RK-701
Based on 1 Customer Validation
RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 2648855-18-7
- Formula: C26H30N4O3
- Molecular Weight:446.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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G9a 23-27 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | GI50 |
21.3 nM
Compound: S-26j; RK-701
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Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 and measured after 12 days by ATPlite assay
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 and measured after 12 days by ATPlite assay
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[PMID: 36882960] |
| MOLT-4 | GI50 |
21.3 nM
Compound: S-26j; RK-701
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Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 by ATPlite assay
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 by ATPlite assay
|
[PMID: 36882960] |
RK-701 (0.01-3 µM; 4 d) up-regulates the expression level of HbF and γ-globin mRNA without affecting cell viability or erythroid differentiation. RK-701 increases the proportion of HbF expressing cells in a concentration-dependent manner. In HUDEP-2 cells and human primary CD34+ cells, RK-701 also selectively up-regulates the expression level of BGLT3 and reduces the proportion of H3K9me2 in β-globin[1].
RK-701 (1 µM; 4 d) significantly reduces the proportion of BCL11A and ZBTB7A in BGLT3 without increasing the expression of BGLT3 in HUDEP-2 cells under the absence of BCL11A or ZBTB7A[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUDEP-2 cells and CD34+-derived cells.
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Concentration:0.01, 0.03, 0.1, 0.3, 1 and 3 µM.
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Incubation Time:4 d.
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Result:Showed activation for HbF, γ- Globin and BGLT3.
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Cell Line:HUDEP-2 cells.
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Concentration:1 µM.
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Incubation Time:4 d.
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Result:Showed inhibition for BCL11A and ZBTB7A.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2648855-18-7
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Appearance Solid
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Molecular Weight 446.54
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Formula C26H30N4O3
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Color Light yellow to yellow
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SMILES
CC1=C(C(N[C@@H](CCC2CC2)C(NC3=CC=C(C=C3)C#N)=O)=O)NC(CC(C)(C4)C)=C1C4=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (223.94 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.
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: 2.5 mg/mL (5.60 mM); Clear solution; Need ultrasonic and warming and heat to 80°C
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Purity & Documentation
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Data Sheet (274 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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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2394 mL | 11.1972 mL | 22.3944 mL | 55.9860 mL |
| 5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 11.1972 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 mL | 5.5986 mL | |
| 15 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL | 3.7324 mL | |
| 20 mM | 0.1120 mL | 0.5599 mL | 1.1197 mL | 2.7993 mL | |
| 25 mM | 0.0896 mL | 0.4479 mL | 0.8958 mL | 2.2394 mL | |
| 30 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
| 40 mM | 0.0560 mL | 0.2799 mL | 0.5599 mL | 1.3997 mL | |
| 50 mM | 0.0448 mL | 0.2239 mL | 0.4479 mL | 1.1197 mL | |
| 60 mM | 0.0373 mL | 0.1866 mL | 0.3732 mL | 0.9331 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2799 mL | 0.6998 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2239 mL | 0.5599 mL |
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