SH514
Based on 1 Customer Validation
SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors .
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 3099543-90-2
- 分子式: C32H38N2O4
- 分子量:514.66
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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
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
SH514 (Compound 41) (0-50 μM, 72 h) targets IRF4 at the cellular level, can selectively inhibit the proliferation of MM cell lines with high IRF4 expression, and displays no cytotoxicity for normal cells[1].
SH514 (100 μM, 1 h) can target IRF4 and reduce its thermal stability, while having almost no effect on the stability of IRF3, a member of the IRF family[1].
SH514 (0.125-1 μM, 24 h) significantly downregulates the expression of IRF4 downstream target genes in NCI-H929 and MM.1R cells, and the inhibitory effect was concentration-dependent in MM cells[1].
SH514 (0-0.5 μM, 24 h) leads to a significant increase in the proportion of cells in the G1 phase and a decrease in cells in the S and G2 phases in NCI-H929 cells[1].
SH514 (0.1-1 μM, 24 h) suppresses the expression of p-AKT, p-ERK, CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC, and increase γH2AX in NCI-H929 cells and MM.1R cells, suggesting that SH514 could induce DNA damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H929, MM.1R, RPMI-8226, HAF, HACAT
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Concentration:0-50 μM
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Incubation Time:72 h
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Result:Demonstrated potent inhibition against IRF4-high expressing cells NCI-H929 (IC50 = 0.08 μM) and MM.1R (IC50 = 0.11 μM).
Showed weaker inhibitory effects on IRF4-low expressing cells RPMI-8226 (IC50 = 1.19 μM).
Exhibited no toxicity towards normal cells, HAF and HACAT (IC50 > 100 μM).
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Cell Line:NCI-H929, MM.1R
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Concentration:0.125 μM, 0.25 μM, 0.5 μM, 1 μM
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Incubation Time:24 h
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Result:Concentration-dependently downregulated the mRNA expression of IRF4 downstream target genes, including CCNC, CANX, E2F5, CMYC, HK2, and Blimp1.
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Cell Line:NCI-H929
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Concentration:0.125 μM, 0.25 μM, 0.5 μM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at the G1 phase in NCI–H929 cells in a concentration-dependent manner.
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Cell Line:NCI-H929, MM.1R
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Concentration:0.1 μM, 0.3 μM, 0.5 μM, 1 μM
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Incubation Time:24 h
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Result:Concentration gradients inhibited the expression of the cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in NCI–H929 cells and MM.1R cells.
| Species | Dose | Route | Tmax | Cmax | AUC0-t | AUC0-∞ | Vz | CL | T1/2 | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice | 1 mg/kg | i.v. | 0.08 h | 174 ng/mL | 81 ng·h/mL | 86 ng·h/mL | 20807 mL/kg | 11818 mL/min/kg | 1.25 h | / |
| Mice | 10 mg/kg | p.o. | 0.53 h | 82 ng/mL | 285 ng·h/mL | 463 ng·h/mL | / | / | 6.71 h | 53.85 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:1 × 107 of H929 cells were injected subcutaneously into BALB/c nude mice by mixing 1:1 with matrix gel[1].
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Dosage:12.5 mg/kg, 25 mg/kg
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Administration:Oral gavage, once daily for 34 days
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Result:Significantly inhibited the tumor volume in mice in a dose-dependent manner.
The body weight of mice showed an overall increasing trend, indicating that the compound had no toxic effect on mice.
Significantly reduced the expression of Ki67.
Effectively inhibited the proliferation of MM tumors in mice without causing toxic effects.
化学情報
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CAS 番号 3099543-90-2
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性状 Solid
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分子量 514.66
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分子式 C32H38N2O4
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Color White to off-white
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SMILES
C[C@]12CC[C@@]3([H])[C@@]([H])(C(C=C4C(C)(C(C(C#N)=C[C@@]43C)=O)C)=O)[C@]1([H])CC[C@@H]2[C@@H](C(NC5=CC=C(C=C5)OC)=O)C
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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
溶剤 & 溶解度
DMSO : 100 mg/mL (194.30 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)
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.
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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 1.9430 mL | 9.7152 mL | 19.4303 mL | 48.5758 mL |
| 5 mM | 0.3886 mL | 1.9430 mL | 3.8861 mL | 9.7152 mL | |
| 10 mM | 0.1943 mL | 0.9715 mL | 1.9430 mL | 4.8576 mL | |
| 15 mM | 0.1295 mL | 0.6477 mL | 1.2954 mL | 3.2384 mL | |
| 20 mM | 0.0972 mL | 0.4858 mL | 0.9715 mL | 2.4288 mL | |
| 25 mM | 0.0777 mL | 0.3886 mL | 0.7772 mL | 1.9430 mL | |
| 30 mM | 0.0648 mL | 0.3238 mL | 0.6477 mL | 1.6192 mL | |
| 40 mM | 0.0486 mL | 0.2429 mL | 0.4858 mL | 1.2144 mL | |
| 50 mM | 0.0389 mL | 0.1943 mL | 0.3886 mL | 0.9715 mL | |
| 60 mM | 0.0324 mL | 0.1619 mL | 0.3238 mL | 0.8096 mL | |
| 80 mM | 0.0243 mL | 0.1214 mL | 0.2429 mL | 0.6072 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4858 mL |
SH514 関連分類
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