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Cat. No.	Product Name	Target	Signaling Pathways
T78956	PROTAC BRD3/BRD4-L degrader-2	Epigenetic Reader Domain	Chromatin/Epigenetic
	PROTACBRD3/BRD4-L degrader-2 是一款可以特异性地降解BRD3和BRD4-L的PROTAC分子，其对BRD3的Ki值为16.91 nM，对BRD4-L为2.8 nM。在小鼠异种移植模型中，该分子展示了卓越的抗肿瘤效果，可被应用于癌症相关研究。
T8932	GSK046 iBET-BD2	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK046 (iBET-BD2) 是一种选择性和具有口服活性的 BET 蛋白 BD2溴结构域的抑制剂，对 BRD2 BD2、BRD3 BD2、BRD4 BD2 和 BRDT BD2的 IC50值为 264、98、49 和 214 nM，具有免疫调节活性。
T2120	I-BET151 GSK1210151A	Epigenetic Reader Domain	Chromatin/Epigenetic
	I-BET151 (GSK1210151A) 是 BRD2/3/4 的特异性 BET 抑制剂，IC50值分别为0.5、0.25、0.79 μM。
T23820	BRD32048 BRD-32048,BRD 32048	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	BRD32048 可以与与 ETV1直接结合，KD 为 17.1 μM。BRD32048调节 ETV1 介导的转录活性和 ETV1 驱动的癌细胞侵袭。 BRD32048可以抑制 ETV1 乙酰化并促进其降解。
T8233	BRD3308	Apoptosis; HIV Protease; HDAC	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	BRD3308 是一种高选择性的HDAC3抑制剂，IC50为 54 nM。它可激活HIV-1转录并破坏HIV-1潜伏期。它抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡，并增加功能性胰岛素释放。
T39457	(R)-BRD3731 (R)-BRD3731
	(R)-BRD3731, a GSK3 inhibitor, specifically compound example 273. It exhibits inhibitory activity with respective IC50 values of 1.05 μM for GSK3β and 6.7 μM for GSK3α.
T61578	BRD3731
	BRD3731 is a selective inhibitor of GSK3β, demonstrating an IC50 value of 15 nM for GSK3β and 215 nM for GSK3α. Due to its inhibitory properties, BRD3731 holds promise for investigating various medical conditions, including post-traumatic stress disorder (PTSD), psychiatric disorders, diabetes, and neurodegenerative disorders [1].
T30578	BRD3067 BRD-3067,BRD 3067
	BRD3067 is a negative control for tubastatin A.
T22345	INCB054329 INCB-054329,INCB-54329,INCB-54329	Epigenetic Reader Domain	Chromatin/Epigenetic
	INCB054329 是一种结构不同的溴结构域和末端外结构域 (BET) 抑制剂，可抑制 BRD2-BD1、BRD2-BD2、BRD3-BD1、BRD3-BD2、BRD4-BD1、BRD4-BD2、BRDT-BD1 和 BRDT-BD2，IC50 值为分别为 44 nM、5 nM、9 nM、1 nM、28 nM、3 nM、119 nM 和 63 nM。
T10638	BY27	Epigenetic Reader Domain	Chromatin/Epigenetic
	BY27 是一种具有强效性和选择性的 BET BD2 抑制剂（Ki：3.1 nM），具有抗癌活性，抑制 BRD2、BRD3、BRD4 和 BRDT 的 BD1/BD2，抑制肿瘤生长。
TQ0253	PLX51107	Epigenetic Reader Domain	Chromatin/Epigenetic
	PLX51107 是一种选择性 BET 抑制剂，与 CBP 和 EP300 的结构域相互作用。它对 BRD2、BRD3、BRD4 和 BRDT 的 BD1 结构域的亲和力Kd 值分别为 1.6、2.1、1.7 和 5 nM，BD2 结构域亲和力Kd 值分别为 5.9、6.2、6.1 和 120 nM。
T6021	GSK1324726A I-BET726	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	GSK1324726A (I-BET726) 是一种选择性有效的BET 蛋白抑制剂，高亲和力结合到BRD2、BRD3和BRD4，IC50值分别为 41 nM、31 nM 和 22 nM。
T5435	ARV-771	Epigenetic Reader Domain	Chromatin/Epigenetic
	ARV-771 是基于 PROTAC 技术的有效 BET 降解剂，对 BRD2(1)、BRD2(2)、BRD3(1)、BRD3(2)、BRD4 (1) 和 BRD4(2)的 Kd 分别为 34、4.7、8.3、7.6、9.6 和 7.6 nM。
T19935	XD14	Epigenetic Reader Domain	Chromatin/Epigenetic
	XD14 是BET 抑制剂，其与 BRD2、BRD3 和 BRD4 的结合常数分别为 170 nM、380 nM 和 160 nM。它具有抗肿瘤活性。
