1. Epigenetics
  2. Histone Demethylase
  3. GSK 690

GSK 690 是赖氨酸特异性去甲基化酶1 (LSD 1) 的可逆抑制剂,其Kd 值为 9 nM,IC50 值为 37 nM。

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 GSK 690 Hydrochloride 通常具有更好的水溶性和稳定性。

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GSK 690 Chemical Structure

GSK 690 Chemical Structure

CAS No. : 2101305-84-2

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GSK 690 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

查看 Histone Demethylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
RD IC50
10.2 μM
Compound: 46; GSK-690
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs
[PMID: 35525212]
RD IC50
11.43 μM
Compound: 46; GSK-690
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs
[PMID: 35525212]
RD IC50
12.35 μM
Compound: 46; GSK-690
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs
[PMID: 35525212]
SJRH30 IC50
10.3 μM
Compound: 46; GSK-690
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs
[PMID: 35525212]
SJRH30 IC50
10.7 μM
Compound: 46; GSK-690
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs
[PMID: 35525212]
SJRH30 IC50
9.93 μM
Compound: 46; GSK-690
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs
[PMID: 35525212]
THP-1 IC50
1.4 μM
Compound: 25, GSK354
Inhibition of LSD1 in human THP1 cells assessed as CD86 level after 24 hrs by ELISA
Inhibition of LSD1 in human THP1 cells assessed as CD86 level after 24 hrs by ELISA
10.1039/C3MD00226H
体外研究
(In Vitro)

GSK690 (1-10μM) acts together with JNJ-26481585 to induce cell death in all four tested RMS cells lines (RD, RH30, RMS13, and TE381.T cells)[2].
GSK690/JNJ-26481585 cotreatment alters the balance between pro- and antiapoptotic proteins with 1 μM GSK690 for RD cells) and 10 μM GSK690 for RH30 cells[2].
GSK690/JNJ-26481585 cotreatment induces caspase-dependent cell death with 1 μM GSK690 for RD cells and 10 μM GSK690 for RH30 cells[2].
The addition of GSK690 further enhances the JNJ-26481585-stimulated G2/M arrest [2].

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

分子量

369.46

Formula

C24H23N3O

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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产品名称:
GSK 690
目录号:
HY-117226
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