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Cat. No.	Product Name	Target	Signaling Pathways
T4365	FL-411 FL 411,FL411,BRD4-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	FL-411 (BRD4-IN-1) 是一种有效的选择性BRD4抑制剂，对BRD4的IC50为 0.43±0.09 μM。
T63471	PARP1/BRD4-IN-1
	PARP1/BRD4-IN-1 是高度选择性的 PARP1(IC50: 49 nM)和BRD4(IC50: 202 nM)的有效抑制剂。PARP1/BRD4-IN-1 能够抑制 PARP1 和 BRD4 的表达与活性，进而协同抑制胰腺癌细胞的恶性生长。
T64058	PLK1/BRD4-IN-1
	PLK1/BRD4-IN-1 (9b) 是一个口服具有活力的 PLK1 (IC50: 22 nM) 和 BRD4 (IC50: 109 nM) 双重抑制剂。PLK1/BRD4-IN-1 能够诱导细胞凋亡，并使细胞周期阻滞 (cell cycle arrest)，将几种增殖相关癌基因的转录下调，并具有良好的体内抗肿瘤作用。
T79768	HDAC/JAK/BRD4-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	HDAC/JAK/BRD4-IN-1（compound 25ap）是一种针对HDAC/JAK/BRD4的三重抑制剂，该化合物能有效抑制MDA-MB-231细胞增殖，并诱导apoptosis，同时在体内表现出显著的抗癌活性。
T63991	BRD4/CK2-IN-1
	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。
T62030	BRD4-BD1-IN-1
	BRD4-BD1-IN-1 (Compound 9a) 是一种BRD4-BD1抑制剂(IC50= 38.20 μM)。
T64089	BRD4 D1-IN-1
	BRD4 D1-IN-1 是 BRD4 D1 的选择性抑制剂，其 IC50<0.092 μM。BRD4 D1-IN-1 对 BRD4 D1 和 BRD4 D2 具有 18 nM 的亲和力和 500 倍以上的选择性。
T61791	BRD4-BD1/2-IN-1
	BRD4-BD1/2-IN-1 is a highly effective inhibitor of BRD4, specifically targeting the BRD4 BD-1 and BRD4 BD-2 domains with IC 50 values of <100 nM each (US20150148375A1, compound 5) [1].
T10521	ODM-207 BET-IN-4,ODM207	Epigenetic Reader Domain	Chromatin/Epigenetic
	ODM-207 (BET-IN-4) 是一种 BET 溴区结构域蛋白的抑制剂，对 BRD4的 IC50值 ≤ 1 μM。
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。
T19618	(R)-(-)-JQ1 Enantiomer (R)-(-)2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂环庚烷-6-基)乙酸叔丁酯	Epigenetic Reader Domain	Chromatin/Epigenetic
	(R)-(-)-JQ1 Enantiomer 是 (+)-JQ1 的立体异构体。 (+)-JQ1 是一种 BET 溴结构域抑制剂，对BRD4(1/2)的IC50 为 77 和 33 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。
T15405	GNE-781	Epigenetic Reader Domain	Chromatin/Epigenetic
	GNE-781 是一种具有口服活性的选择性 CBP 抑制剂，在 TR-FRET 实验中 IC50为 0.94 nM。它还抑制BRET 和BRD4 (1)，IC50分别为 6.2 和 5100 nM，有抗肿瘤活性。
T9619	I-BET567
	I-BET567 是一种有效、具有口服活性的泛BET 候选抑制剂，对 BRD4 BD1 和 BD2 的pIC50s 分别为 6.9 和 7.2。I-BET567 在肿瘤和炎症的小鼠模型中已被证明有效。
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。
T36242	PROTAC BRD4 Degrader-5 PROTAC BRD4 Degrader-5
	PROTAC BRD4 Degrader-5 is a PROTAC-based BRD4 degrader. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines[1].
T36628	PROTAC BRD4 Degrader-8 PROTAC BRD4 Degrader-8
	PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degra...
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 。
T79167	BET-IN-15	Epigenetic Reader Domain	Chromatin/Epigenetic
	BET-IN-15（化合物1）为一种有效的口服活性BET抑制剂，其对BRD4-BD1及BRD4-BD2的IC50分别为0.64 nM和0.25 nM，具有明显的抗增殖活性。
T75149	PROTAC BRD4 Degrader-19
