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Search Results for " bromodomain-containing "

Targets Recommended: Epigenetic Reader Domain

30

抑制剂 & 化合物

1

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T6859	I-BRD9 GSK602	Epigenetic Reader Domain	Chromatin/Epigenetic
	I-BRD9 (GSK602) 是一种选择性的 BRD9 细胞抑制剂，pIC50 为 7.3。
T9552	BAZ1A-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	BAZ1A-IN-1 是BAZ1A（含溴结构域蛋白）抑制剂(Kd:0.52 μM)。它对低表达BAZ1A 的癌细胞表现出弱活性或无活性，但对高表达BAZ1A 的癌细胞系显示出良好的抗生存作用。
T6032	Birabresib OTX-015,OTX015 （MK 8628/Birabresib）,MK-8628	Epigenetic Reader Domain	Chromatin/Epigenetic
	Birabresib (MK-8628) 是一种 BRD2/3/4抑制剂，IC50值为 92 到 112 nM 之间，具有潜在的抗肿瘤活性。
T8609	6-Bromo-3-methyl-1,4-dihydroquinazolin-2-one	Epigenetic Reader Domain	Chromatin/Epigenetic
	6-Bromo-3-methyl-1,4-dihydroquinazolin-2-one 是含溴结构域蛋白 4（人）的抑制剂。
T8601	1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one 4H-Indol-4-one, 2-ethyl-1,5,6,7-tetrahydro-1-(phenylmethyl)-	Epigenetic Reader Domain	Chromatin/Epigenetic
	1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one 是含溴结构域蛋白 4（人）的抑制剂。
T31221	dBRD9 dBRD-9,dBRD 9	PROTACs	PROTAC
	dBRD9是一种 PROTAC。dBRD9是一种双重作用的分子，一部分连接 Bromodomain-containing protein 9 （BRD9）的溴域，另一部分招募小脑 E3泛素连接酶的配体（ligand that recruits the cereblon E3 ubiquitin ligase）。dBRD9对 MOLM-13细胞中 BRD9具有抑制作用，可使其降解，IC50为104 nM。
T6222	PFI-1 PF-6405761,PFI 1,PFI1	Apoptosis; Epigenetic Reader Domain; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic
	PFI-1 (PF-6405761) 是一种BET 抑制剂，能有效抑制 BRD4，IC50值为 0.22 μM。
T3712	Mivebresib ABBV-075,米维布塞	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	Mivebresib (ABBV-075) 是一种有效的，口服活性的溴结构域和末端结构域 (BET) 抑制剂，结合BRD4的Ki 值是 1.5 nM。
TQ0083	NI-57	Epigenetic Reader Domain	Chromatin/Epigenetic
	NI-57 是溴结构域和植物同源锌指结构域 (BRPF) 蛋白家族的一种抑制剂，对 BRPF1、BRPF2 (BRD1) 和 BRPF3 的 IC50值分别为 3.1、46 和 140 nM。
T6828	ZL0420	Epigenetic Reader Domain	Chromatin/Epigenetic
	ZL0420 是有效且选择性的 BET 溴结构域 4 (BRD4) 抑制剂，对 BRD4 的溴结构域 (BD) 具有纳摩尔结合亲和力。ZL0420 对 BRD4 BD1和 BRD4 BD2 的IC50分别为 27 nM 和 32 nM。
T4247	I-CBP112 hydrochloride	Epigenetic Reader Domain	Chromatin/Epigenetic
	I-CBP112 hydrochloride 是含溴结构域转录因子的选择性抑制剂，靶向 CBP/p300 溴结构域。在体内外，它以剂量依赖性方式显着降低 MLL-AF9(+) 急性髓细胞白血病细胞的白血病起始潜力，还增加 BET 溴结构域抑制剂 JQ1 以及阿霉素的细胞毒活性。
T10526	β-NF-JQ1	Others; PROTACs	Others; PROTAC
	β-NF-JQ1是一种PROTAC，可将芳烃受体E3 （AhR E3）连接酶招募到目标蛋白上。β-NF-JQ1使用β-NF 作为AhR 配体靶向含溴odomain（BRD）的蛋白，诱导AhR 和BRD 蛋白相互作用。β-NF-JQ1显示出与蛋白敲除活性相关的强大的抗癌活性。
T10773	CF53	Epigenetic Reader Domain; CDK	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	CF53 是一种高效、选择性、可口服的 BET 抑制剂，对 BRD4 BD1 的 Ki 值为 <1 nM，Kd 值为 2.2 nM，IC50 值为 2 nM；CF53 对 BRD2，BRD3，BRD4 和 BRDT BET 蛋白的 BD1 和 BD2 两个结构域都有高亲和性，对其选择性远高于非含溴结构域 BET 蛋白。CF53 在体外和体内都具有显著的抗肿瘤活性。
