1. Epigenetics
  2. Histone Methyltransferase
  3. PRMT5-IN-1

PRMT5 IN-1 是一种半缩醛胺,是一种有效的选择性蛋白精氨酸甲基转移酶5 (PRMT5) 抑制剂,抑制 PRMT5/MEP50 的 IC50 值为 11 nM。PRMT5 IN-1 在生理条件下可以转化为醛并与 C449 反应形成共价加合物。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 PRMT5-IN-1 hydrochloride 通常具有更好的水溶性和稳定性。

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PRMT5-IN-1 Chemical Structure

PRMT5-IN-1 Chemical Structure

CAS No. : 2366149-83-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions[1].

IC50 & Target[1]

PRMT5

 

体外研究
(In Vitro)

PRMT5 IN-1 (0-500 nM) inhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×105 M-1 min-1] very rapidly with a Kinact of 0.068 min-1 and a good binding affinity (KI=55 nM)[1].
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) inhibits the expression of cellular sDMA with an IC50 value of 0.012 μM[1].
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) inhibits cell proliferation in a dose-dependent manner with an IC50 value of 0.06 μM[1].

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

Cell Viability Assay[1]

Cell Line: Granta-519 cells
Concentration: 0, 0.0001524, 0.000457, 0.001372, 0.004115, 0.012346, 0.037037, 0.111111, 0.333333 and 1 μM
Incubation Time: 10 days
Result: Inhibited cell proliferative, in which cells died on day 10 at high concentrations (0.3 and 1 μM).

Western Blot Analysis[1]

Cell Line: Granta-519 cells
Concentration: 0, 0.05, 0.15, 0.46, 1.37, 4, 12, 37, 111, 333, 1000 nM
Incubation Time: 3 days
Result: Inhibited cellular sDMA in Granta-519 cells in a dose-dependent manner.
分子量

418.83

Formula

C19H19ClN4O5

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-IN-1 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)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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PRMT5-IN-1
目录号:
HY-126256
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