中文名称 :[优选]I-BRD9
英文名称 :I-BRD9
英文别名 :N-(1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-5-ethyl-4-oxo-7-(3-(trifluoromethyl)phenyl)-4,5-dihydrothieno[3,2-c]pyridine-2-carboximidamide;I-BRD9;GSK602;5-ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]-thieno[3,2-c]pyridine-2-carboximidamide;N'-[1,1-Bis(Oxidanylidene)thian-4-Yl]-5-Ethyl-4-Oxidanylidene-7-[3-(Trifluoromethyl)phenyl]thieno[3,2-C]pyridine-2-Carboximidamide;H1B;compound 45 [PMID 25856009];GTPL8397
Cas No. :1714146-59-4
分子式 :C22H22F3N3O3S2
分子量 :497.55
生物活性
I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC50 value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways.
性状
Solid
体外研究(In Vitro)
I-BRD9 (10 μM, 6 h) has a regulation role in cancer and immunology pathways.
I-BRD9 (10 μM) has high BRD9 affinity and excellent broader bromodomain selectivity.
I-BRD9 (10 μM) has affinity for BRD9 (TR-FRET), BRD4 BD1 (TR-FRET) and BRD9 NanoBRET with pIC50 values of 7.3 μM, 5.3 μM and 6.8 μM.
I-BRD9 (10 μM) has high aqueous solubility (CLND) with 359 μM.
I-BRD9 (10 μM) displays >625 fold selectivity in binding with endogenous BRD9 against BET family member BRD3 in HUT-78 cell lysate.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR
Cell Line: Kasumi-1 cells
Concentration: 10 μM
Incubation Time: 6 h
Result: Showed 4 genes (CLEC1, 62 DUSP6, 63 FES64 and SAMSN165) that were strongly down-regulated and not by I-BET151.
运输条件
Room temperature or refrigerated transportation.
