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Cat. No. | Product Name | Target | Signaling Pathways |
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T14776 |
BRD4 Inhibitor-10
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4 Inhibitor-10 是一种BRD4-BD1抑制剂,IC50为 8 nM。 | |||
T78555 |
BRD4 Inhibitor-27
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4 Inhibitor-27 是一种有效的 BRD4 抑制剂,对 BRD4 BD1 和 BRD4 BD2 具有抑制作用, IC50 分别为 9.6 和 11.3 μM。BRD4 Inhibitor-27 具有抗癌活性,可用于研究乳腺癌。 | |||
T12551 |
PROTAC BRD4 ligand-1
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Epigenetic Reader Domain; Ligands for Target Protein for PROTAC | Chromatin/Epigenetic; PROTAC |
PROTAC BRD4 ligand-1 是 PROTAC GNE-987 靶向 BRD4 蛋白的配体,也是一种 BET 的抑制剂。 | |||
T9629 |
BRD4 Inhibitor-24
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4 Inhibitor-24 是一种具有抗肿瘤活性的 BRD4 小分子抑制剂。 | |||
T77339 |
BRD4-IN-4
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4-IN-4 是一种具有选择性的 BRD4 抑制剂 ,对 BRD4 的IC50值为 6.83 μM。BRD4-IN-4 选择性抑制 MV4-11 细胞系增殖并将细胞阻滞在 G1 期。BRD4-IN-4可用于研究 MLL 白血病。 | |||
T40072 |
PROTAC BRD4 Degrader-9
PROTAC BRD4 Degrader-9 |
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PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound consisting of ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound can effectively degrade the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM. | |||
T36628 |
PROTAC BRD4 Degrader-8
PROTAC BRD4 Degrader-8 |
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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... | |||
T39628 |
PROTAC BRD4 ligand-2
PROTAC BRD4 ligand-2 |
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PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718. | |||
T40075 |
PROTAC BRD4 Degrader-13
PROTAC BRD4 Degrader-13 |
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PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound that functions as a proteolysis targeting chimera (PROTAC), linking ligands for von Hippel-Lindau and BRD4 proteins. In the context of PC3 prostate cancer cells, this compound effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies. The degradation of BRD4 protein is achieved with remarkable potency, exhibiting a DC 50 of 0.025 nM and 6.0 nM when combined with STEAP1 and CLL1 antibodies, respectively. | |||
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。 | |||
T40305 |
BRD4-IN-2
BRD4-IN-2 |
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BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC 50 value of 9.9 nM. | |||
T40074 |
PROTAC BRD4 Degrader-15
PROTAC BRD4 Degrader-15 |
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PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2. Additionally, PROTAC BRD4 Degrader-15 demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells. | |||
T36242 |
PROTAC BRD4 Degrader-5
PROTAC BRD4 Degrader-5 |
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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]. | |||
T40073 |
PROTAC BRD4 Degrader-10
PROTAC BRD4 Degrader-10 |
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PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM. | |||
T30580 |
BRD4-Kinases-IN-3
BRD4 kinases inhibitor 3,BRD4-Kinases inhibitor-3 |
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BRD4-Kinases-IN-3 is a dual BRD4-Kinases inhibitor that can be used as a value-added multi-targeted chemical probe for cancer therapy. | |||
T61318 |
BRD4 Inhibitor-20
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4 Inhibitor-20是一种有效的溴结构域蛋白4(BRD4)抑制剂,具有口服活性。BRD4 Inhibitor-20在癌细胞系中具有抗增殖活性,并被用于各种癌症的研究,如结肠癌。 | |||
T39629 |
BRD4 ligand-Linker Conjugate 1
BRD4 ligand-Linker Conjugate 1 |
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BRD4 Ligand-Linker Conjugate 1 is a compound consisting of a ligand and a linker, specifically designed to bind to the target protein BRD4. This conjugate serves as a valuable tool for synthesizing PROTACs, molecules utilized for targeted protein degradation. | |||
T5439 |
BRD4 degrader AT1
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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。 | |||
T13833 |
PROTAC BRD4 Degrader-1
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Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM). | |||
T64117 |
BRD4-BD1-IN-2
