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Cat. No. | Product Name | Form | Specificity Of Inhibition |
---|---|---|---|
CL0072 |
BET inhibitor kit
BET inhibitor kit |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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. | |||
T64117 |
BRD4-BD1-IN-2
|
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。 | |||
T73296 |
iBRD4-BD1
|
||
iBRD4-BD1 是选择性 BRD4溴结构域抑制剂。iBRD4-BD1 对 BRD4溴结构域具有抑制活性,IC50值为 12 nM。iBRD4-BD1 可用于炎症和肿瘤学的研究。 | |||
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。 | |||
T60072 |
ZL0590
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
ZL0590 是一种有效的特异性 BD1-BRD4 抑制剂 (IC50 = 90 nM),具有抗炎活性。 | |||
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]. | |||
T62030 |
BRD4-BD1-IN-1
|
||
BRD4-BD1-IN-1 (Compound 9a) 是一种BRD4-BD1抑制剂(IC50= 38.20 μM)。 | |||
T63707 |
BRD4-BD1/2-IN-2
|
||
BRD4-BD1/2-IN-2 是 BRD4-BD2 的有效抑制剂,能够作用于 BRD4 BD2 (IC50<0.5 nM) 和 BRD4 BD1 (IC50<300 nM)。 | |||
T7488 |
BD1063 dhydrochloride
BD1063 |
Sigma receptor | GPCR/G Protein |
BD1063 dhydrochloride 是有效选择性的 sigma 1受体拮抗剂。 | |||
TP2162 |
D-JBD19
|
Others | Others |
D-JBD19 is a non-permeable peptide with neuroprotective effects. | |||
T82541 |
D-JBD19 TFA
|
||
D-JBD19 TFA为一种不可渗透性多肽,具备神经保护功能。 | |||
TP2162L |
D-JBD19 TFA (954134-42-0 free base)
D-JBD19 TFA |
Others | Others |
D-JBD19 TFA is a non-permeable peptide with neuroprotective effects. | |||
T62603 |
NVP-BBD130
|
||
NVP-BBD130 是一种稳定的、ATP 竞争性的、有效的、口服具有活力的 PI3K 和 mTOR 抑制剂。 | |||
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。 | |||
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。 | |||
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。 | |||
T14776 |
BRD4 Inhibitor-10
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4 Inhibitor-10 是一种BRD4-BD1抑制剂,IC50为 8 nM。 | |||
T13392 |
ZEN-3219
|
Others; Epigenetic Reader Domain | Chromatin/Epigenetic; Others |
ZEN-3219 是一种 BET 抑制剂,对 BRD4(BD1),BRD4(BD2) 和 BRD4(BD1BD2)既有抑制作用,ZEN-3219对 BRD4(BD1),BRD4(BD2) 和 BRD4(BD1BD2)的 IC50 分别为 0.48, 0.16 和 0.47 μM。ZEN-3219 是 PROTAC 分子的组成部分,可诱导 BRD4 降解。。 | |||
T70375 |
ZEN-2759
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
ZEN-2759 是一种有效的 BET 小分子抑制剂,对 BRD4(BD1)、BRD4(BD2) 和 BRD4(BD1BD2) 有抑制作用。 | |||
T13394 |
ZEN-3862
ZEN3862,ZEN 3862 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
ZEN-3862 (Willardiine) 是一种 BET 抑制剂,抑制 BRD4(BD1) 和 BRD4(BD2) 的 IC50 分别为 0.16 和 0.13 μM。ZEN-3862 可用于合成 PROTAC 分子,从而诱导 BRD4 降解。 | |||
T13393 |
ZEN-3411
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
ZEN-3411 是一种可口服且具有高效性的 BET 抑制剂,抑制 BRD4(BD1),BRD4(BD2) 和BRD4(BD1BD2),抑制过度产生 BET 蛋白的肿瘤细胞的生长。 | |||
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。 | |||
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。 | |||
T78555 |
BRD4 Inhibitor-27
|
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。 | |||
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。 | |||
T16154 |
MS417
GTPL7512 |
Epigenetic Reader Domain; HIV Protease | Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome |
MS417 (GTPL7512) 是一种 BET 特异性 BRD4 抑制剂,与 BRD4-BD1 和 BRD4-BD2 结合,Kd 值分别为 36.1和25.4 nM,IC50值分别为 30和46 nM。它对 CBP BRD 的选择性较低,IC50值为 32.7 μM。 | |||
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。 | |||
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。 | |||
T5434 |
ARV-825
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
ARV-825 是一种双功能 PROTAC,蛋白水解靶向嵌合体,将 BRD4 募集到 E3 泛素连接酶大脑中,导致 BRD4 在所有测试的 BL 细胞系中快速、有效和延长降解。对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd 值分别为 90 和 28 nM。 | |||
T10520 |
BET-IN-2
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BET-IN-2 is a BET inhibitor (IC50: 52 nM for BRD4-BD1). | |||
