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Submit ReviewBMS 509744 is a potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitor (IC50 = 19 nM). Displays 200-fold selectivity over Tec family kinases and 55-fold selectivity over other kinases tested. Reduces HIV infection of primary CD4+ T cells and attenuates the establishment of HIV infection in vitro. Reduces T cell proliferation and IL-2 production in vitro. Reduces lung inflammation in a mouse model of ovalbumin-induced allergy/asthma.
BMS 509744 is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 623.83 |
公式 | C32H41N5O4S2 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 439575-02-7 |
PubChem ID | 11467730 |
InChI Key | ZHXNIYGJAOPMSO-UHFFFAOYSA-N |
Smiles | COC1=CC(C)=C(SC3=CN=C(NC(C4=CC=C(CNC(C)C(C)(C)C)C=C4)=O)S3)C=C1C(N2CCN(C(C)=O)CC2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Kutach et al (2010) Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation. Chem Biol Drug Des. 76 154 PMID: 20545945
Das et al (2006) Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. Bioorg.Med.Chem.Lett. 16 3706 PMID: 16682193
Readinger et al (2008) Selective targeting of ITK blocks multiple steps of HIV replication. Proc.Natl.Acad.Sci.U.S.A. 105 6684 PMID: 18443296
关键词: BMS 509744, BMS 509744 supplier, BMS509744, lung, inflammation, allergy, asthma, inducible, T, cell, kinase, emt, tsk, HIV, potent, selective, ITK, inhibitors, inhibits, Il2, 5009, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BMS 509744 的部分引用包括:
Mamand et al (2018) Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma. Sci Rep 8 14216 PMID: 30242208
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