KSI-028
Based on 1 Customer Validation
KSI-028 is a STING inhibitor. KSI-028 disrupts STING-mediated signal transduction, reduces IFN-β and pro-inflammatory cytokine (IL-6, IL-1β and TNF-α) production. KSI-028 inhibits the phosphorylation of STING, TBK1, IRF3, and STAT1. KSI-028 attenuates renal and hepatic injury in a Cisplatin (HY-17394)-induced acute kidney injury mouse model.
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- Purity : 98.42%
- 화학식: C18H14N4O5S
- 분자량:398.39
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
IL-1β |
IL-6 |
TBK1 |
STAT1 |
In Vitro
KSI-028 (0.3-20 μM; 1 h pretreatment) potently inhibits STING-dependent ISRE reporter activity in RAW264.7 cells with an IC50 of 0.652 μM for cGAMP (HY-12512) (10 μg/mL)-induced activity and 2.261 μM for MSA-2 (HY-136927) (100 μM)-induced activity, while maintaining high cell viability[1].
KSI-028 (0.3-20 μM; 1 h pretreatment) dose-dependently inhibits STING-dependent ISRE reporter activity in human THP-1 cells without inducing cytotoxicity[1].
KSI-028 (1.25-20 μM; 2 h pretreatment) potently suppresses STING-dependent IFN-β cytokine and IL-6, TNF-α pro-inflammatory factor production in RAW264.7 cells following stimulation with cGAMP or MSA-2[1].
KSI-028 (5-10 μM; 2 h pretreatment) disrupts STING-mediated signal transduction in RAW264.7 cells by inhibiting the phosphorylation of STING, TBK1, IRF3, and STAT1[1].
KSI-028 (20 μM) directly engages STING in intact RAW264.7 and THP-1 cells, increasing the protein's thermal stability[1].
KSI-028 (5-10 μM; 2 h pretreatment) broadly suppresses STING-dependent interferon-stimulated gene expression in RAW264.7 cells activated by cGAMP or MSA-2[1].
KSI-028 (10 μM; 5 min) exhibits modest, partial inhibition of human CYP450 isoforms 1A2, 2C9, 2D6, and 3A4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine RAW264.7 cells
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Concentration:5, 10 μM
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Incubation Time:2 h pretreatment
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Result:Markedly reduced the phosphorylation of STING, TBK1, IRF3, and STAT1 following stimulation with either cGAMP or MSA-2.
Left total protein levels of STING, TBK1, IRF3, and STAT1 unchanged.
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Cell Line:murine RAW264.7 cells
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Concentration:5, 10 μM
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Incubation Time:2 h pretreatment
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Result:Significantly suppressed the transcription of multiple ISGs including ifnb, cxcl10, isg15, irf7, oas1a, ifit1, ifit2, ifit3, pkr, and rsad2 in cells activated by either cGAMP or MSA-2.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute kidney injury C57BL/6J mice (male, 8 weeks old, Cisplatin-induced acute kidney injury)[1]
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Dosage:30 mg/kg
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Administration:i.p.; twice daily; 3 days
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Result:Significantly reduced blood urea nitrogen and serum creatinine levels compared to the Cisplatin-only group.
Significantly lowered serum aspartate aminotransferase and alanine aminotransferase levels.
Substantially attenuated Cisplatin-induced elevations in mRNA levels of interferon-stimulated genes including ifnb, cxcl10, isg15, and irf7, as well as pro-inflammatory cytokine genes including IL-6, TNF-α, and IL-1β.
Reduced Cisplatin-induced increases in STING protein levels, phosphorylated TBK1, and phosphorylated p65.
Showed no significant systemic toxicity based on survival and body weight monitoring.
Chemical Information
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Appearance Solid
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분자량 398.39
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화학식 C18H14N4O5S
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SMILES
O=C(C1=CC=C(O1)[N+]([O-])=O)NC2=CC3=C(CCCN3C(C4=CC=NS4)=O)C=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (251.01 mM; ultrasonic and warming and heat to 60°C; 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.
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: ≥ 2.5 mg/mL (6.28 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
순도&문서
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Data Sheet (281 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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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 2.5101 mL | 12.5505 mL | 25.1010 mL | 62.7526 mL |
| 5 mM | 0.5020 mL | 2.5101 mL | 5.0202 mL | 12.5505 mL | |
| 10 mM | 0.2510 mL | 1.2551 mL | 2.5101 mL | 6.2753 mL | |
| 15 mM | 0.1673 mL | 0.8367 mL | 1.6734 mL | 4.1835 mL | |
| 20 mM | 0.1255 mL | 0.6275 mL | 1.2551 mL | 3.1376 mL | |
| 25 mM | 0.1004 mL | 0.5020 mL | 1.0040 mL | 2.5101 mL | |
| 30 mM | 0.0837 mL | 0.4184 mL | 0.8367 mL | 2.0918 mL | |
| 40 mM | 0.0628 mL | 0.3138 mL | 0.6275 mL | 1.5688 mL | |
| 50 mM | 0.0502 mL | 0.2510 mL | 0.5020 mL | 1.2551 mL | |
| 60 mM | 0.0418 mL | 0.2092 mL | 0.4184 mL | 1.0459 mL | |
| 80 mM | 0.0314 mL | 0.1569 mL | 0.3138 mL | 0.7844 mL | |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6275 mL |
KSI-028 Related Classifications
HY-183537 Related Classifications
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