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MS417

NMR下載 COA and HPLC MSDS下載
names：
MS417
CAS號：
916489-36-6
MDL Number： No data available
MF(分子式)： C20H19ClN4O2S MW(分子量)： 414.91
EINECS:No data available Reaxys Number:No data available
Pubchem ID:59190723 Brand:BIOFOUNT

MS-417(916489-36-6,GTPL7512)是thienotriazolodiazepines類的成員，是[（6S）-4-（4-氯苯基）-2,3,9-三甲基-6H-thieno [3,2-f] [1]的甲酯，2,4]三唑并[4,3-a] [1,4]二氮雜-6-6基]乙酸。屬于基于硫二氮雜卓類化合物的一組溴結(jié)構(gòu)域和末端外域（BET）特異性抑制劑它是硫雜三氮雜二氮雜卓，是一氯苯和甲基酯的成員。它是MS-566的對映異構(gòu)體。

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM000665-10mg	10mg	99.51%	￥ 3543.00	￥ 3543.00		2-3天	- +	￥ 0.00
YZM000665-5mg	5mg	99.51%	￥ 2437.50	￥ 2437.50		2-3天	- +	￥ 0.00

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中文別名	MS417(916489-36-6),GTPL7512;
英文別名	MS417(916489-36-6),GTPL7512;
CAS號	916489-36-6
Inchi	InChI=1S/C20H19ClN4O2S/c1-10-11(2)28-20-17(10)18(13-5-7-14(21)8-6-13)22-15(9-16(26)27-4)19-24-23-12(3)25(19)20/h5-8,15H,9H2,1-4H3/t15-/m0/s1
InchiKey	GGRCIHACOIMRKY-HNNXBMFYSA-N
分子式 Formula	C20H19ClN4O2S
分子量 Molecular Weight	414.91
溶解度Solubility	生物體外In Vitro:Ethanol : 50 mg/mL(120.51 mM;Need ultrasonic)
性狀	固體粉末,Power
儲藏條件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

MS-417(916489-36-6,GTPL7512)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:MS-417試劑,MS-417雜質(zhì),MS-417中間體,MS-417密度,MS-417合成,MS-417溶解度,MS-417旋光度,MS-417閃點,MS-417熔點,MS-417購買,

產(chǎn)品說明	MS-417(916489-36-6,GTPL7512)是BET特異性蛋白BRD4的抑制劑,能夠與BRD4-BD1和BRD4-BD2 結(jié)合,
Introduction	MS-417(916489-36-6,GTPL7512)is a BETpecificBRD4inhibitor, binds to BRD4D1 and BRD4D2 withIC50s of 30, 46 nM andKds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
Application1	MS-417(916489-36-6,GTPL7512)是BET特異性蛋白BRD4的抑制劑,能夠與BRD4-BD1和BRD4-BD2 結(jié)合,IC50值分別是30,46nM,Kd值分別是 36.1,25.4nM;MS417對CBP BRD的選擇性較低,IC50值是32.7μM
Application2	MS417對CBP BRD的選擇性較低,IC50值是32.7μM
Application3

MS-417(916489-36-6,GTPL7512)藥理學：

MS417 是一種選擇性的 BET 特異性蛋白 BRD4 的抑制劑，能夠與 BRD4-BD1 和 BRD4-BD2 結(jié)合，IC₅₀ 值分別為 30，46 nM，K_d 值分別為 36.1，25.4 nM; MS417 對 CBP BRD 的選擇性較低，IC₅₀ 值為 32.7 μM。

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

Zhang G, et al. Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem. 2012 Aug 17;287(34):28840-51.

Tanaka et al. Design and Characterization of Bivalent BET Inhibitors. Nature Chemical Biology, doi: 10.1038/nchembio.2209, published online 24 October 2016 Nature Chemical Biology

Nowak et al. Plasticity in binding confers selectivity in ligand induced protein degradation. Nature Chemical Biology, doi: 10.1038/s41589-018-0055-y, published online 11 June 2018 Nature Chemical Bi

Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition The Journal of biological chemistry22645123 2012-08-17

Flow Cytometric Analysis of HIV-1 Transcriptional Activity in Response to shRNA Knockdown in A2 and A72 J-Lat Cell Lines PMID 29082287; Bio-protocol 2017 Jun; 7(11): Name matches: i-bet151 ms417

MS-417(916489-36-6,GTPL7512)參考文獻：

1、Design and characterization of bivalent BET inhibitors
Minoru Tanaka, Justin M Roberts, Hyuk-Soo Seo, Amanda Souza, Joshiawa Paulk, Thomas G Scott, Stephen L DeAngelo, Sirano Dhe-Paganon & James E Bradner

Abstract：Cellular signaling is often propagated by multivalent interactions. Multivalency creates avidity, allowing stable biophysical recognition. Multivalency is an attractive strategy for achieving potent binding to protein targets, as the affinity of bivalent ligands is often greater than the sum of monovalent affinities. The bromodomain and extraterminal domain (BET) family of transcriptional coactivators features tandem bromodomains through which BET proteins bind acetylated histones and transcription factors. All reported antagonists of the BET protein BRD4 bind in a monovalent fashion. Here we describe, to our knowledge for the first time, a bivalent BET bromodomain inhibitor—MT1—which has unprecedented potency. Biophysical and biochemical studies suggest MT1 is an intramolecular bivalent BRD4 binder that is more than 100-fold more potent, in cellular assays, than the corresponding monovalent antagonist, JQ1. MT1 significantly (P < 0.05) delayed leukemia progression in mice, as compared to JQ1. These data qualify a powerful chemical probe for BET bromodomains and a rationale for further development of multidomain inhibitors of epigenetic reader proteins.

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