T9703L	GSK778 hydrochloride	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK778 hydrochloride hydrochloride 是一种有效的、选择性的 BET 蛋白 BD1 溴结构域抑制剂，IC50 分别为 75 nM (BRD2 BD1)、41 nM (BRD3 BD1)、41 nM (BRD4 BD1) 和 143 nM (BRDT BD1)。它对 pan-BET 抑制剂在癌症模型中的作用进行表型复制。
T12112	MS402	Epigenetic Reader Domain	Chromatin/Epigenetic
	MS402 是一种新型 BD1 选择性 BET BrD 抑制剂，阻断 Th17 细胞分化并改善小鼠结肠炎，对BRD4(BD1)、BRD4(BD2)、BRD3(BD1)、BRD3(BD2)、BRD2(BD1)和BRD2(BD2)的Ki 分别为 77 、718、110、200、83 和 240 nM。
T9703	GSK778	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK778 是BET 蛋白BD1溴结构域的选择性抑制剂，对BRD2 BD1、BRD3 BD1、BRD4 BD1、BRDT BD1的IC50分别为75 nM，41 nM，41 nM 和143 nM。
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。
T28628	RVX-297 RVX297	Epigenetic Reader Domain	Chromatin/Epigenetic
	RVX-297 是口服具有活性的，对BD2有选择性的BET 高效抑制剂，作用于BRD2(BD2)、BRD3(BD2)、BRD4(BD2) 的IC50分别为 0.08、0.05、0.02 μM。它能够阻碍多种免疫细胞炎症基因的表达，对临床前模型急性炎症及自身免疫均有效。
T15484	HJB97	Epigenetic Reader Domain	Chromatin/Epigenetic
	HJB97 可用于开发设计 PROTAC BET 的降解剂，具有抗肿瘤活性。HJB97 是高亲和力的 BET 抑制剂，Ki 值分别为 0.9 nM (BRD2 BD1)，0.27 nM (BRD2 BD2)，0.18 nM (BRD3 BD1)，0.21 nM (BRD3 BD2)，0.5 nM (BRD4 BD1)，1.0 nM (BRD4 BD2)。
T28630	RX-37 RX37
	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
T41198	BRD PHOTAC-I-3
	BRD PHOTAC-I-3 is a photoswitchable BET bromodomain degrader (PHOTAC, PHOtochemically TArgeting Chimera). BRD PHOTAC-I-3 comprises a ligand for an E3 ligase, a photoswitch, and the BET bromodomain targeting ligand (+)-JQ1. Exhibits cytotoxicity and degrades BRD4, BRD3 and to a lesser extent BRD2 in lymphoblast cells upon irradiation with 390 nm light, but not in the dark.
T13786	MZP-55	Epigenetic Reader Domain	Chromatin/Epigenetic
	MZP-55 is a selective BRD3/4 degrader based on PROTAC technology(Brd4BD2 with Kd of 8 nM)
T39998	BET bromodomain inhibitor 1
	BET bromodomain inhibitor 1 is an orally active, selective inhibitor of bromodomain and extra-terminal (BET) proteins. It specifically inhibits BRD4 with an IC50 of 2.6 nM. Additionally, BET bromodomain inhibitor 1 demonstrates high affinities towards BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, and 2.1 nM, respectively. This compound exhibits anti-cancer activity.
T74391	OARV-771
	OARV-771 是一种基于 VHL 的 BET 降解剂 (PROTAC)，具有改善的细胞通透性。OARV-771 显示 Brd4、Brd2 和 Brd3的 DC50分别为 6、1 和 4 nM。
T79034	GXF-111	Epigenetic Reader Domain	Chromatin/Epigenetic
	GXF-111是一种PROTAC分子，能够选择性促进BRD3与BRD4-L在细胞内的降解。该分子与BRD3BD1和BRD3BD2的结合亲和力显著，Ki值分别为11.97 nM和2.35 nM。GXF-111主要用于癌症研究领域。
T41226	SIM1
	SIM1 is a potent and selective trivalent PROTAC®Degrader based on BET bromodomain inhibitors linked to a Von Hippel Lindau (VHL) ligand via branched linkers. SIM1 degrades all BET family proteins with a preference for BRD2 (DC50values = 0.7 nM, 1.1 nM and 3.3 nM for BRD4, BRD2 and BRD3, respectively). SIM1 degrades BRD2 more significantly and rapidly than BRD3 and BRD4, and degrades BET proteins with a higher potency than a bivalent degrader. SIM1 also decreases protein levels for Myc and HMOX1 ...
T63858	I-BET282E
	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。
