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PFI-1,≥98% (HPLC)

别名:2-甲氧基-N-(3-甲基-2-氧代-1,2,3,4-四氢喹唑啉-6-基)苯磺酰胺;2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydro-quinazolin-6-yl)-bezenesulfonamide, PF-06405761

Empirical Formula (Hill Notation): C16H17N3O4S CAS号: 1403764-72-6 分子量: 347.39 MDL编号: MFCD22580416 PubChem化学物质编号: 329825355 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML0352
CAS号: 1403764-72-6
MDL号: MFCD22580416
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$245.16

说明

PFI-1 已被用作乳腺癌细胞系 MCF7 去绒毛膜斑马鱼胚胎中的溴结构域抑制剂。 它还被用于人外周血单核细胞 (PBMC),以抑制脂多糖 (LPS) 激发试验中白细胞介素 6 的释放。
PFI-1 是一种喹唑啉酮,可抑制前列腺癌细胞中的雄激素受体 (AR) 介导的信号传导。 它引起最小的毒性,对抗 HIV 潜伏治疗有效。 在白血病细胞中,PFI-1 抑制 Aurora B 激酶并促进半胱天冬酶依赖性细胞凋亡。
人类 BET 家族,包括 BRD2、BRD3、BRD4 和 BRDT,在基因转录的调控中发挥作用。 PFI-1 是一种选择性 BET 溴结构域抑制剂,对 BRD2 (IC50 = 98 nM) 和 BRD4 (IC50 = 220 nM) 具有活性。

应用

PFI-1 has been used as a bromodomain inhibitor in breast cancer cell line MCF7 dechorionated zebrafish embryos. It has also been used in human peripheral blood mononuclear cells (PBMCs), to inhibit the release of interleukin-6 in lipopolysaccharide (LPS) challenge assay.
 

包装

5, 25 mg in glass bottle
 

生化/生理作用

PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells. It elicits minimum toxicity and is effective for anti-HIV-latency therapy. In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.
The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). For full characterization details, please visit the PFI-1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 

特点和优势

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
PFI-1 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
 

其他说明

PFI-1 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PFI-1 probe summary on the Chemical Probes Portal website.
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: ≥10 mg/mL

储存温度

2-8°C

SMILES string

COc1ccccc1S(=O)(=O)Nc2ccc3NC(=O)N(C)Cc3c2

InChI

1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)

InChI key

TXZPMHLMPKIUGK-UHFFFAOYSA-N

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16