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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
T60079	GNE-064 GNE064	Epigenetic Reader Domain	Chromatin/Epigenetic
	GNE-064 是一种选择性的，具有口服活性的以及高可溶性的 SMARCA4，SMARCA2 和 PBRM1 bromodomains 5 抑制剂。GNE-064 对 SMARCA4 具有抑制作用，其 IC50 值为 0.035 μM，对 SMARCA2 也具有抑制作用，其 EC50 值为 0.10 μM。GNE-064 对 SMARCA4，SMARCA2，PBRM1 bromodomains 5 和 PBRM1 bromodomains 2 的 Kd 值为 0.01，0.016，0.018 以及 0.049 μM。GNE-064 可以作为一种药物探针，用于药物合成的研究。
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。
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。
T1972	GSK-5959	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK 5959 是一种选择性的、细胞渗透性的BRPF1溴端结构域的抑制剂，其IC50值为 80 nM。她对 BRPF1 的选择性是 35 个其他溴结构域的 100 倍以上。
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。
T3973	PF-CBP1	Epigenetic Reader Domain	Chromatin/Epigenetic
	PF-CBP1 是一种高选择性的 CREB 结合蛋白 (CREBBP) 溴结构域抑制剂。它抑制 CREBBP (IC50: 125 nM) 和 p300 溴结构域 (IC50: 363 nM)。
T15784	LP99	Epigenetic Reader Domain	Chromatin/Epigenetic
	LP99 是一种表观遗传探针，可破坏 BRD7 和 BRD9 与细胞中染色质的结合。它是一种选择性的 BRD7 和 BRD9 溴结构域抑制剂，对 BRD9 的 Kd 为 99 nM。
T2436	GSK2801	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	GSK2801 是一种有口服活性的和细胞活性的乙酰赖氨酸竞争性BAZ2A 和BAZ2B 溴结构域选择性抑制剂，Kd 值分别为 136 nM 和 257 nM。
T8658	NEO2734 EP31670	Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic
	NEO2734 (EP31670) 是一种具有口服活性的选择性 p300/CBP 和 BET 溴结构域抑制剂，其 IC50值均小于30 nM，可用于前列腺癌的研究。
T3969	I-CBP112	Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic
	I-CBP112 是一种特异性的乙酰赖氨酸竞争性蛋白质-蛋白质相互作用抑制剂，靶向 CBP/p300 溴结构域，增强 p300 的乙酰化作用。
T6939	PFI-3 PFI 3	Epigenetic Reader Domain	Chromatin/Epigenetic
	PFI-3是一种选择性，可渗透细胞的SMARCA2/4溴结构域抑制剂，Kd 值为89 nM，可延迟和预防乳腺癌。
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。
T3217	PF-CBP1 hydrochloride PF-CBP1 HCl	Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic
	PF-CBP1 hydrochloride (PF-CBP1 HCl) 是 CREB 结合蛋白溴结构域的一种高选择性抑制剂，抑制 CREBBP 和 EP300溴结构域的 IC50分别为 125 和 363 nM。它降低 LPS 诱导的巨噬细胞中炎症因子的表达，也可下调皮质神经元 RGS4 的表达，可用于癫痫和帕金森病等神经疾病的研究。
T9020	GSK620	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK620 是一种有口服活性的泛BD2抑制剂，在人全血中表现出抗炎表型，有良好的广谱选择性、可开发性和体内口服药代动力学。它对 BET-BD2 家族蛋白具有高度选择性，其选择性超过所有其他 BET 溴结构域 200 倍以上。
T27071	CPI571
	CPI571 is a potent and selective inhibitor for the bromodomains of CREBBP/EP300.
T69952	BiBET
	BiBET is a potent, selective, bivalent inhibitor of BET bromodomains.
T26758	BDOIA383
	BDOIA383 is a novel inhibitor of CBP/p300 Bromodomains.
T39461	MT1
	MT1, a bivalent chemical probe targeting BET bromodomains, demonstrates an IC50 value of 0.789 nM for BRD4(1).
T69588	GSK789
	GSK789 is a selective inhibitor of the first bromodomains (BD1) of the bromo and extra terminal domain (BET) proteins.
T41202	TP 472N
	TP 472N is a negative control forTP 472. Inactive against other bromodomains (>20μM against BRD9).
T14512	BAZ2-ICR	Epigenetic Reader Domain	Chromatin/Epigenetic
	BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.
T70593	GW-841819X
	GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia. Bromodomain and extra-terminal (BET) proteins belong to a class of proteins collectively called epigenetic readers". BET bromodomains have emerged as promising drug targets for treatment of cancers
T27068	CPI098 CPI-098,CPI 098
	CPI098 is a potent and selective inhibitors for the bromodomains of CREBBP/EP300. CREBBP/EP300 bromodomains play a critical role in regulatory T cell biology. T cell recruitment to tumors is a major mechanism of immune evasion by cancer cells.
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).
T12798	(S)-GNE-987	Epigenetic Reader Domain	Chromatin/Epigenetic
	(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
T39826	CBP/p300-IN-8 CBP/p300-IN-8
	CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains . CBP/p300-IN-8 inhibits CBP ( IC 50 =0.01-0.1 μΜ) and BRD4 ( IC 50 =1-1000 μΜ) activity.
T11292	FKBP12 PROTAC dTAG-7 dTAG-7	Epigenetic Reader Domain	Chromatin/Epigenetic
	FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.
T39073	Amredobresib
	Amredobresib is a potent BET inhibitor that impedes the interaction between bromodomains and acetylated lysines on histone H3 and H4, thereby serving as crucial regulators of gene transcription. It proves valuable in the investigation of acute myeloid leukemia (AML) and cancer.
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。
T79907	HPP-9
	HPP-9为一种蛋白降解靶向嵌合体(PROTACs)，基于Hedgehog通路抑制剂(HPI-1)开发，pIC50值为6.71，能够降解BET溴结构域，并表现出抗肿瘤活性[1]。
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...
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...
T11441	GNE-987	Epigenetic Reader Domain	Chromatin/Epigenetic
	GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03
T11291	FKBP12 PROTAC dTAG-13 dTAG-13	Epigenetic Reader Domain	Chromatin/Epigenetic
	FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader.
T36109	L Moses dihydrochloride
	High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 P...
T63220	Bromodomain inhibitor-9
	Bromodomain inhibitor-9 是Bromodomains 抑制剂，可选择性抑制 BRD4-1的活性，其 Kd 值为 12 nM。Bromodomain inhibitor-9 能够用于与全身或脂质代谢、组织炎症、纤维化或慢性自身免疫性疾病相关疾病的研究。
T73390	I-BET432
	I-BET432 是一种BET 抑制剂。I-BET432 抑制BRD4的 N 端溴化域 (BD1) 和 C 端溴化域 (BD2) 的pIC50值分别为 7.5 和 7.2。I-BET432 可作为多种肿瘤和炎症疾病研究的口服候选分子。
T79642	IV-275	Epigenetic Reader Domain	Chromatin/Epigenetic
	IV-275为BRG1与BRM溴域的抑制剂，能够增强Temozolomide和Bleomycin所诱导的DNA损害。此外，IV-275可抑制GBM（Glioblastoma multiforme）细胞的侵袭性，并增强Temozolomide所诱导的细胞凋亡。
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.
T37151	NVS-CECR2-1 NVS-CECR2-1
	NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 μM by Alpha screen, Kd = 0.80 μM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has n...
T74271	TRIM24/BRPF1-IN-2
	TRIM24/BRPF1-IN-2 (compound 20l) 是一种有效的 TRIM24/BRPF1双重抑制剂，IC50值分别为 0.98 和 1.16 μM。 TRIM24/BRPF1-IN-2 显示出 TRIM24/BRPF1 溴结构域结合亲和力。 TRIM24/BRPF1-IN-2 可用于前列腺癌研究。
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。