T13785	MZP-54	Epigenetic Reader Domain	Chromatin/Epigenetic
	MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)
T18598	PROTAC BRD2/BRD4 degrader-1	Others	Others
	PROTAC BRD2/BRD4 degrader-1 (compound 15) serves as a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination of BRD4 and BRD2 compared to BRD3. Its efficacy in suppressing solid tumors manifest with minimal cytotoxic effects. This compound comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN)/cullin 4A[1].
T63924	XY153
	XY153 (compound 8l) 是一种 BD2 选择性的 BET 抑制剂，能够选择性的结合 BRD4 BD2 。XY153 可以结合 BRD4 BD2 (IC50: 0.79 nM)，BRD3 BD2 (IC50: 5.31 nM) 和 BRD2 BD2 (IC50: 5.09 nM)。XY153 对多种肿瘤细胞系表现出有效的抗增殖效果。XY153 能够用于研究急性髓性白血病和癌症。
T39601	GSK973 GSK973
	GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5.
T36573	NHWD-870	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	NHWD-870 是一种有效且特异性的 BET 家族溴结构域抑制剂，仅与 BRD2、BRD3、BRD4 (IC50 = 2.7 nM) 和 BRDT 结合。 NHWD-870 具有强大的抗肿瘤功效，并通过增加肿瘤细胞凋亡和抑制肿瘤增殖来抑制癌细胞-巨噬细胞相互作用。
T36574	GW841819X GW841819X
	GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70...
T78851	BRD4 Inhibitor-28	Epigenetic Reader Domain	Chromatin/Epigenetic
	BRD4Inhibitor-28（Compound 18）是一款具有口服活性的BRD4抑制剂，其针对BRD40-BD1和BRD40-BD2的IC50值分别为15和55 nM。该化合物同时对BRD2-BD1、BRD3-BD1和BRDT-BD1也表现出抑制作用，对应的IC50值依次为19、25和68 nM。此外，BRD4Inhibitor-28在抗黑色素瘤方面展现出活性。
T69963	Birabresib dihydrate
	Birabresib dihydrate was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and dif...
T18060	KB02-JQ1	Others	Others
	KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a link...
T70210	FT-1101 free base
	FT-1101 is an orally bioavailable, potent and selective BET inhibitor. FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional r...
T14550	BETd-260 ZBC 260	Epigenetic Reader Domain	Chromatin/Epigenetic
	BETd-260是一种 PROTAC，由 Cereblon 配体和 BET 配体相连，对白血病细胞株 BRD4蛋白的抑制作用。
T5436	MZ 1	Epigenetic Reader Domain	Chromatin/Epigenetic
	MZ 1 是由 von Hippel-Lindau 配体和 BRD4配体相连的 PROTAC，是一种 BRD4 蛋白降解剂。
T12660L	BAY1238097	Epigenetic Reader Domain	Chromatin/Epigenetic
	BAY1238097 是一种具有有效性和选择性的溴结构域和末端外基序(BET)抑制剂，具有抗癌活性，在AML (急性髓性白血病) 和MM (多发性骨髓瘤) 模型中表现出较强的抗增殖活性。BAY1238097 可用于研究晚期难治性恶性肿瘤。
T4697	ABBV-744 ABBV744	Epigenetic Reader Domain; HIV Protease	Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome
	ABBV-744 是一种 BDII 选择性 BET 溴结构域抑制剂，可抑制 BRD2/3/4。它可研究炎症性疾病、癌症和艾滋病。
T79527	BET BD2-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	BET BD2-IN-1（compound 45）为BETBD2选择性抑制剂，IC50值为1.6 nM，通过抑制STAT3与NF-κB活性，阻断Th17细胞的分化，适用于银屑病与炎症性肠病研究。
T5439	BRD4 degrader AT1	Epigenetic Reader Domain	Chromatin/Epigenetic
	BRD4 degrader AT1 是基于 PROTAC 技术的高选择性 Brd4 降解剂，在细胞中对 Brd4BD2 的 Kd 为 44 nM。
T11887	LT052	Epigenetic Reader Domain	Chromatin/Epigenetic
	LT052 是一种高活性和选择性BET BD1抑制剂，其IC50为 87.7 nM。LT052 表现出纳摩尔级别的 BRD4 BD1 的抑制活性，选择性是 BRD4 BD2 的 138 倍 (IC50=12.130 μM)。LT052 具有抗炎活性，可用于治疗急性痛风性关节炎。
T15419	GS-626510	Epigenetic Reader Domain	Chromatin/Epigenetic
	GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).

