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化學性質:
規(guī)格 | 5mg 25mg |
CAS | 1714146-59-4 |
別名 |
|
化學名 | 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 |
分子式 | C22H22F3N3O3S2 |
分子量 | 497.55 |
溶解度 | DMF: 30 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 25 mg/mL |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
pIC50: 7.3
I-BRD9 is a BRD9 inhibitor.
BRD9 is identified as a bromodomain containing protein forming a small sub-branch of the bromodomain family tree. Human BRD9 has a single bromodomain and contains five isoforms which are produced by alternative splicing.
In vitro: In previous study, the I-BRD9 development was driven by iterative medicinal chemistry, using structure based design to result in nanomolar potency at BRD9, over 700-fold selectivity against the BET family as well as more than 70-fold to a panel of 34 bromodomains. In Kasumi-1 cells, I-BRD9 could downregulate DUSP6, CLEC1, SAMSN1 and FES genes. Moreover, I-BRD9 was used to expore genes regulated by BRD9 in Kasumi-1 cells involved in immune response and oncology pathways. In addition, when BRD4 was used as a representative member of the BET family for initial selectivity screening, I-BRD9 was found to have a pIC50 of 5.3 against this protein. I-BRD9 thus represented the first available selective tool compound to investigate the cellular phenotype of the inhibition of BRD9 bromodomain [1].
In vivo: So far, there is no animal in vivo data reported for I-BRD9.
Clinical trial: Up to now, I-BRD9 is still in the preclinical development stage.
特別提醒:
1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區(qū)。
2. 為了您的安全和健康,請穿好實驗服并佩戴一次性手套和口罩操作。
原創(chuàng)作者:上海莼試生物技術有限公司
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賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業(yè)部
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