	PROTACBRD4 Degrader-19 (化合物 176)，一种针对BRD4蛋白的PROTAC，具有可靶向降解BRD4蛋白的特性，主要应用于癌症研究。
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].
T17477	Azido-PEG1-CH2COO-Cl	Others	Others
	Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker, commonly employed in the synthesis of PROTAC BRD4 Degrader-1[1].
T61187	BRD4 Inhibitor-17
	BRD4 Inhibitor-17 (Compound 5i) is a highly potent inhibitor of BRD4, exhibiting an impressive IC50 value of 0.33 μM. It fulfills a crucial regulatory function in transcription by effectively modulating the expression of inflammatory, proliferation, and cell cycle genes. Moreover, BRD4 Inhibitor-17 shows promise as a potential remedy for arsenical-induced toxicity, thus highlighting its potential as an antidote in such cases [1].
T78647	PROTAC BRD4 Degrader-16	PROTACs	PROTAC
	PROTACBRD4Degrader-16是一种高效的PROTAC BRD4降解剂，具有对BRD4(BD1)和BRD4(BD2)分别为34.58 nM及40.23 nM的IC50值。该化合物有效抑制G2/M阶段细胞周期蛋白B1（Cyclin B1）的表达，并显著诱导MV-4-11细胞的细胞凋亡（apoptosis）。
T79818	PROTAC BRD4 Degrader-21	Epigenetic Reader Domain	Chromatin/Epigenetic
	PROTACBRD4 Degrader-21 (Comp 74)为BRD4降解剂，其在小鼠荷瘤异种移植模型中展现出显著抑制肿瘤生长的能力，适用于抗癌研究。
T61327	BRD4 Inhibitor-15
	BRD4 Inhibitor-15 (compound 13) is a highly potent and specific inhibitor of BRD4, effectively inhibiting it with an IC50 of 18 nM. By regulating the Bcl-2/Bax proteins and activating the caspase-3 signaling pathway, BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells. Additionally, it effectively down-regulates the c-Myc level in 22RV1 cells. Due to its properties, BRD4 Inhibitor-15 is a valuable compound for research related to prostate cancer [1].
T74126	PROTAC BRD4 Degrader-14
	PROTACBRD4Degrader-14 是一种由 von Hippel-Lindau 配体和 BRD4配体相连的 PROTAC，对 BRD4BD1和 BD2的 IC50值分别为 1.8 nM 和 1.7 nM。PROTACBRD4Degrader-14 能够有效降解 PC3 前列腺癌细胞中的 BRD4蛋白。
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。
T81386	PROTAC BRD4 Degrader-22	Epigenetic Reader Domain	Chromatin/Epigenetic
	PROTACBRD4Degrader-22 (Compd 44h) 作为BRD4PROTAC降解剂，展现出高效性，其在MOLT4细胞中24小时处理后的pDC50值达到9.2。
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].
T62715	BPTF-IN-1
	BPTF-IN-1 (compound AU1) 是一种选择性 BPTF 溴结构域抑制剂 (Kd: 2.8 μM)，对 BPTF 的选择性比对 BRD4 溴结构域高。BPTF-IN-1 具有出抗疟作用。
T73958	PROTAC BRD4 Degrader-6
	PROTACBRD4Degrader-6 (compound 32a) 是一种有效的小分子 BRD4降解剂,BRD4BD1 的 IC50值为 2.7 nM。PROTACBRD4Degrader-6 能有效降解 BRD4蛋白并抑制 c-Myc 的表达。PROTACBRD4Degrader-6 能抑制胰腺癌细胞系 BxPC3 的增殖并诱导细胞凋亡。PROTACBRD4Degrader-6 可用于人类胰腺癌研究。
T18554	Pomalidomide-PEG1-azide	Others	Others
	Pomalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that combines the cereblon ligand based on Pomalidomide with a linker. This compound is instrumental in designing PROTAC BRD4 Degrader-1[1].
