YZ-836P
Based on 1 Customer Validation
YZ-836P is a Protein arginine methyltransferase 5 (PRMT5) targeting agent. YZ-836P promotes ubiquitination and proteasomal degradation of PRMT5 in a cereblon (CRBN)-dependent manner, which in turn reduces levels of its downstream target KLF5. YZ-836P induces G1 phase cell cycle arrest in triple-negative breast cancer cells. YZ-836P induces Apoptosis in triple-negative breast cancer cells. YZ-836P exerts cytotoxic effects on triple-negative breast cancer cells. YZ-836P inhibits the growth of triple-negative breast cancer patient-derived organoids. YZ-836P inhibits the growth of triple-negative breast cancer xenografts in nude mice. YZ-836P can be used for the research of triple-negative breast cancer.
(Pink: PRMT5 ligand (HY-173562); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3086041-35-9
- Formula: C45H57N9O7
- Molecular Weight:835.99
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Storage:
-20°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)
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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PRMT5 |
Cereblon |
In Vitro
YZ-836P (0-6 µM; 48 h) potently reduces cell viability in HCC1806 (IC50 = 2.1 µM) and HCC1937 (IC50 = 1.0 µM) TNBC cell lines after 48 h treatment[1].
YZ-836P (0-10 µM; 48 h) and (4 µM; 0-72 h) dose-dependently and time-dependently reduces PRMT5 and KLF5 protein levels in HCC1806 and HCC1937 TNBC cell lines[1].
YZ-836P (0.25-1.00 µM; 2 days) concentration-dependently inhibits colony formation in HCC1806 and HCC1937 TNBC cell lines when applied for an initial 2-day treatment[1].
YZ-836P (1-6 µM; 24 h) concentration-dependently inhibits DNA synthesis in HCC1806 and HCC1937 TNBC cell lines after 24 h treatment[1].
YZ-836P (2-6 µM; 48 h) concentration-dependently induces G1 phase cell cycle arrest in HCC1806 and HCC1937 TNBC cell lines after 48 h treatment[1].
YZ-836P (2-6 µM; 48 h) concentration-dependently modulates cell cycle-related protein expression (reduces Cyclin D1, CDK4, CDK6; increases p21, p27) in HCC1806 and HCC1937 TNBC cell lines after 48 h treatment[1].
YZ-836P (2-6 µM; 48 h) concentration-dependently modulates apoptosis-related protein expression (increases cleaved PARP, cleaved Caspase 3; reduces XIAP, Mcl-1) in HCC1806 and HCC1937 TNBC cell lines after 48 h treatment[1].
YZ-836P (2-6 µM; 48 h) concentration-dependently induces apoptosis in HCC1806 and HCC1937 TNBC cell lines after 48 h treatment[1].
YZ-836P (4 µM) directly binds to PRMT5, increasing its thermostability (CETSA assay) and reducing its susceptibility to protease degradation (DARTS assay) in HCC1806 and HCC1937 TNBC cell lines[1].
YZ-836P (4 µM; 48 h) increases PRMT5 ubiquitination and promotes CRBN-dependent, proteasomal-mediated degradation of PRMT5 in HEK293T cells[1].
YZ-836P (0-10 µM; 48 h) potently reduces viability of TNBC patient-derived organoids PDO-32 (IC50 = 2.072 µM) and PDO-33 (IC50 = 4.746 µM) after 48 h treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC1806, HCC1937 triple-negative breast cancer (TNBC) cell lines
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Concentration:0, 2, 4, 6 µM
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Incubation Time:48 h
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Result:Significantly reduced cell viability of HCC1806 and HCC1937 cells.
Exhibited IC50 values of 2.1 µM in HCC1806 cells and 1.0 µM in HCC1937 cells.
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Cell Line:HCC1806, HCC1937 TNBC cell lines
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Concentration:0, 2, 4, 6, 8, 10 µM (concentration-dependent); 4 µM (time-dependent)
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Incubation Time:48 h (concentration-dependent); 0, 6, 12, 24, 48, 72 h (time-dependent)
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Result:Dramatically decreased protein levels of PRMT5 and its downstream target KLF5 in both cell lines.
Reduced levels in a concentration-dependent manner (0-10 µM, 48 h) and a time-dependent manner (4 µM, 0-72 h).
Detected reductions as early as 6 h.
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Cell Line:HCC1806, HCC1937 TNBC cell lines
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Concentration:0, 2, 4, 6 µM
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Incubation Time:48 h
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Result:Reduced protein levels of Cyclin D1, CDK4, and CDK6, and increased levels of p21 and p27 in both cell lines in a concentration-dependent manner.\nPromoted a concentration-dependent increase of cleaved PARP and cleaved Caspase 3, and reduced levels of anti-apoptotic proteins XIAP and Mcl-1 in both cell lines.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (approximately 6 weeks old)[1]
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Dosage:50 mg/kg
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Administration:i.p.; every other day; 4 total doses
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Result:Reduced tumor volumes and weights significantly compared to control.
Increased the proportion of cleaved Caspase 3-positive cells in tumor tissue significantly.
Caused no significant changes in mouse body weight, serum creatinine, alanine transaminase, or aspartate transaminase levels relative to controls.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3086041-35-9
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Appearance Solid
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Molecular Weight 835.99
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Formula C45H57N9O7
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Color Light yellow to yellow
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SMILES
O=C1N(C2C(NC(CC2)=O)=O)C(C3=CC=C(NCCCCCCCCCC(N4CCC(CC4)NC5=NC=NC(C(NC[C@H](O)CN6CC7=CC=CC=C7CC6)=O)=C5)=O)C=C31)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°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
In Vitro:
DMSO : 100 mg/mL (119.62 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 (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)
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 (2.99 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (2.99 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.
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. * 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 (276 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 |
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| DMSO | 1 mM | 1.1962 mL | 5.9809 mL | 11.9619 mL | 29.9047 mL |
| 5 mM | 0.2392 mL | 1.1962 mL | 2.3924 mL | 5.9809 mL | |
| 10 mM | 0.1196 mL | 0.5981 mL | 1.1962 mL | 2.9905 mL | |
| 15 mM | 0.0797 mL | 0.3987 mL | 0.7975 mL | 1.9936 mL | |
| 20 mM | 0.0598 mL | 0.2990 mL | 0.5981 mL | 1.4952 mL | |
| 25 mM | 0.0478 mL | 0.2392 mL | 0.4785 mL | 1.1962 mL | |
| 30 mM | 0.0399 mL | 0.1994 mL | 0.3987 mL | 0.9968 mL | |
| 40 mM | 0.0299 mL | 0.1495 mL | 0.2990 mL | 0.7476 mL | |
| 50 mM | 0.0239 mL | 0.1196 mL | 0.2392 mL | 0.5981 mL | |
| 60 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4984 mL | |
| 80 mM | 0.0150 mL | 0.0748 mL | 0.1495 mL | 0.3738 mL | |
| 100 mM | 0.0120 mL | 0.0598 mL | 0.1196 mL | 0.2990 mL |
YZ-836P Related Classifications
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