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Cat. No.	Product Name	Target	Signaling Pathways
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].
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。
T26897	BRD2492	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	BRD2492 是一种具有选择性和有效的 HDAC1 和 HDAC2 双重抑制剂，具有潜在的抗癌、抗肿瘤和抗增殖活性，抑制 HDAC1/2 、HDAC3 和 HDAC6。BRD2492 对乳腺癌细胞系的生长有抑制作用，诱导细胞凋亡。
T25176	BRD2577 BRD-2577,BRD 2577
	BRD2577 is an HDAC inhibitor, by suppressing multiple HDAC enzymes and modulating acetylation levels in cells.
T26898	BRD2879 BRD 2879,BRD-2879
	BRD2879 is a potent and cell-active inhibitor of IDH1-R132H (IC50 = 50 nM).
T69645	BRD20322
	BRD20322 is a novel potent inhibitor of spCas9, disrupting spCas9-DNA binding and exerting dose and temporal control of spCas9 in human cell lines.
T74406	BRD2889
	BRD2889 是生物碱胡椒胺的类似物。BRD2889 是肺动脉高压 (PH) 中GSTP1-ISCU 轴的强大调节剂。
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。
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。
T6255	Bromosporine	Epigenetic Reader Domain; CDK	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	Bromosporine 是广谱 BRD2/4/9 和 CECR2 溴结构域抑制剂，IC50为0.41、0.29、0.122和0.017 μM。
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。
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。
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。
T72058L	CDD-1102 HCl CDD-1102 HCl(2757619-84-2 Free base)	Epigenetic Reader Domain	Chromatin/Epigenetic
	CDD-1102 HCl 是一种新型BRDT-BD4 / BRD2-BD1302选择性抑制剂，在体内外实验中显示出非激素避孕潜力。
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。
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。
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。
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。
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。
T1854	MS436	Epigenetic Reader Domain	Chromatin/Epigenetic
	MS436 是溴结构域抑制剂，作用于 BRD4 BrD1的Ki 为 30 到 50 nM 之间，比作用于 BrD2 选择性高 10 倍。
T78682	SJ1461	Epigenetic Reader Domain	Chromatin/Epigenetic
	SJ1461为一种BET抑制剂，具有口服活性。该化合物针对BRD2(BD1)、BRD2(BD2)、BRD4(BD1)与BRD4(BD2)展现出抑制作用，对应IC50值依次为1.6 nM、0.1 nM、6.5 nM及0.2 nM。
T28931	TC-AC28 TC AC28
	TC-AC28 is a novel potent and selective Brd2(2) ligand.
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)。
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).
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。
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 ...
T10522	BET-IN-6	Epigenetic Reader Domain	Chromatin/Epigenetic
	BET-IN-6 是一种有效且高亲和力的BRD2/BRD4抑制剂。BET-IN-6 是靶蛋白 BRD2/4 的配体，可用于合成 PROTAC BRD2/BRD4 degrader-1 。
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。
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
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.
T64192	BRD4 D1-IN-2
	BRD4 D1-IN-2 (compound 26) 是一种选择性的、有效的 BRD4 D1 抑制剂，其 IC50 值小于 0.092 μM。BRD4 D1-IN-2 对 BRD4 D1 具有 15 nM 亲和力，对 BRD2 D1 和 BRD4 D2 具有 500 倍以上的选择性。
T18808	Thalidomide-NH-C4-NH2 TFA	Others	Others
	Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate consisting of an E3 ligase ligand-linker, incorporating the Thalidomide-based cereblon ligand and a linker moiety. This compound, Thalidomide-NH-C4-NH2 TFA, is utilized as a component in PROTAC BRD2/BRD4 degrader-1, which is a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].
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.
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.
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。
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。
T79065	WWL0245	Epigenetic Reader Domain	Chromatin/Epigenetic
	WWL0245是一种高效的选择性BRD4 PROTAC，能够在DC50小于1 nM的低浓度下选择性地降解BRD4，而对BRD2/3和PLK1的降解效果则在DC50大于1 μM时才显现。在BETi敏感的多种癌细胞系中，尤其是AR阳性的前列腺癌细胞系，WWL0245展现出显著的选择性细胞毒性效果。作为AR阳性前列腺癌研究的潜力药物，WWL0245也被视为研究BRD4生物学功能的重要工具化合物。
T69506	dBRD4-BD1
	dBRD4-BD1 is a selective BRD4 bromodomain inhibitor. dBRD4-BD1 can selectively degrade BRD4 (DC50 = 280 nM). Notably, dBRD4-BD1 upregulates BRD2/3, a result not observed with degraders using pan-BET ligands. Designing BRD4 selectivity up front enables analysis of BRD4 biology without wider BET-inhibition and simplifies designing BRD4-selective heterobifunctional molecules, such as degraders with new E3 recruiting ligands or for additional probes beyond degraders.
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。
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。
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...
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...
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...
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。
T38381	CAY17c
	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,...
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。