T15397	GNE-049	Epigenetic Reader Domain	Chromatin/Epigenetic
	GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
T69815	SB-284851-BT
	SB-284851-BT 是一种 BRD4/p38α/BRDT 抑制剂。SB-284851-BT 抑制BRD4-BD1(IC50=1.7 µM)、p38α(Kd=0.47 nM)、BRDT(1) (IC50=18 µM) 和BRD4(1) (IC50=3.7 µM)。SB-284851-BT 通过抑制p38α以减少IL-8的产生，抑制BRD4以下调癌症的c-Myc 和NF-κB 基因通路。SB-284851-BT 能与溴结构域和超末端结构域 (BET) 结合。
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.
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。
T74125	PROTAC BRD4 Degrader-12
	PROTACBRD4Degrader-12 (compound 9c) 是一种由 von Hippel-Lindau 配体和 BRD4配体相连的 PROTAC。PROTACBRD4Degrader-12 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4蛋白，DC50值分别为 0.39 nM 和 0.24 nM。
T74270	PROTAC BRD4 Degrader-17
	PROTACBRD4 Degrader-17 (compound 13i)，作为一种高效的 PROTACBRD4 降解剂，其 IC50 值分别为 29.54 nM（针对 BRD4(BD1)）和 3.82 nM（针对 BRD4(BD2)）。该化合物有效抑制 G2/M 相的细胞周期蛋白 B1 (Cyclin B1) 的表达，并在 MV-4-11 细胞中显著诱导细胞凋亡（apoptosis）。
T74124	PROTAC BRD4 Degrader-11
	PROTACBRD4Degrader-11 (compound 9a) 是一种有效的由von Hippel-Lindau 配体和BRD4配体相连的PROTAC。PROTACBRD4Degrader-11 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的BRD4蛋白，DC50值分别为 0.23 nM 和 0.38 nM。
T79168	CBP-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	CBP-IN-1（化合物12）是一种高效CBP抑制剂，其IC50为1.5 nM。此外，该化合物对CBP BRET和BRD4(1)的抑制作用，其IC50分别达到690 nM和3100 nM。
T15399	GNE-207	Epigenetic Reader Domain	Chromatin/Epigenetic
	GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).
T18067	Lenalidomide-PEG1-azide	Others	Others
	Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].
T78933	BD-9136	Epigenetic Reader Domain	Chromatin/Epigenetic
	BD-9136为一高选择性BRD4降解剂，具备抑制小鼠肿瘤生长的能力，且未对小鼠产生不良影响，适用于肿瘤研究领域。
T74823	Bromodomain IN-2
	BD-IN-1 是一种泛溴结构域 (bromodomain (BD)) 抑制剂，对BRD4(1), CBP, BRPF1B,BRD7,BRD9, BRDT(1),CECR2的KD 值分别为 250、420、130、430、67、240、970 nM。BD-IN-1 具有抗增殖活性。
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...
T74380	XY-06-007
	XY-06-007 是一种有效的选择性 B&H-PROTACBRD4BD1L94V 降解剂。XY-06-007 对BRD4BD1L94V 的DC50, 6 h 为 10 nM。XY-06-007 且具有适合的体内药代动力学特征。
T36103	TW9 TW9
	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...
T39634	GSK097
	GSK097 is a highly potent and selective inhibitor of the second bromodomain (BD2) found in bromodomain and extra-terminal domain (BET) proteins. It exhibits a remarkable 2000-fold selectivity for BD2 over BD1, as indicated by BRD4 data. Additionally, GSK097 demonstrates solubility of over 1 mg/mL in FaSSIF media.
T72872	HDAC/BET-IN-1	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	HDAC/BET-IN-1表现出对HDAC1 (IC50= 0.163 μM) 和HDAC6 (IC50= 0.067 μM) 的亚微摩尔级别抑制作用，以及对BRD4 (Ki= 0.076 μM) 的抑制活性，同时也显示出显著的抗白血病活性。

