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

PRMT5 IN-1 是一種半縮醛胺，是一種有效的選擇性蛋白精氨酸甲基轉(zhuǎn)移酶5 (PRMT5) 抑制劑，抑制 PRMT5/MEP50 的 IC50 值為 11 nM。PRMT5 IN-1 在生理條件下可以轉(zhuǎn)化為醛并與 C449 反應形成共價加合物。

在相同的摩爾濃度下，化合物鹽形式與游離形式有相同的生物活性，但鹽形式 PRMT5-IN-1 hydrochloride 通常具有更好的水溶性和穩(wěn)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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PRMT5-IN-1 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of PRMT5-IN-1:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
Granta-519 IC50
0.012 μM
Compound: 9
Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
[PMID: 31312404]
Granta-519 IC50
0.06 μM
Compound: 9
Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
[PMID: 31312404]
體外研究
(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 號
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
純度 & 產(chǎn)品資料
參考文獻

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  • 稀釋計算器

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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.

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產(chǎn)品名稱：
PRMT5-IN-1
目錄號：
HY-126256
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