40633861
Upregulation of miR-520c-3p via hepatitis B virus drives hepatocellular migration and invasion by the PTEN/AKT/NF-κB axis. Mol Ther Nucleic Acids 2022 May 20:29:47-63. PMID: 35795482
Attenuation of NF-κB in Intestinal Epithelial Cells Is Sufficient to Mitigate the Bone Loss Comorbidity of Experimental Mouse Colitis. J Bone Miner Res 2019 Oct;34(10):1880-1893. PMID: 31107556
Cryptosporidium parvum upregulates miR-942-5p expression in HCT-8 cells via TLR2/TLR4-NF-κB signaling. Parasit Vectors 2020 Aug 31;13(1):435. PMID: 32867835
Inhibition of IκB Kinase 2 Attenuated the Proliferation and Induced Apoptosis of Gastric Cancer. Dig Dis Sci 2019 May;64(5):1204-1216.
bioRxiv. 2023 Apr 17.