化合物

Cat.No: T6828

Target: Epigenetic Reader Domain

Cat.No: T36573

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T60079

Synonym: GNE064

Target: Epigenetic Reader Domain

I-CBP112 hydrochloride

Cat.No: T4247

Target: Epigenetic Reader Domain

Cat.No: T6255

Target: Epigenetic Reader Domain, CDK

Cat.No: T1972

Target: Epigenetic Reader Domain

Cat.No: T1854

Target: Epigenetic Reader Domain

Cat.No: T3973

Target: Epigenetic Reader Domain

Cat.No: T15784

Target: Epigenetic Reader Domain

Cat.No: T2436

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T8658

Synonym: EP31670

Target: Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T3969

Target: Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T6939

Synonym: PFI 3

Target: Epigenetic Reader Domain

Cat.No: T28628

Synonym: RVX297

Target: Epigenetic Reader Domain

PF-CBP1 hydrochloride

Cat.No: T3217

Synonym: PF-CBP1 HCl

Target: Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T9020

Target: Epigenetic Reader Domain

Cat.No: T27071

Cat.No: T69952

Cat.No: T26758

Cat.No: T39461

Cat.No: T69588

Cat.No: T41202

Cat.No: T14512

Target: Epigenetic Reader Domain

Cat.No: T70593

Cat.No: T27068

Synonym: CPI-098,CPI 098

Cat.No: T15419

Target: Epigenetic Reader Domain

Cat.No: T12798

Target: Epigenetic Reader Domain

Cat.No: T39826

Synonym: CBP/p300-IN-8

FKBP12 PROTAC dTAG-7

Cat.No: T11292

Synonym: dTAG-7

Target: Epigenetic Reader Domain

Cat.No: T39073

Cat.No: T63858

Cat.No: T79907

Birabresib dihydrate

Cat.No: T69963

Cat.No: T36574

Synonym: GW841819X

Cat.No: T11441

Target: Epigenetic Reader Domain

FKBP12 PROTAC dTAG-13

Cat.No: T11291

Synonym: dTAG-13

Target: Epigenetic Reader Domain

L Moses dihydrochloride

Cat.No: T36109

Bromodomain inhibitor-9

Cat.No: T63220

Cat.No: T73390

Cat.No: T79642

Target: Epigenetic Reader Domain

Cat.No: T39601

Synonym: GSK973

Cat.No: T37151

Synonym: NVS-CECR2-1

TRIM24/BRPF1-IN-2

Cat.No: T74271

BRD4 Inhibitor-28

Cat.No: T78851

Target: Epigenetic Reader Domain

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