化合物PCI29732 T4337

Product Introduction
Bioactivity


英文名: PCI 29732

描述: PCI 29732 是一种有效的可逆BTK 抑制剂，对 BTK、Lck 和 Lyn 的Kiapp 值分别为 8.2、4.6 和 2.5 nM。它通过竞争性结合ABCG2 的 ATP 结合位点来抑制ABCG2的功能。

体外活性: PCI 29732(compound 1) has a 8.2 nM potency against Btk in a FRET based biochemical enzymology assay. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase, probably due to the difference at the 'gatekeeper” residue. In human CD20+ B cells stimulated at the BCR, PCI-29732 blocked the transcriptional up-regulation of a panel of B-cell activation genes that occurs within 6 h of stimulation. Pulse exposure to the reversible inhibitor PCI-29732 did not result in BCR inhibition.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : >53 mg/mL


关键字: cytotoxicity | Bruton tyrosine kinase | Inhibitor | Btk | PCI 29732 | ABCG2 | reversible | BCR | inhibit | B-cell | BCRP | oral | Breast cancer resistance protein

相关产品: Triclabendazole sulfoxide | CP-100356 hydrochloride | ABCG2-IN-1 | YHO-13351 free base | Fumitremorgin C | Zamicastat | 6,8-Diprenylnaringenin | ABCG2-IN-2 | KS176 | Ko 143

相关库: Ion Channel Inhibitor Library | Angiogenesis related Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Tyrosine Kinase Inhibitor Library | NO PAINS Compound Library | Covalent Inhibitor Library

化合物PCI29732 T4337信息由TargetMol中国为您提供，如您想了解更多关于化合物PCI29732 T4337报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途