SKLB325
Based on 2 publication(s) in Google Scholar
SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .
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- Pureza: 99.21%
- No. CAS: 66680-03-3
- Fòrmula: C12H12N4O2
- Peso molecular:244.25
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
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Anti-Cancer Metabolism Compound Library
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Heterocyclic Compound Library
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Cysteine Targeted Covalent Library
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Cell Death Library
HY-L162
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
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RNA Binding Bioactive Compound Library
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Publications Citing Use of MedChemExpress (MCE) SKLB325
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Actividad biológica
SKLB325 suppresses ovarian cancer growth through inhibition of proliferation and induction of apoptosis and cell death, and inhibiting angiogenesis may play a significant role in inhibiting tumor growth[1].
SKLB325 (0.25-16 μM; for 24-72 h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4 μM, and the optimal duration of action is 72 h[1].
SKLB325 upregulates the expression of p53 and its downstream effectors at both the mRNA and protein levels in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3, ES2, A2780s and CP70 cells
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Concentration:0, 0.25, 0.5, 1, 2, 4, 8, and 16 μM
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Incubation Time:24 h, 48 h, and 72 h
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Result:With increasing SKLB325 concentration, the inhibitory effect also increased, exhibiting a significant dose-response relationship. There was a significant difference between the drug group across different doses and the control group.
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Cell Line:SKOV3, ES2 and A2780s cells
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Concentration:4 μM
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Incubation Time:72 hours
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Result:p53, p21, and PUMA protein levels were significantly upregulated in SKOV3, ES2 and A2780s cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic BALB/c nude mice[1]
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Dosage:10 mg/kg
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Administration:I.p. injections every three days for eight doses total
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Result:The average weight of intraperitoneal tumor nodules was 1.56 ± 0.70, 1.04 ± 0.62, and 0.14 ± 0.11 g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.
Chemical Information
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No. CAS 66680-03-3
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Appearance Solid
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Peso molecular 244.25
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Fòrmula C12H12N4O2
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Color White to off-white
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SMILES
OC1=NC(N/N=C/C2=CC=CC=C2O)=NC(C)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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J Transl Med
JMJD6 K375 acetylation restrains lung cancer progression by enhancing METTL14/m6A/SLC3A2 axis mediated cell ferroptosis. [Abstract]2025 Feb 26;23(1):233. PMID: 40011892 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164
Solvente y solubilidad
DMSO : 20.83 mg/mL (85.28 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)
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: ≥ 2.08 mg/mL (8.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Heng Zheng, et al. Jumonji domain-containing 6 (JMJD6) identified as a potential therapeutic target in ovarian cancer. Signal Transduct Target Ther.2019 Jul 26;4:24. [Content Brief]
[2]. Chuanjie Zhang, et al. Epigenome screening highlights that JMJD6 confers an epigenetic vulnerability and mediates sunitinib sensitivity in renal cell carcinoma. Clin Transl Med. 2021 Feb;11(2):e328. [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 | 4.0942 mL | 20.4708 mL | 40.9417 mL | 102.3541 mL |
| 5 mM | 0.8188 mL | 4.0942 mL | 8.1883 mL | 20.4708 mL | |
| 10 mM | 0.4094 mL | 2.0471 mL | 4.0942 mL | 10.2354 mL | |
| 15 mM | 0.2729 mL | 1.3647 mL | 2.7294 mL | 6.8236 mL | |
| 20 mM | 0.2047 mL | 1.0235 mL | 2.0471 mL | 5.1177 mL | |
| 25 mM | 0.1638 mL | 0.8188 mL | 1.6377 mL | 4.0942 mL | |
| 30 mM | 0.1365 mL | 0.6824 mL | 1.3647 mL | 3.4118 mL | |
| 40 mM | 0.1024 mL | 0.5118 mL | 1.0235 mL | 2.5589 mL | |
| 50 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0471 mL | |
| 60 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7059 mL | |
| 80 mM | 0.0512 mL | 0.2559 mL | 0.5118 mL | 1.2794 mL |
SKLB325 Related Classifications
HY-139782 Related Classifications
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