產(chǎn)品目錄

規(guī)格	10mg 50mg
CAS
別名
化學(xué)名	(S)-1-(7-(3,4-dimethoxyphenyl)-9-((1-methylpiperidin-3-yl)methoxy)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)propan-1-one
分子式	C27H36N2O5
分子量	468.59
溶解度	Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl
儲存條件	Store at 4°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 All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Description:IC50: 170 nm (CREBBP/EP300)

A bromodomain is an approximately 110 amino acid protein domain that recognizes monoacetylated lysine residues such as those on the N-terminal tails of histones. Members of the BET family (Bromodomain and extraterminal domain family) have been implicated as targets in human cancer. Inhibitors of BET have shown therapeutic effects in multiple models of hematological malignancies as well as solid tumors. SGC have developed an inhibitor, I-CBP112, against the CREBBP and EP300 Bromodomains.

In vitro: A CREBBP/EP300-selective chemical probe from a completely different structural class which was also developed by the SGC is I-CBP112. I-CBP112 has an IC50 value of 170 nm in the CREBBP AlphaScreen assay, and is selective against the bromodomain proteins ATAD2, BAZ2B, BRD2(BD2), BRD4 (BD1), PB1(BD5), PCAF, PHIP(BD2), TRIM24/TIF-1a. In U2OS cells no significant cytotoxicity up to 50 mm was found. Similar to bromosporine 129, data related to SGCCBP30 and I-CBP112 are reported on the SGC homepage exclusively [1].

In vivo: Currently, I-CBP112 is still in the in-vitro investigation, and no animal in-vivo study is on-going.

Clinical trial: I-CBP112 is currently in the preclinical development and no clinical trial is ongoing.

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)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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