化合物

PROTAC BRD3/BRD4-L degrader-2

Cat.No: T78956

Target: Epigenetic Reader Domain

Cat.No: T8932

Synonym: iBET-BD2

Target: Epigenetic Reader Domain

Cat.No: T2120

Synonym: GSK1210151A

Target: Epigenetic Reader Domain

Cat.No: T23820

Synonym: BRD-32048,BRD 32048

Target: DNA/RNA Synthesis

Cat.No: T8233

Target: Apoptosis, HIV Protease, HDAC

Cat.No: T39457

Synonym: (R)-BRD3731

Cat.No: T61578

Cat.No: T30578

Synonym: BRD-3067,BRD 3067

Cat.No: T22345

Synonym: INCB-054329,INCB-54329,INCB-54329

Target: Epigenetic Reader Domain

Cat.No: T10638

Target: Epigenetic Reader Domain

Cat.No: TQ0253

Target: Epigenetic Reader Domain

Cat.No: T6021

Synonym: I-BET726

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T5435

Target: Epigenetic Reader Domain

Cat.No: T19935

Target: Epigenetic Reader Domain

GSK778 hydrochloride

Cat.No: T9703L

Target: Epigenetic Reader Domain

Cat.No: T12112

Target: Epigenetic Reader Domain

Cat.No: T9703

Target: Epigenetic Reader Domain

Cat.No: T10773

Target: Epigenetic Reader Domain, CDK

Cat.No: T28628

Synonym: RVX297

Target: Epigenetic Reader Domain

Cat.No: T15484

Target: Epigenetic Reader Domain

Cat.No: T28630

Synonym: RX37

BRD PHOTAC-I-3

Cat.No: T41198

Cat.No: T13786

Target: Epigenetic Reader Domain

BET bromodomain inhibitor 1

Cat.No: T39998

Cat.No: T74391

Cat.No: T79034

Target: Epigenetic Reader Domain

Cat.No: T41226

Cat.No: T63858

Cat.No: T13785

Target: Epigenetic Reader Domain

PROTAC BRD2/BRD4 degrader-1

Cat.No: T18598

Target: Others

Cat.No: T63924

Cat.No: T39601

Synonym: GSK973

Cat.No: T36573

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T36574

Synonym: GW841819X

BRD4 Inhibitor-28

Cat.No: T78851

Target: Epigenetic Reader Domain

Birabresib dihydrate

Cat.No: T69963

Cat.No: T18060

Target: Others

FT-1101 free base

Cat.No: T70210

Cat.No: T14550

Synonym: ZBC 260

Target: Epigenetic Reader Domain

Cat.No: T5436

Target: Epigenetic Reader Domain

Cat.No: T12660L

Target: Epigenetic Reader Domain

Cat.No: T4697

Synonym: ABBV744

Target: Epigenetic Reader Domain, HIV Protease

Cat.No: T79527

Target: Epigenetic Reader Domain

BRD4 degrader AT1

Cat.No: T5439

Target: Epigenetic Reader Domain

Cat.No: T11887

Target: Epigenetic Reader Domain

Cat.No: T15419

Target: Epigenetic Reader Domain

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