2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. PRMT1-IN-3

PRMT1-IN-3 是一种强效的蛋白精氨酸甲基转移酶 1 (PRMT1) 抑制剂，其 IC50 为 4.11 μM。PRMT1-IN-3 能够抑制 PRMT6 和 PRMT8，其 IC50 值分别为 23.3 和 30.1 μM。PRMT1-IN-3 可抑制三阴性乳腺癌 (TNBC) 细胞中的不对称二甲基精氨酸 (ADMA) 水平和组蛋白 H4R3me2a 修饰。PRMT1-IN-3 可诱导 MDA-MB-231 细胞周期停滞、凋亡 (apoptosis)，并抑制细胞的迁移和集落形成。PRMT1-IN-3 可作为 Paclitaxel (HY-B0015) 的化疗增敏剂。PRMT1-IN-3 可用于 TNBC 的研究。

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PRMT1-IN-3

PRMT1-IN-3 Chemical Structure

CAS No. : 892570-48-8

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PRMT1-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC[1].

IC50 & Target[1]

PRMT1

4.11 μM (IC50)

PRMT3

> 100 μM (IC50)

PRMT4

> 100 μM (IC50)

PRMT6

23.3 μM (IC50)

PRMT5

> 100 μM (IC50)

PRMT8

30.1 μM (IC50)

PRMT7

> 100 μM (IC50)

体外研究
(In Vitro)

PRMT1-IN-3 (Compound YH-4) (10 μM，37-65°C) 显著增强 PRMT1 的热稳定性 (ΔTm = +5.2°C) ，对其他 PRMT 亚型无显著影响[1]。
PRMT1-IN-3 (0.01-100 μM，48 小时) 抑制 MDA-MB-231、HCT116、HeLa 和 A549 细胞生长，IC50 分别为 6.38 μM、15.29 μM、12.97 μM 和 9.187 μM[1]。
PRMT1-IN-3 (1.25-10 μM，48小时) 以剂量依赖性方式抑制 MDA-MB-231 细胞中的 ADMA 水平和 H4R3me2a 修饰[1]。
PRMT1-IN-3 (0-20 μM, 72 小时) (耐药指数：9.0) 在 MDA-MB-231 细胞和 MDA-MB-231/Taxol 细胞中与 Paclitaxel (PTX) (耐药指数：92.7) 表现出协同作用[1]。
PRMT1-IN-3 (0-40 μM, 0-48 小时) 诱导 G0/G1 期停滞和细胞凋亡，并抑制 MDA-MB-231 细胞的细胞迁移[1]。
PRMT1-IN-3 (0-20 μM, 10 天) 在 20 μM 浓度下几乎完全抑制 MDA-MB-231 细胞的集落形成[1]。

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

PRMT1-IN-3 相关抗体:

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 5, 20 and 40 μM
Incubation Time: 48 h
Result: Resulted in an increase in early apoptosis from 2.34 % to 34.3 % from 2.5 μM to 40 μM.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Observed that the proportion of cells in the G0/G1 phase increased in a dose-dependent manner from 41.8 % to 60.9 %, while the proportions of cells in the S phase and G2/M phase decreased in a dose-dependent manner from 33.2 % to 23.6 % and from 24.9 % to 15.2 %, respectively.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 0, 12, 36, and 48 h
Result: Decreased the healing rate to 18.52% after 48 h at 20 μM.
体内研究
(In Vivo)

PRMT1-IN-3 (Compound YH-4) (30 mg/kg，腹腔注射，持续一周，然后停药三天，共 21 天) 是 PTX 的化疗增敏剂，可增强其治疗效果，同时显著减少所需剂量并减轻其在 TNBC 小鼠模型中的毒副作用[1]。

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

Animal Model: MDA-MB-23-YFP-Luc cells induced xenograft model established in female nude mice 4-5 weeks old weighing 16-18 g[1]
Dosage: 30 mg/kg with or without PTX
Administration: Intraperitoneal injection (i.p.), for one week, then discontinue for three days, for a total of 21 days
Result: Demonstrated significant inhibitory effects on tumor volume, with the combination of PTX showing a markedly superior antitumor efficacy compared to the monotherapies.
分子量

302.39

Formula

C18H23FN2O
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

PRMT1-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

PRMT1-IN-3892570-48-8Histone MethyltransferaseApoptosisPRMT1 inhibitorTriple-negative breast cancerVirtual screeningChemotherapeutic sensitizersInhibitorinhibitorinhibit

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