2. Epigenetics PROTAC
  3. Epigenetic Reader Domain PROTACs
  4. GXF-111

GXF-111 是一种 PROTAC 分子，可以促进细胞 BRD3 和 BRD4-L 的选择性降解。GXF-111 对 BRD3 BD1 和 BRD3 BD2 具有结合亲和力，Ki 值分别为 11.97 nM 和 2.35 nM。GXF-111可用于癌症的研究。

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GXF-111 Chemical Structure

GXF-111 Chemical Structure

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GXF-111 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer[1].

IC50 & Target

Ki: 11.97 nM (BRD3 BD1); 2.35 nM (BRD3 BD2) [1].
IC50: 6.31 nM (MV4-11 cell); 95.2 nM (MM.1 S cell) [1].
体外研究
(In Vitro)

GXF-111 (Compound 24) 对 BRD3 BD1 和 BRD3 BD2 具有结合亲和力，Ki 值分别为 11.97 nM 和 2.35 nM[1]。
GXF-111 在 MV4-11 和 MM.1 S 细胞系中具有细胞活性，IC50 值分别为 6.31 nM 和 95.2 nM[1]。
GXF-111 (2, 10 nM; 24 h) 对 MM.1 S 细胞中 BET 家族蛋白的降解具有有效的细胞生长抑制活性[1]。
GXF-111 (4 days) 在 7 种人类癌细胞系中具有抗增殖活性，IC50 值范围为 6.31 nM 至 17.25 μM[1]。

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

GXF-111 相关抗体:

Western Blot Analysis[1]

Cell Line: MM.1 S cells；MM.1 S, HGC-27, and MCF-7 cells；Multiple cancer cell lines
Concentration: 2, 10 nM; 0.1, 0.3, 1, 3 nM; 30 nM; 3, 10, 30, 100, 300 nM
Incubation Time: 24 h; 8 h; 1, 3, 6, 8, 24 h; 24 h
Result: Efficiently depleted BRD3 and BRD4-L in MM.1 S cells at 2 nM.
Dose-dependently depleted BRD3 and BRD4-L and partially depleted BRD2 at 10 nM.
Had good degradation kinetics of BET proteins in three selected cancer cell lines, i.e. MM.1S, MCF-7, and HGC-27 cells.
Only BRD3 and BRD4-L, were depleted dose-dependently in five cancer cell lines, i.e. HGC27, MCF-7, A549, Hela, and HepG2 cells.

Cell Cycle Analysis[1]

Cell Line: MM.1 S cell
Concentration: 1, 3, 10, 30, 100, 300 nM
Incubation Time: 24 h
Result: Dose-dependently induced cell cycle arrest at G1 phase.
分子量

728.28

Formula

C42H42ClN7O3
非同位 CAS

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

GXF-111 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 *
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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:

GXF-111GXF111GXF 111Epigenetic Reader DomainPROTACsPROTACBRD3BRD4-Lcanceranti-tumorInhibitorinhibitorinhibit

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