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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PRMT5 |
Cereblon |
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.
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.
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)
Purity & Documentation
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Data Sheet (271 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YZ-836P Related Classifications
HY-182820 Related Classifications
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