GSK 4027|2079896-25-4|-陌孚医药/Medlife

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GSK 4027

目录号: PL13509 纯度: ≥98%

CAS No. :2079896-25-4

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中文名称	GSK 4027
中文别名	4-溴-2-甲基-5-[[(3R,5R)-1-甲基-5-苯基-3-哌啶基]氨基]-3(2H)-哒嗪酮
英文名称	GSK 4027
英文别名	4-Bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)-amino)pyridazin-3(2H)-one;4-Bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-3(2H)-pyridazinone;GSK 4027;GSK4027;4-Bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one;4-bromo-2-methyl-5-[[(3~{R},5~{R})-1-methyl-5-phenyl-piperidin-3-yl]amino]pyridazin-3-one;BDBM50234923;J3.613.274D;9ST
Cas No.	2079896-25-4
分子式	C₁₇H₂₁BrN₄O
分子量	377.28
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GSK 4027 是一种 PCAF/GCN5 溴结构域的化学探针，作用于 PCAF，pIC₅₀ 为 7.4±0.11。
生物活性	GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC 50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
性状	Solid
IC50 & Target[1][2]	pIC50: 7.4±0.11 (PCAF)
体外研究(In Vitro)	GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel with pKi of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with Ki of 1.4 nM for both bromodomains. As expected due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full length PCAF from histone H3.3 with little drop-
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
参考文献	[1]. Humphreys PG, et al. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. J Med Chem. 2017 Jan 26;60(2):695-709.

溶解度数据	In Vitro: DMSO : 50 mg/mL (132.53 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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