PRC1-IN-1
Based on 1 Customer Validation
PRC1-IN-1 is a PRC1 complex inhibitor. PRC1-IN-1 binds to both RING1A and RING1B proteins, and inhibits the activities of RING1B-BMI1 and RING1B-PCGF1. PRC1-IN-1 effectively inhibits H2AK119 ubiquitination and induces cell differentiation in leukemia cells. PRC1-IN-1 can be used for the research of leukemia.
For research use only. We do not sell to patients.
- Purity: 97.30%
- CAS No.: 2396639-29-3
- Formula: C24H19ClFN3O2
- Molecular Weight:435.88
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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
Biological Activity
PRC1-IN-1 (compound RB-4) (0-220 μM) binds to RING1B-BMI1, RING1A-BMI1 and RING1B-PCGF1 heterodimers with similarly high affinity, with corresponding KD values of 1.7 μM, 2.0 μM and 1.7 μM[1].
PRC1-IN-1 (0.3-24 μM) inhibits the E3 ligase activity of RING1B-BMI1, RING1A-BMI1 and RING1B-PCGF1 heterodimers in vitro, with IC50 values of 2.8 μM, 2.6 μM and 1.8 μM, respectively[1].
PRC1-IN-1 (3.1-25 μM; 4 days) inhibits global H2A ubiquitination, reduces the expression of the CD34 stem cell marker, and upregulates the expression of the CEBPα differentiation marker in TEX leukemia cells after 4 days of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TEX cells
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Concentration:3.1, 6.2, 12.5, 25 μM
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Incubation Time:4 days
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Result:Resulted in a dose-dependent loss of global H2Aub levels.
Chemical Information
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CAS No. 2396639-29-3
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Appearance Solid
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Molecular Weight 435.88
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Formula C24H19ClFN3O2
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Color Off-white to light yellow
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SMILES
CC(C1=C(NC(C(O)=O)=C1C2=C(C=CC3=C2C=CN3)Cl)C4=CC(F)=CC5=C4C=CN5)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (229.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (5.74 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.74 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (278 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 (sealed storage, away from moisture and light). 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 | 2.2942 mL | 11.4710 mL | 22.9421 mL | 57.3552 mL |
| 5 mM | 0.4588 mL | 2.2942 mL | 4.5884 mL | 11.4710 mL | |
| 10 mM | 0.2294 mL | 1.1471 mL | 2.2942 mL | 5.7355 mL | |
| 15 mM | 0.1529 mL | 0.7647 mL | 1.5295 mL | 3.8237 mL | |
| 20 mM | 0.1147 mL | 0.5736 mL | 1.1471 mL | 2.8678 mL | |
| 25 mM | 0.0918 mL | 0.4588 mL | 0.9177 mL | 2.2942 mL | |
| 30 mM | 0.0765 mL | 0.3824 mL | 0.7647 mL | 1.9118 mL | |
| 40 mM | 0.0574 mL | 0.2868 mL | 0.5736 mL | 1.4339 mL | |
| 50 mM | 0.0459 mL | 0.2294 mL | 0.4588 mL | 1.1471 mL | |
| 60 mM | 0.0382 mL | 0.1912 mL | 0.3824 mL | 0.9559 mL | |
| 80 mM | 0.0287 mL | 0.1434 mL | 0.2868 mL | 0.7169 mL | |
| 100 mM | 0.0229 mL | 0.1147 mL | 0.2294 mL | 0.5736 mL |
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