2. Epigenetics
  3. Histone Methyltransferase
  4. PRMT5-IN-53

PRMT5-IN-53 是一种口服有效的肠道限制性 PRMT5 抑制剂，其针对 hPRMT5 和 mPRMT5 的 pIC50 值 ≥ 9.7。PRMT5-IN-53 与 PRMT5:MEP50 复合物结合的 KD 值为 11.3 pM。PRMT5-IN-53 可有效抑制小鼠肠道内的 PRMT5，显著减少息肉的数量和面积，同时避免全身血液学毒性 (如贫血、中性粒细胞减少)。PRMT5-IN-53 可用于结直肠癌的研究，尤其是家族性腺瘤性息肉病 (FAP) 的研究。

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PRMT5-IN-53

PRMT5-IN-53 Chemical Structure

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PRMT5-IN-53 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-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP)[1].

IC50 & Target[1]

PRMT5

≥ 9.7 (pIC50)

体外研究
(In Vitro)

PRMT5-IN-53 (Compound 9) 可抑制 A549 细胞中的整体 SDMA 甲基化，pIC50 值为 9.4 μM[1]。

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

PRMT5-IN-53 相关抗体:
体内研究
(In Vivo)

PRMT5-IN-53 (Compound 9) (25-75 mg/kg，每日两次，连续 7-21 天) 表现出显著的结肠药理效应，并在 DSS (HY-116282C) 诱导的 ApcMin/+ 小鼠息肉模型中显示出疗效[1]。

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

Animal Model: DSS-induced polyp-bearing model established in Female ApcMin/+ (C57BL/6J-ApcMin/J, aged 4−5 weeks)[1]
Dosage: 25 and 75 mg/kg
Administration: Intragastric administration (i.g.), twice daily for 14-21 days
Result: Significantly reduced SDMA and SmD3-Me2 during 2 weeks in the colon tissue, bone marrow and spleen showed no changes in SDMA signals during 1 week.
Reduced the number and size of polyps during 3 weeks.
Did not cause systemic targeted toxicity.
分子量

390.44

Formula

C21H22N6O2
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-IN-53 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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-IN-53Histone MethyltransferaseColorectal Cancer (CRC)Adenomatous Polyposis Coli (APC)Familial Adenomatous PolyposisSymmetrical DimethylargininePharmacokinetics (PK)Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-178028
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