Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13833 |
PROTAC BRD4 Degrader-1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM). | |||
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]. | |||
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. | |||
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。 | |||
T14408 |
Azido-PEG1-CH2CO2H
4-哌啶酮缩乙二醇 |
Others; PROTAC Linker | Others; PROTAC |
Azido-PEG1-CH2CO2H 是属于 alkyl/ether 类的PROTAC linker,可用于合成 PROTAC BRD4 Degrader-1. | |||
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。 | |||
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]. | |||
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... | |||
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]. | |||
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。 | |||
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。 | |||
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 。 | |||
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。 | |||
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)。 | |||
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]. | |||
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。 | |||
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]. | |||
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。 | |||
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。 | |||
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]. | |||
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。 | |||
T82053 | IR808-TZ | PROTACs | PROTAC |
IR808-TZ,作为一种BRD4BT-PROTAC降解剂,表现出高效性能。该化合物展现了在设计针对不同蛋白的BT-PROTAC方面的应用潜力。 | |||
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。 | |||
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。 | |||
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)。 | |||
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。 | |||
T74380 |
XY-06-007
|
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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。 |