2. Epigenetics
  3. Histone Methyltransferase
  4. PRMT5-IN-30

PRMT5-IN-30 (compound 17) 是一种有效的选择性蛋白精氨酸甲基转移酶 5 (PRMT5) 抑制剂，IC50 为 0.33 μM，Kd 为 0.987 μM。PRMT5-IN-30 对一组其他甲基转移酶表现出广泛的选择性。PRMT5-IN-30 抑制 PRMT5 介导的 SmD3 甲基化。

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PRMT5-IN-30 Chemical Structure

PRMT5-IN-30 Chemical Structure

CAS No. : 330951-01-4

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PRMT5-IN-30 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 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-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation[1].

IC50 & Target[1]

PRMT5

0.33 μM (IC50)

PRMT5

0.987 μM (Kd)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 100 μM
Compound: 17
Inhibition of recombinant human N-terminal FLAG-tagged PRMT4 (2 to end residues) expressed in HEK293F cells using of histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA
Inhibition of recombinant human N-terminal FLAG-tagged PRMT4 (2 to end residues) expressed in HEK293F cells using of histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA
[PMID: 28650658]
HEK293 IC50
0.33 μM
Compound: 17
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl meth
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl meth
[PMID: 28650658]
JeKo-1 EC50
15 μM
Compound: 17
Cytotoxicity against human JeKo1 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
Cytotoxicity against human JeKo1 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
[PMID: 28650658]
KOPN-8 EC50
15 μM
Compound: 17
Cytotoxicity against human KOPN8 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
Cytotoxicity against human KOPN8 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
[PMID: 28650658]
MV4-11 EC50
25.73 μM
Compound: 17
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
[PMID: 28650658]
MV4-11 EC50
6.53 μM
Compound: 17
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
[PMID: 28650658]
MV4-11 EC50
80.74 μM
Compound: 17
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 4 days by Cell Titer-Glo assay
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 4 days by Cell Titer-Glo assay
[PMID: 28650658]
Z-138 EC50
15 μM
Compound: 17
Cytotoxicity against human Z138 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
Cytotoxicity against human Z138 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
[PMID: 28650658]
分子量

371.41

Formula

C18H17N3O4S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 99.17%

COA (286 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

PRMT5-IN-30 相关分类

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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)
× = ×
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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-30330951-01-4Histone MethyltransferasePRMT5 inhibitorSmD3 methylationantitumor activityInhibitorinhibitorinhibit

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