化合物

PROTAC BRD2/BRD4 degrader-1

Cat.No: T18598

Target: Others

Cat.No: T8932

Synonym: iBET-BD2

Target: Epigenetic Reader Domain

Cat.No: T2120

Synonym: GSK1210151A

Target: Epigenetic Reader Domain

Cat.No: T26897

Target: HDAC

Cat.No: T25176

Synonym: BRD-2577,BRD 2577

Cat.No: T26898

Synonym: BRD 2879,BRD-2879

Cat.No: T69645

Cat.No: T74406

Cat.No: T22345

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

Target: Epigenetic Reader Domain

Cat.No: T10638

Target: Epigenetic Reader Domain

Cat.No: T6021

Synonym: I-BET726

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T6255

Target: Epigenetic Reader Domain, CDK

Cat.No: TQ0253

Target: Epigenetic Reader Domain

Cat.No: T4697

Synonym: ABBV744

Target: Epigenetic Reader Domain, HIV Protease

Cat.No: T5435

Target: Epigenetic Reader Domain

Cat.No: T19935

Target: Epigenetic Reader Domain

Cat.No: T72058L

Synonym: CDD-1102 HCl(2757619-84-2 Free base)

Target: Epigenetic Reader Domain

GSK778 hydrochloride

Cat.No: T9703L

Target: Epigenetic Reader Domain

Cat.No: T12112

Target: Epigenetic Reader Domain

Cat.No: T10773

Target: Epigenetic Reader Domain, CDK

Cat.No: T9703

Target: Epigenetic Reader Domain

Cat.No: T28628

Synonym: RVX297

Target: Epigenetic Reader Domain

Cat.No: T6032

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

Target: Epigenetic Reader Domain

Cat.No: T1854

Target: Epigenetic Reader Domain

Cat.No: T78682

Target: Epigenetic Reader Domain

Cat.No: T28931

Synonym: TC AC28

Cat.No: T15484

Target: Epigenetic Reader Domain

Cat.No: T15419

Target: Epigenetic Reader Domain

Cat.No: T63858

Cat.No: T41226

Cat.No: T10522

Target: Epigenetic Reader Domain

Cat.No: T74391

Cat.No: T28630

Synonym: RX37

BET bromodomain inhibitor 1

Cat.No: T39998

Cat.No: T64192

Thalidomide-NH-C4-NH2 TFA

Cat.No: T18808

Target: Others

BRD PHOTAC-I-3

Cat.No: T41198

Cat.No: T39601

Synonym: GSK973

Cat.No: T63924

Cat.No: T36573

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T79065

Target: Epigenetic Reader Domain

Cat.No: T69506

BRD4 Inhibitor-28

Cat.No: T78851

Target: Epigenetic Reader Domain

Cat.No: T14550

Synonym: ZBC 260

Target: Epigenetic Reader Domain

Cat.No: T18060

Target: Others

Birabresib dihydrate

Cat.No: T69963

FT-1101 free base

Cat.No: T70210

Cat.No: T5436

Target: Epigenetic Reader Domain

Cat.No: T38381

Cat.No: T12660L

Target: Epigenetic Reader Domain

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