化合物

Cat.No: T4365

Synonym: FL 411,FL411,BRD4-IN-1

Target: Epigenetic Reader Domain

PARP1/BRD4-IN-1

Cat.No: T63471

PLK1/BRD4-IN-1

Cat.No: T64058

HDAC/JAK/BRD4-IN-1

Cat.No: T79768

Target: Epigenetic Reader Domain

BRD4/CK2-IN-1

Cat.No: T63991

BRD4-BD1-IN-1

Cat.No: T62030

Cat.No: T64089

BRD4-BD1/2-IN-1

Cat.No: T61791

Cat.No: T10521

Synonym: BET-IN-4,ODM207

Target: Epigenetic Reader Domain

Cat.No: T6222

Synonym: PF-6405761,PFI 1,PFI1

Target: Apoptosis, Epigenetic Reader Domain, Autophagy

(R)-(-)-JQ1 Enantiomer

Cat.No: T19618

Synonym: (R)-(-)2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂环庚烷-6-基)乙酸叔丁酯

Target: Epigenetic Reader Domain

Cat.No: T10773

Target: Epigenetic Reader Domain, CDK

Cat.No: T15405

Target: Epigenetic Reader Domain

Cat.No: T9619

GSK778 hydrochloride

Cat.No: T9703L

Target: Epigenetic Reader Domain

PROTAC BRD4 Degrader-5

Cat.No: T36242

Synonym: PROTAC BRD4 Degrader-5

PROTAC BRD4 Degrader-8

Cat.No: T36628

Synonym: PROTAC BRD4 Degrader-8

Cat.No: T10522

Target: Epigenetic Reader Domain

Cat.No: T79167

Target: Epigenetic Reader Domain

PROTAC BRD4 Degrader-19

Cat.No: T75149

PROTAC BRD2/BRD4 degrader-1

Cat.No: T18598

Target: Others

Azido-PEG1-CH2COO-Cl

Cat.No: T17477

Target: Others

BRD4 Inhibitor-17

Cat.No: T61187

PROTAC BRD4 Degrader-16

Cat.No: T78647

Target: PROTACs

PROTAC BRD4 Degrader-21

Cat.No: T79818

Target: Epigenetic Reader Domain

BRD4 Inhibitor-15

Cat.No: T61327

PROTAC BRD4 Degrader-14

Cat.No: T74126

Cat.No: T79065

Target: Epigenetic Reader Domain

PROTAC BRD4 Degrader-22

Cat.No: T81386

Target: Epigenetic Reader Domain

Thalidomide-NH-C4-NH2 TFA

Cat.No: T18808

Target: Others

Cat.No: T62715

PROTAC BRD4 Degrader-6

Cat.No: T73958

Pomalidomide-PEG1-azide

Cat.No: T18554

Target: Others

Cat.No: T15397

Target: Epigenetic Reader Domain

Cat.No: T69815

Cat.No: T39826

Synonym: CBP/p300-IN-8

PROTAC BRD3/BRD4-L degrader-2

Cat.No: T78956

Target: Epigenetic Reader Domain

PROTAC BRD4 Degrader-12

Cat.No: T74125

PROTAC BRD4 Degrader-17

Cat.No: T74270

PROTAC BRD4 Degrader-11

Cat.No: T74124

Cat.No: T79168

Target: Epigenetic Reader Domain

Cat.No: T15399

Target: Epigenetic Reader Domain

Lenalidomide-PEG1-azide

Cat.No: T18067

Target: Others

Cat.No: T78933

Target: Epigenetic Reader Domain

Bromodomain IN-2

Cat.No: T74823

Cat.No: T18060

Target: Others

Cat.No: T74380

Cat.No: T36103

Synonym: TW9

Cat.No: T39634

Cat.No: T72872

Target: HDAC

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