I-BRD9 ( I-BRD9 | I-BRD-9 | I-BRD 9 )

产品货号. M12612 CAS No. 1714146-59-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

I-BRD9
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

第一个针对 BRD9 的选择性细胞化学探针，pIC50 为 7.3。
产品描述

The first selective cellular chemical probe for BRD9 with pIC50 of 7.3; displays 700-fold selectivity over the BET family and 200-fold over the highly homologous BRD7; decreases cell proliferation, G1-arrest and apoptosis in rhabdoid tumor cells; shows synergistic inhibitory effects on cell proliferation combined with doxorubicin or carboplatin.
体外实验

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. 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.
体内实验

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同义词

I-BRD9 | I-BRD-9 | I-BRD 9
通路

Chromatin/Epigenetic
靶点

Bromodomain
受体

BRD4|BRD9
研究领域

Other Indications
适应症

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CAS Number

1714146-59-4
分子量

497.5536
分子式

C22H22F3N3O3S2
纯度

>98% (HPLC)
溶解度

DMSO: 15.5 mg/mL
SMILES

N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O
化学全称

Thieno[3,2-c]pyridine-2-carboximidamide, 5-ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]-

1. Theodoulou NH, et al. J Med Chem. 2016 Feb 25;59(4):1425-39. 2. Kr?mer KF, et al. Int J Mol Sci. 2017 Jul 16;18(7). pii: E1537.

计算器

产品手册

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