GSK046 - CAS:2474876-09-8

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GSK046 (Synonyms:iBET-BD2)

目录号 : KM5160 CAS No. : 2474876-09-8 纯度 : 98%

Data Sheet 产品使用指南

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。

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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC₅₀s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.

体外研究

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.
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.
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.
GSK046 (0.005-10 μM; 48 hours) impairs macrophage activation following PMA stimulation, without impacting cellular viability.

Cell Proliferation Assay

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

GSK046 (40 mg/kg/QD; s.c. for 14 days) has immunomodulatory activity.
GSK046 exhibits C_max (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).
GSK046 exhibits C_max (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).

Animal Model:	Male C57BL/6 mice (8/10-weeks-old) are injected with keyhole limpet hemocyanin (KLH)
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
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral administration
Result:	C_max (1859 ng/mL), T_1/2 (1.8 h).

Animal Model:	Male C57BL/6 mice
Dosage:	40 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral administration
Result:	C_max (2993 ng/mL), T_1/2 (1.9 h).

Animal Model:	Female Lewis rat
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral administration
Result:	C_max (202 ng/mL), T_1/2 (1.4 h).

分子式

C₂₃H₂₇FN₂O₄

分子量

414.47

CAS号

2474876-09-8

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4127 mL	12.0636 mL	24.1272 mL
5 mM	0.4825 mL	2.4127 mL	4.8254 mL
10 mM	0.2413 mL	1.2064 mL	2.4127 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°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 (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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
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。