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

YZ-836P 是一种 PRMT5 PROTAC 降解剂。YZ-836P 可通过依赖 CRBN 的方式促进 PRMT5 的泛素化和蛋白酶体降解，进而降低其下游靶点 KLF5 的水平。YZ-836P 可诱导三阴性乳腺癌细胞发生 G1 期细胞周期阻滞。YZ-836P 可诱导三阴性乳腺癌细胞凋亡 (Apoptosis)。YZ-836P 对三阴性乳腺癌细胞具有细胞毒性作用。YZ-836P 可抑制三阴性乳腺癌患者来源类器官的生长。YZ-836P 可抑制裸鼠体内三阴性乳腺癌异种移植物的生长。YZ-836P 可用于三阴性乳腺癌的相关研究。
(粉色: PRMT5 配体 (HY-173562)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子)。

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YZ-836P

YZ-836P Chemical Structure

CAS No. : 3086041-35-9

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1 mg ￥3100
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YZ-836P 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

YZ-836P (0-6 µM; 48 h) 可强效降低 HCC1806 (IC50 = 2.1 µM) 和 HCC1937 (IC50 = 1.0 µM) 三阴性乳腺癌 (TNBC) 细胞系的细胞活力，处理时长为 48 h[1]。
YZ-836P (0-10 µM; 48 h) 和 (4 µM; 0-72 h) 可呈剂量依赖性和时间依赖性降低 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系中的 PRMT5 和 KLF5 蛋白水平[1]。
YZ-836P (0.25-1.00 µM; 2 days) 以浓度依赖的方式抑制 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系的集落形成，该作用在初始处理 2 天后显现[1]。
YZ-836P (1-6 µM; 24 h) 可浓度依赖性地抑制 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系中的 DNA 合成[1]。
YZ-836P (2-6 µM; 48 h) 可浓度依赖性地诱导 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系发生 G1 期细胞周期阻滞[1]。
YZ-836P (2-6 µM; 48 h) 可浓度依赖性地调控 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系中细胞周期相关蛋白的表达 (下调 Cyclin D1、CDK4、CDK6；上调 p21、p27)，处理时长为 48 h[1]。
YZ-836P (2-6 µM; 48 h) 可浓度依赖性地调控 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系中凋亡相关蛋白的表达 (上调剪切型 PARP、剪切型 Caspase 3；下调 XIAP、Mcl-1)，处理时长为 48 h[1]。
YZ-836P (2-6 µM; 48 h) 可浓度依赖性地诱导 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系发生细胞凋亡[1]。
YZ-836P (4 µM) 可直接结合 PRMT5，在 HCC1806 和 HCC1937 三阴性乳腺癌 (TNBC) 细胞系中提高其热稳定性 (CETSA assay) 并降低其对蛋白酶降解的敏感性 (DARTS assay)[1]。
YZ-836P (4 µM; 48 h) 可在 HEK293T 细胞中增强 PRMT5 的泛素化水平，并促进依赖 CRBN 的蛋白酶体介导的 PRMT5 降解[1]。
YZ-836P (0-10 µM; 48 h) 可强效降低三阴性乳腺癌 (TNBC) 患者来源类器官 PDO-32 (IC50 = 2.072 µM) 和 PDO-33 (IC50 = 4.746 µM) 的存活率，处理时长为 48 h[1]。

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

YZ-836P 相关抗体:

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.
体内研究
(In Vivo)

YZ-836P (50 mg/kg；腹腔注射；每 2 天 1 次；共给药 4 次) 对 TNBC 异种移植物具有强效的体内抗肿瘤活性，可抑制肿瘤生长且不会引发可检测到的全身毒性[1]。

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.
分子量

835.99

Formula

C45H57N9O7
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

YZ-836P 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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