SP-100030
Based on 1 publication(s) in Google Scholar
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).
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- 純度: 99.57%
- CAS 番号: 154563-54-9
- 分子式: C14H5ClF9N3O
- 分子量:437.65
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 SP-100030
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | EC50 |
550 nM
Compound: 6; SP100030
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Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay
Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay
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[PMID: 39005064] |
| Jurkat | IC50 |
0.05 μM
Compound: 1, SP100030
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Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
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[PMID: 24831826] |
| Jurkat | IC50 |
0.05 μM
Compound: 1, SP100030
|
Inhibition of NF-kappaB-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
Inhibition of NF-kappaB-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
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[PMID: 24831826] |
| Jurkat | IC50 |
0.05 μM
Compound: 1
|
Concentration required to inhibit activator protein-1(AP-1) mediated transcriptional activation in human Jurkat T-cells
Concentration required to inhibit activator protein-1(AP-1) mediated transcriptional activation in human Jurkat T-cells
|
[PMID: 11052805] |
| Jurkat | IC50 |
0.05 μM
Compound: 1
|
Concentration required to inhibit nuclear factor-kappa B) mediated transcriptional activation in human Jurkat T-cells.
Concentration required to inhibit nuclear factor-kappa B) mediated transcriptional activation in human Jurkat T-cells.
|
[PMID: 11052805] |
| Jurkat | IC50 |
0.05 μM
Compound: 28
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In vitro inhibitory activity against human Jurkat T-Cells stably transfected with activating transcription factor 1
In vitro inhibitory activity against human Jurkat T-Cells stably transfected with activating transcription factor 1
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[PMID: 9484492] |
| Jurkat | IC50 |
0.05 μM
Compound: 28
|
In vitro inhibitory activity against human Jurkat T-Cells stably transfected with an Nuclear factor kappa B transcription factor
In vitro inhibitory activity against human Jurkat T-Cells stably transfected with an Nuclear factor kappa B transcription factor
|
[PMID: 9484492] |
SP-100030 blocks the production of IL-2 and IL-8 in Jurkat T-cells at the same concentrations as seen in the luciferase assay (IC50≈30 nM)[1].
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ELISA and RT-PCR confirmed that IL-2, IL-8, and TNF-alpha production by activated Jurkat and other T cell lines were inhibited by SP100030[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.
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Animal Model:Six- to 8-wk-old male DBA/1J mice (immunized with type II collagen)[2]
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Dosage:10 mg/kg
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Administration:I.p.; daily, starting at day 21 to the end of the study on day 34
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Result:Significantly decreased arthritis scores compared with controls; Histologic evaluation of the paws from mice treated from day 20 to 34 showed a trend toward decreased inflammation.
化学情報
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CAS 番号 154563-54-9
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性状 Solid
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分子量 437.65
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分子式 C14H5ClF9N3O
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Color Off-white to light yellow
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SMILES
FC(F)(F)C1=CC(C(F)(F)F)=CC(NC(C2=CN=C(Cl)N=C2C(F)(F)F)=O)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Adv
Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis. [Abstract]2025 Jan 24;11(4):eadq2395. PMID: 39841821
溶剤 & 溶解度
DMSO : 50 mg/mL (114.25 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Sullivan RW, et al. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry. J Med Chem. 1998;4 [Content Brief]
[2]. Gerlag DM, et al. The effect of a T cell-specific NF-kappa B inhibitor on in vitro cytokine production and collagen-induced arthritis. J Immunol. 2000;165(3):1652-1658. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2849 mL | 11.4247 mL | 22.8493 mL | 57.1233 mL |
| 5 mM | 0.4570 mL | 2.2849 mL | 4.5699 mL | 11.4247 mL | |
| 10 mM | 0.2285 mL | 1.1425 mL | 2.2849 mL | 5.7123 mL | |
| 15 mM | 0.1523 mL | 0.7616 mL | 1.5233 mL | 3.8082 mL | |
| 20 mM | 0.1142 mL | 0.5712 mL | 1.1425 mL | 2.8562 mL | |
| 25 mM | 0.0914 mL | 0.4570 mL | 0.9140 mL | 2.2849 mL | |
| 30 mM | 0.0762 mL | 0.3808 mL | 0.7616 mL | 1.9041 mL | |
| 40 mM | 0.0571 mL | 0.2856 mL | 0.5712 mL | 1.4281 mL | |
| 50 mM | 0.0457 mL | 0.2285 mL | 0.4570 mL | 1.1425 mL | |
| 60 mM | 0.0381 mL | 0.1904 mL | 0.3808 mL | 0.9521 mL | |
| 80 mM | 0.0286 mL | 0.1428 mL | 0.2856 mL | 0.7140 mL | |
| 100 mM | 0.0228 mL | 0.1142 mL | 0.2285 mL | 0.5712 mL |