2. PROTAC Epigenetics GPCR/G Protein
  3. PROTACs Histone Methyltransferase GLP Receptor
  4. PROTAC G9a/GLP degrader 1

PROTAC G9a/GLP degrader 1 是一种 G9a/GLP PROTAC 降解剂，其 DC50 分别为 336 nM (G9a) 和 988 nM (GLP)。PROTAC G9a/GLP degrader 1 对 G9a 表现出抑制活性，其 IC50 为 98 nM。PROTAC G9a/GLP degrader 1 可有效抑制乳腺癌 MCF-7 细胞的迁移，且不抑制细胞增殖。PROTAC G9a/GLP degrader 1 可用于乳腺癌的研究 (粉色：G9a/GLP 配体 (HY-152775)；蓝色：VHL 配体 (HY-125845)；黑色：连接子 (HY-140468))。

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PROTAC G9a/GLP degrader 1

PROTAC G9a/GLP degrader 1 Chemical Structure

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PROTAC G9a/GLP degrader 1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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 ASH1L/KMT2H 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

PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468))[1].

IC50 & Target[1]

G9a

336 nM (DC50)

GLP

988 nM (DC50)

VHL

 

体外研究
(In Vitro)

PROTAC G9a/GLP degrader 1 (Compound 4) (0.03-10 μM, 0-72 h) 表现出强效且持久的 G9a/GLP 降解能力，并有效降低乳腺癌 MCF-7 细胞中 G9a 催化产物 H3K9me2 的水平[1]。
PROTAC G9a/GLP degrader 1 (0.1-10 μM, 24-72 h) 显著抑制 MCF-7 细胞的迁移能力，但对 MCF-7 细胞的活力无显著影响[1]。

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

PROTAC G9a/GLP degrader 1 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 0, 3, 6, 12, 24, 48 and 72 h
Result: Initiated the degradation of G9a/GLP within 6 hours and persisted for at least 72 hour.
Effectively reduced the level of the catalytic product H3K9me2 of G9a.

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 72 h
Result: Did not reduce the MCF-7 cell viability.

Cell Migration Assay [1]

Cell Line: MCF-7 cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Suppressed the migration of MCF-7 cells.
分子量

1081.33

Formula

C57H76N8O11S
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

PROTAC G9a/GLP degrader 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.

Keywords:

PROTAC G9a/GLP degrader 1PROTACsHistone MethyltransferaseGLP ReceptorPROTACRK-701H3K9me2MCF-7Chemical ProbeInhibitorinhibitorinhibit

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PROTAC G9a/GLP degrader 1
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HY-178065
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