GSK778(Synonyms: iBET-BD1)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GSK778 (Synonyms: iBET-BD1) 纯度: 99.25%

GSK778 (iBET-BD1) 是一种有效和选择性的 BET 蛋白 BD1 溴结构域的抑制剂，IC50 值为 75 nM (BRD2 BD1)，41 nM (BRD3 BD1)，41 nM (BRD4 BD1) 和143 nM (BRDT BD1)。GSK778 表型化了 pan-BET 抑制剂在癌症模型中的作用。

GSK778(Synonyms: iBET-BD1)

GSK778 Chemical Structure

CAS No. : 2451862-42-1

规格 价格 是否有货 数量
5 mg ￥7000 In-stock
10 mg ￥12000 In-stock
25 mg ￥25000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

GSK778 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1].

IC50 & Target[1]

BRD2 BD1

75 nM (IC50)

BRD3 BD1

41 nM (IC50)

BRD4 BD1

41 nM (IC50)

BRDT BD1

143 nM (IC50)

体外研究
(In Vitro)

GSK778 inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively[1].
GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22[1].
GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells[1].
GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells[1].
GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Human primary CD4+ T cell
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited the proliferative activity of the cells and the production of effector cytokines.

Cell Viability Assay[1]

Cell Line: MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 5 days
Result: Inhibited the growth and viability of human cancer cell lines.

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM13, MDA-MB-231 and MB453 cells
Concentration: 1000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation and induced a cell cycle arrest and apoptosis.

体内研究
(In Vivo)

GSK778 (15 mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model[1].
GSK778 (15 mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated[1].
GSK778 exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10 mg/kg) in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells[1]
Dosage: 15 mg/kg/BID
Administration: I.p. injections for 30 days
Result: Increased the survival rate of leukemia mice.
Animal Model: Male CD1 mice[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: P.o. administration
Result: Cmax (85 ng/mL), Tmax (1.48 h); AUC∞ (132 ng.h/mL).

分子量

511.61

Formula

C30H33N5O3
CAS 号

2451862-42-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL (81.45 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9546 mL 9.7731 mL 19.5461 mL
5 mM 0.3909 mL 1.9546 mL 3.9092 mL
10 mM 0.1955 mL 0.9773 mL 1.9546 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.07 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.07 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.07 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.07 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务