T15627	(S)-JQ-35 TEN-010	Others	Others
	(S)-JQ-35 (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins. It has a potential antineoplastic activity.
T17294	ZL0454	Epigenetic Reader Domain	Chromatin/Epigenetic
	ZL0454 is an effective and selective Bromodomain-containing protein 4 inhibitors (IC50: 49 and 32 nM for BD1 and BD2).
T12113	MS645	Epigenetic Reader Domain	Chromatin/Epigenetic
	MS645 是一种含溴结构域蛋白 4 (BRD4) 的抑制剂，对 BRD4-BD1/BD2 的 Ki 值为 18.4 nM。
T81383	PROTAC BRD9 Degrader-5	PROTACs	PROTAC
	PROTACBRD9 Degrader-5为针对BRD9的专一性靶向降解PROTAC，具备选择性地介导BRD9蛋白的降解能力。
T28630	RX-37 RX37	Others	Others
	RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell
T77680	BRD7-IN-3	Epigenetic Reader Domain	Chromatin/Epigenetic
	BRD7-IN-3 (compound 1-78) 作为BRD7/BRD9的双抑制剂，其IC50s分别是1.6 μM和2.7 μM。
T74919	QA-68	Others	Others
	QA-68 (QA-68-ZU81) 为一种高效BRD9降解剂。该化合物抑制细胞周期进展与细胞集落生成，对急性髓系白血病（AML）细胞系展现出抗增殖能力。
T36103	TW9 TW9	Others	Others
	TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistica...
T61727	HDAC6/8/BRPF1-IN-1	Others	Others
	HDAC6/8/BRPF1-IN-1 is a dual inhibitor that targets HDAC6, HDAC8, and the bromodomain and PHD finger containing protein 1 (BRPF1). It exhibits inhibitory activity against HDAC1, HDAC6, and HDAC8 with IC50 values of 797 nM, 344 nM, and 908 nM, respectively. In addition, it inhibits BRPF1 with a Kd value of 175.2 nM. This compound is utilized in cancer research [1].
T63858	I-BET282E	Others	Others
	I-BET282E 是八种 BET bromodomains 泛抑制剂，对其他代表性含溴代烷的蛋白质表现出选择性。I-BET282E 能够作用于 8 种 BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), BRD4 (BD1/BD) ，他们的 pIC50值为 6.4-7.7。
T78801	BRD7-IN-2	Epigenetic Reader Domain	Chromatin/Epigenetic
	BRD7-IN-2（化合物2-77）是针对前列腺癌细胞的有效BRD7抑制剂，具有对BRD7的选择性但不选择性抑制BRD9，IC50分别为5.4 μM和>300 μM。
T21920	UMB-32	Others	Others
	UMB-32 是一种有效的选择性BRD4抑制剂，结合 BRD4 的Kd 为 550 nM，IC50为 637 nM。UMB-32 还显示出对TAF1的效力，TAF1是一种含溴结构域的转录因子。
T75135	FHD-609	Others	Others
	FHD-609 为含溴结构域蛋白BRD9的抑制剂及降解剂，针对ncBAF，适用于研究含BAF复合亚基突变的多种癌症。FHD-609与Telomelysin或INO5401联用，或对肾上腺皮质癌(ACC)的研究具有潜在作用。
T81675	NICE-01 AP1867-PEG2-JQ1,AP-PEG2-JQ1
	NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1)是一款具有双功能的化合物，它通过特异性结合到细胞内特定亚细胞区室中的蛋白质，并以BRD4蛋白的核定位含溴结构域作为诱导，实现将胞浆中的货物输送至细胞核。
T36800	EN219	Others	Others
	EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP hum...
T38381	CAY17c	Others	Others
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...
T63991	BRD4/CK2-IN-1	Others	Others
	BRD4/CK2-IN-1 是高效的、口服具有活力的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂，能够作用于 BRD4 (IC50: 180 nM) 和 CK2 (IC50: 230 nM)。在三阴性乳腺癌 (TNBC) 中，BRD4/CK2-IN-1 能够诱导细胞凋亡和自噬相关的细胞死亡。BRD4/CK2-IN-1 表现出显著的抗癌效果，且没有明显毒性。

