2. Epigenetics PROTAC MAPK/ERK Pathway
  3. Histone Methyltransferase PROTACs KLF
  4. YZ-836P

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.

YZ-836P

YZ-836P Chemical Structure

CAS No. : 3086041-35-9

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Based on 1 publication(s) in Google Scholar

YZ-836P Related Antibodies

Top Publications Citing Use of Products

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1]. (Pink: PRMT5 ligand (HY-173562); Blue: Cereblon ligand (HY-14658); Black: linker).

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.

YZ-836P Related Antibodies

Cell Viability Assay[1]

Cell Line: HCC1806, HCC1937 triple-negative breast cancer (TNBC) cell lines
Concentration: 0, 2, 4, 6 µM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: HCC1806, HCC1937 TNBC cell lines
Concentration: 0, 2, 4, 6, 8, 10 µM (concentration-dependent); 4 µM (time-dependent)
Incubation Time: 48 h (concentration-dependent); 0, 6, 12, 24, 48, 72 h (time-dependent)
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.

Western Blot Analysis[1]

Cell Line: HCC1806, HCC1937 TNBC cell lines
Concentration: 0, 2, 4, 6 µM
Incubation Time: 48 h
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

YZ-836P (50 mg/kg; i.p.; every other day; 4 total doses) exerts potent in vivo anti-tumor activity against TNBC xenografts, reducing tumor growth without inducing measurable systemic toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (approximately 6 weeks old)[1]
Dosage: 50 mg/kg
Administration: i.p.; every other day; 4 total doses
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.
Molecular Weight

835.99

Formula

C45H57N9O7
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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
References
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YZ-836P Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YZ-836P3086041-35-9Histone MethyltransferasePROTACsKLFKrüppel-like factornude micetriple-negative breast cancer patient-derived organoidsPRMT5Protein arginine methyltransferase 5KLF5triple-negative breast cancer cellscereblontriple-negative breast cancer xenograftsCRBNHCC1806Inhibitorinhibitorinhibit

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