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。 | |||
T5436 |
MZ 1
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
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。 | |||
T14910 |
CD161
NKR-P1A |
Others | Others |
CD161 is a potent, selective, and orally bioavailable BET bromodomain inhibitor (IC50s: 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2) with good anticancer activity. | |||
T13833 |
PROTAC BRD4 Degrader-1
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM). | |||
T11887 |
LT052
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
LT052 是一种高活性和选择性BET BD1抑制剂,其IC50为 87.7 nM。LT052 表现出纳摩尔级别的 BRD4 BD1 的抑制活性,选择性是 BRD4 BD2 的 138 倍 (IC50=12.130 μM)。LT052 具有抗炎活性,可用于治疗急性痛风性关节炎。 | |||
T12113 |
MS645
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
MS645 是一种含溴结构域蛋白 4 (BRD4) 的抑制剂,对 BRD4-BD1/BD2 的 Ki 值为 18.4 nM。 | |||
T16701 |
QCA570
|
Others; PROTACs | Others; PROTAC |
QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein). | |||
T17294 |
ZL0454
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
ZL0454 is an effective and selective Bromodomain-containing protein 4 inhibitors (IC50: 49 and 32 nM for BD1 and BD2). | |||
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)。 | |||
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。 | |||
T15443 |
GSK8814
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
GSK8814 is a selective and ATAD2/2B bromodomain chemical probe and inhibitor (binding constant pKd=8.1 and a pKi=8.9 in BROMOscan). GSK8814 displays 500-fold selectivity for ATAD2 over BRD4 BD1. GSK8814 binds to ATAD2 and BRD4 BD1 (pIC50s: 7.3 and 4.6). | |||
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。 | |||
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). | |||
T5440 |
Dbet57
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
dBET57 是基于 PROTAC 技术的 BRD4 异双功能降解剂,对 BRD4BD1 有显著降解作用,DC50/5h 为 500 nM。 | |||
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。 | |||
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). | |||
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). | |||
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。 | |||
T63302 |
BRD4 Inhibitor-19
|
||
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。 | |||
T69588 |
GSK789
|
||
GSK789 is a selective inhibitor of the first bromodomains (BD1) of the bromo and extra terminal domain (BET) proteins. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-04170 |
DEFB1 Protein, Human, Recombinant (hFc)
DEFB101,defensin, β1,β Defensin <... |
Human | HEK293 Cells |
The DEFB1 gene, encoding for the constitutively expressed human beta-defensin 1 (hBD1) antimicrobial peptide is a potential candidate when studying genetic susceptibility to caries. DEFB1 genetic variations have been reported as contributing to hBD1 production impairment, leading to a greater susceptibility to be infected by oral pathogens, also leading to periodontitis. To counteract host immunity, Cryptosporidium parvum has evolved multiple strategies to suppress host antimicrobial defense. On... | |||
TMPJ-00003 |
DEFB1 Protein, Human, Recombinant
Beta-Defensin 1,BD-1,HBD... |
Human | E. coli |
β-Defensin 1 (DEFB1) is a member of the β-defensin family, which is highly expressed by epithelial cells. β-defensins are expressed as the C-terminal portion of precursors and are released by proteolytic cleavage of a signal peptide. β-defensins contain a six-cysteine motif that forms three intra-molecular disulfide bonds. β-defensin 1 is an antimicrobial peptide implicated in the resistance of epithelial surfaces to microbial colonization. Defects in β-Defensin-1 contribute to asthma diagnosis,... |