1. Epigenetics
  2. Histone Methyltransferase DNA Methyltransferase
  3. CM-579

CM-579 是首创的、可逆的,G9a 和DNA 甲基转移酶 (DNMT) 的双抑制剂,其IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。

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 CM-579 trihydrochloride 通常具有更好的水溶性和稳定性。

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CM-579 Chemical Structure

CM-579 Chemical Structure

CAS No. : 1846570-40-8

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CM-579 的其他形式现货产品:

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Other Forms of CM-579:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells[1].

IC50 & Target[1]

DNA Methyltransferase

32 nM (IC50)

DNMT1

1.5 nM (Kd)

DNMT3A

92 nM (IC50)

DNMT3B

1000 nM (IC50)

G9a

16 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MM1.S GI50
3842 nM
Compound: 6; CM-579
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay
[PMID: 33661013]
OCI-Ly10 GI50
< 31 nM
Compound: 12
Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay
Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay
[PMID: 29890830]
OCI-Ly3 GI50
202 nM
Compound: 12
Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay
Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay
[PMID: 29890830]
体外研究
(In Vitro)

The Kd of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC50s of 92 nM and 1000 nM, respectively[1].

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

分子量

492.65

Formula

C29H40N4O3

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
  • 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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CM-579
目录号:
HY-117421
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