2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. PRMT5-MTA-IN-8

PRMT5-MTA-IN-8 是一种具有口服活性的 PRMT5-MTA 复合物抑制剂 (IC50 = 4.4 nM)。PRMT5-MTA-IN-8 可抑制细胞内对称性二甲基精氨酸 (SDMA) 的生成以及 MTAP 缺失型细胞的增殖。PRMT5-MTA-IN-8 在三阴性乳腺癌小鼠模型中通过抑制 PRMT5、降低 SDMA 水平并诱导肿瘤细胞凋亡 (Apoptosis) 表现出抗肿瘤功效。PRMT5-MTA-IN-8 可用于三阴性乳腺癌等癌症的相关研究。

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PRMT5-MTA-IN-8

PRMT5-MTA-IN-8 Chemical Structure

CAS No. : 3105952-57-3

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PRMT5-MTA-IN-8 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

PRMT5-MTA-IN-8 is an orally active PRMT5-MTA complex inhibitor (IC50 = 4.4 nM). PRMT5-MTA-IN-8 inhibits the intracellular production of symmetric dimethylarginine (SDMA) as well as the proliferation of MTAP-deficient cells. PRMT5-MTA-IN-8 exerts antitumor efficacy by inhibiting PRMT5, reducing SDMA levels and inducing tumor cell apoptosis in mouse models of triple-negative breast cancer. PRMT5-MTA-IN-8 can be used in research related to cancers such as triple-negative breast cancer[1].

IC50 & Target

PRMT5

 

体外研究
(In Vitro)

PRMT5-MTA-IN-8 (Compound I-14) 可抑制 HCT116 MTAP-null 细胞中 PRMT5 依赖的 SDMA 形成 (IC50 = 0.8 nM)，以及抑制 HCT116 MTAP-null 细胞的增殖 (IC50 = 3.9 nM)[1]。
PRMT5-MTA-IN-8 (0.1-1000 nM, 6 days) 可抑制 MDA-MB-231 细胞中 PRMT5 依赖的 SDMA 生成，其 IC50 为 0.25 nM，提高 PRMT5 的热稳定性[1]。
PRMT5-MTA-IN-8 在大鼠肝微粒体和血浆中表现出高代谢稳定性，半衰期分别为 131 和 136 min[1]。

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

PRMT5-MTA-IN-8 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.01, 0.1, 1.0, 10, 100, and 1000 nM
Incubation Time: 6 days
Result: Decreased global SDMA.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.01, 0.1, 1.0, 10, 100, and 1000 nM
Incubation Time: 6 days
Result: Improved the thermal stability of PRMT5 to 64°C and inhibited its degradation at 61°C.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax Vz Cmax C0 Bioavailability
Rat[1] 2 mg/kg i.v. 448.373 μg/L·h 449.564 μg/L·h 0.879 h 0.923 h 2.02 h 0.125 h 13.523 L/kg 593.75 μg/L 803.704 μg/L /
Rat[1] 20 mg/kg p.o. 1460.7 μg/L·h 1479.9 μg/L·h 3.241 h 3.408 h 1.827 h 1.375 h 44.385 L/kg 347.75 μg/L / 35.2 %
体内研究
(In Vivo)

PRMT5-MTA-IN-8 (I-14) (25-100 mg/kg; p.o.; daily; 28 days) 在 MDA-MB-231 TNBC 异种移植物模型中通过靶向抑制 PRMT5、降低 SDMA 水平并诱导肿瘤细胞凋亡展现抗肿瘤功效[1]。

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

Animal Model: NSG mouse (female, 4-6 weeks old, subcutaneous injection of 5×106 MDA-MB-231 cells)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 28 days
Result: Achieved a tumor growth inhibition and reduced tumor volume.\n
Induced dose-dependent reduction in tumor tissue SDMA protein expression.
Increased cleaved-caspase 3 and cPARP protein expression in tumor tissue.\n
Reduced tumor tissue PARP1 protein expression.\n
Maintained normal mouse physical activity.
分子量

441.28

Formula

C19H17BrN6O2
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

PRMT5-MTA-IN-8 相关分类

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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:

PRMT5-MTA-IN-83105952-57-3Histone MethyltransferaseApoptosisPRMT5-MTA complex Inhibitortriple-negative breast cancerNSG mouseHCT116 MTAP-null cells
Inhibitorinhibitorinhibit

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