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GSK046
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK046图片
CAS NO:2474876-09-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
iBET-BD2
产品介绍
GSK046 (iBET-BD2) 是一种有效,选择性和具有口服活性的BET蛋白BD2溴结构域的抑制剂,IC50值为 264 nM (BRD2 BD2),98 nM (BRD3 BD2),49 nM (BRD4 BD2) 和 214 nM (BRDT BD2)。GSK046 具有免疫调节活性。
生物活性

GSK046 (iBET-BD2) is a potent, selective and orally activeBD2bromodomaininhibitor of theBETproteins, withIC50s of 264 nM (BRD2BD2), 98 nM (BRD3BD2), 49 nM (BRD4BD2) and 214 nM (BRDTBD2), respectively. GSK046 has immunomodulatory activity[1].

IC50& Target[1]

BRD2 BD2

264 nM (IC50)

BRD3 BD2

98 nM (IC50)

BRD4 BD2

49 nM (IC50)

BRDT BD2

214 nM (IC50)

体外研究
(In Vitro)

GSK046 (1000 nM; refresh every three days) reduces the recruitment of BET proteins to interferon (IFN) target genes following IFN-γ stimulation. GSK046 appears to more prominently affect the recruitment of BRD2 and BRD3 compared to BRD4[1].
GSK046 (0.1-10 μM) displays a more selective phenotypic fingerprint, particularly inhibiting the production of key pro-inflammatory mediators including Th17 cytokines in the B and T cell co-culture system[1].
GSK046 (0.01-10 μM; 72 hours) does not affect the proliferative activity of human primary CD4+T cells but still inhibits the production of effector cytokines including IFNγ, IL-17A and IL-22[1].
GSK046 (0.005-10 μM; 48 hours) impairs macrophage activation following PMA stimulation, without impacting cellular viability[1].

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:Did not affect the proliferative activity of the cells but still inhibited the production of effector cytokines.
体内研究
(In Vivo)

GSK046 (40 mg/kg/QD; s.c. for 14 days) has immunomodulatory activity[1].
GSK046 exhibits Cmax(C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg)[1].
GSK046 exhibits Cmax(mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1].

Animal Model:Male C57BL/6 mice (8/10-weeks-old) are injected with keyhole limpet hemocyanin (KLH)[1]
Dosage:40 mg/kg/QD
Administration:S.c. injections for 14 days
Result:Reduced the production of anti-keyhole limpet hemocyanin (KLH) IgM and was well tolerated.
Animal Model:Female C57BL/6 mice[1]
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Cmax(1859 ng/mL), T1/2(1.8 h).
Animal Model:Male C57BL/6 mice[1]
Dosage:40 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Cmax(2993 ng/mL), T1/2(1.9 h).
Animal Model:Female Lewis rat[1]
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Cmax(202 ng/mL), T1/2(1.4 h).
分子量

414.47

性状

Solid

Formula

C23H27FN2O4

CAS 号

2474876-09-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL(201.05 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4127 mL12.0636 mL24.1272 mL
5 mM0.4825 mL2.4127 mL4.8254 mL
10 mM0.2413 mL1.2064 mL2.4127 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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 (5.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.02 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-CDin saline)

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.02 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 900 μL20% 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 (5.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.02 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本网站选购。