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4-BD1-IN-2 是一种具有选择性和有效性的 BRD4-BD1 抑制剂,IC50 值为 2.51 µM ,是对 BRD4-BD2 抑制活性的 20 倍。BRD4-BD1-IN-2 可用于研究心血管疾病和癌症相关疾病。 | |||
T13834 | PROTAC BRD4 Degrader-2 | Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM). | |||
T13835 |
PROTAC BRD4 Degrader-3
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Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4. | |||
T18598 |
PROTAC BRD2/BRD4 degrader-1
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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]. | |||
T18603 | PROTAC BRD4 degrader for PAC-1 | Others | Others |
PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1. | |||
T18599 |
PROTAC BRD4-binding moiety 1
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Others | Others |
PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand through a linker, enabling the formation of a PROTAC complex. This complex efficiently degrades BRD4[1]. | |||
T18601 |
Desmethyl-QCA276
PROTAC BRD4-binding moiety 4 |
Others | Others |
Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1]. | |||
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。 | |||
T28004 |
MDK8228
PF-CBP/BRD4,MDK-8228,MDK 8228 |
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MDK8228 is an inhibitor of CBP/p300 and BRD4 bromodomain. MDK8228 downregulates IL-6, IL-ß and IFN-ß in macrophages. | |||
T63352 |
BRD4 Inhibitor-18
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BRD4 Inhibitor-18 是一种高效的、具有疏水乙酰环戊基侧链的 BRD4 抑制剂 (IC50: 110 nM)。BRD4 Inhibitor-18 可以明显降低 BRD4 水平较高的 MV-4-11 细胞的增殖,抑制 G0/G1 周期的活性,并促使细胞凋亡 (apoptosis)。 | |||
T73830 | BRD4 Inhibitor-16 | ||
BRD4Inhibitor-16 (Compound 4) 是溴域 4 (BRD4) 的有效抑制剂。 溴结构域 4 (BRD4) 的过表达通过调节组蛋白翻译后修饰与多种人类癌症密切相关。BRD4Inhibitor-16 是探索性研究 BRD4抑制的有用工具,例如更好地了解 BRD4抑制剂释放相关信息。 | |||
T61327 |
BRD4 Inhibitor-15
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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]. | |||
T62883 | BRD4 Inhibitor-23 | ||
BRD4 Inhibitor-23 是一种有效的、口服具有活力的 BRD4 抑制剂,作用于 BRD4 BD-1 (IC50: 6.21 nM) 和 BRD4 BD-2 (IC50: 1.44 nM)。 | |||
T63302 |
BRD4 Inhibitor-19
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BRD4 inhibitors -19 是 BET 抑制剂,能够作用于 BRD4-BD1 (IC50: 55 nM),能够用于研究多发性骨髓瘤。 | |||
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]. | |||
T72630 | BRD4 Inhibitor-25 | ||
BRD4Inhibitor-25 是一种BRD4抑制剂,对BRD4的BD1和BD2结构域的IC50为 0.82 μM,1.94 μM。BRD4Inhibitor-25 在卵巢癌细胞中诱导凋亡和自噬细胞死亡。BRD4Inhibitor-25 可用于癌症、心血管、神经肌肉和炎症性疾病的研究。 | |||
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。 | |||
T72636 | BRD4 Inhibitor-26 | ||
BRD4Inhibitor-26 是一种溴结构域蛋白 4(BRD4)抑制剂/一氧化氮供体。BRD4Inhibitor-26 抑制BRD4(BD1) 和BRD4(BD2),IC50值分别为 0.82 μM 和 1.94 μM。BRD4Inhibitor-26 可用于卵巢癌的研究。 | |||
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。 | |||
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。 | |||
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
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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)。 | |||
T78647 |
PROTAC BRD4 Degrader-16
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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)。 | |||
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。 | |||
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。 | |||
T73958 |
PROTAC BRD4 Degrader-6
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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。 | |||
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。 | |||
T74090 |
PROTAC BRD4 Degrader-7
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PROTACBRD4Degrader-7 是一种有效的溴结构域BRD4降解剂,对 BRD4-BD1 和 BRD4-BD2 的IC50分别为 15.5 和 12.3 nM。 | |||
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。 | |||
T79818 |
PROTAC BRD4 Degrader-21
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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。 | |||
T13086 |
I-BET762 carboxylic acid
Molibresib carboxylic acid,PROTAC BRD4-binding moiety 2,GSK525762A carboxylic acid |
Epigenetic Reader Domain | Chromatin/Epigenetic |
I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1). |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN1973 |
Naringenin triacetate
三乙酸柚皮素酯 |
Others | Others |
Naringenin triacetate exhibits a better binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) when compared with the known inhibitors. |