化合物

Cat.No: T6859

Synonym: GSK602

Target: Epigenetic Reader Domain

Cat.No: T9552

Target: Epigenetic Reader Domain

Cat.No: T6032

Synonym: OTX-015,OTX015 （MK 8628/Birabresib）,MK-8628

Target: Epigenetic Reader Domain

6-Bromo-3-methyl-1,4-dihydroquinazolin-2-one

Cat.No: T8609

Target: Epigenetic Reader Domain

1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one

Cat.No: T8601

Synonym: 4H-Indol-4-one, 2-ethyl-1,5,6,7-tetrahydro-1-(phenylmethyl)-

Target: Epigenetic Reader Domain

Cat.No: T31221

Synonym: dBRD-9,dBRD 9

Target: PROTACs

Cat.No: T6222

Synonym: PF-6405761,PFI 1,PFI1

Target: Apoptosis, Epigenetic Reader Domain, Autophagy

Cat.No: T3712

Synonym: ABBV-075,米维布塞

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: TQ0083

Target: Epigenetic Reader Domain

Cat.No: T6828

Target: Epigenetic Reader Domain

I-CBP112 hydrochloride

Cat.No: T4247

Target: Epigenetic Reader Domain

Cat.No: T10526

Target: Others, PROTACs

Cat.No: T10773

Target: Epigenetic Reader Domain, CDK

Cat.No: T15627

Synonym: TEN-010

Target: Others

Cat.No: T17294

Target: Epigenetic Reader Domain

Cat.No: T12113

Target: Epigenetic Reader Domain

PROTAC BRD9 Degrader-5

Cat.No: T81383

Target: PROTACs

Cat.No: T28630

Synonym: RX37

Target: Others

Cat.No: T77680

Target: Epigenetic Reader Domain

Cat.No: T74919

Target: Others

Cat.No: T36103

Synonym: TW9

Target: Others

HDAC6/8/BRPF1-IN-1

Cat.No: T61727

Target: Others

Cat.No: T63858

Target: Others

Cat.No: T78801

Target: Epigenetic Reader Domain

Cat.No: T21920

Target: Others

Cat.No: T75135

Target: Others

Cat.No: T81675

Synonym: AP1867-PEG2-JQ1,AP-PEG2-JQ1

Cat.No: T36800

Target: Others

Cat.No: T38381

Target: Others

Cat.No: T63991

Target: Others

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPJ-00694	BRD4 Protein, Human, Recombinant (His & Flag) MCAP,HUNK1,HUNKI,bromodomain-containing pr...	Human	E. coli
	Bromodomain-containing protein 4 (BRD4) is a member of the BET class chromatin reader proteins that bind acetylated histones and play a key role in transcriptional regulation and transmission of epigenetic memory. Remains associated with acetylated chromatin throughout the entire cell cycle and provides epigenetic memory for postmitotic G1 gene transcription by preserving acetylated chromatin status and maintaining high-order chromatin structure. BRD bromodomains serve as recognition motifs for ...

重组蛋白

BRD4 Protein, Human, Recombinant (His & Flag)

Cat.No: TMPJ-00694

Species: Human

Expression System: E. coli

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