Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2072 |
BET bromodomain inhibitor
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BET bromodomain inhibitor 是 BET 的一种有效抑制剂。 | |||
T39998 |
BET bromodomain inhibitor 1
|
||
BET bromodomain inhibitor 1 is an orally active, selective inhibitor of bromodomain and extra-terminal (BET) proteins. It specifically inhibits BRD4 with an IC50 of 2.6 nM. Additionally, BET bromodomain inhibitor 1 demonstrates high affinities towards BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, and 2.1 nM, respectively. This compound exhibits anti-cancer activity. | |||
T2120 |
I-BET151
GSK1210151A |
Epigenetic Reader Domain | Chromatin/Epigenetic |
I-BET151 (GSK1210151A) 是 BRD2/3/4 的特异性 BET 抑制剂,IC50值分别为0.5、0.25、0.79 μM。 | |||
T6859 |
I-BRD9
GSK602 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
I-BRD9 (GSK602) 是一种选择性的 BRD9 细胞抑制剂,pIC50 为 7.3。 | |||
T79084 |
BET bromodomain inhibitor 3
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BET bromodomain inhibitor 3为BET溴区结构域抑制剂,对BrdT抑制作用显示Ki值高于40 µM,适用于避孕、癌症和心脏病相关研究。 | |||
T62655 |
BET bromodomain inhibitor 2
|
||
BET bromodomain inhibitor 2 是一种 BET 型溴化域的有效抑制剂 (IC50: 14.1 μM)。 | |||
T6026 |
CPI-203
CPI 203,CPI203 |
Apoptosis; Epigenetic Reader Domain | Apoptosis; Chromatin/Epigenetic |
CPI-203 是一种选择性的,细胞通透的 BET 溴结构域抑制剂,抑制 BRD4,IC50值约为 37 nM。 | |||
T8495 |
Alobresib
Vorolanib,GS-5829 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
Alobresib (Vorolanib) 是一种BET 溴结构域抑制剂,是一种抗肿瘤候选药物。 | |||
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。 | |||
T5362 |
Y06036
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
Y06036 是一种选择性 BET 抑制剂,具有抗肿瘤活性,可与 BRD4(1)溴结构域结合,Kd 值为 82 nM。 | |||
T6032 |
Birabresib
OTX-015,OTX015 (MK 8628/Birabresib),MK-8628 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
Birabresib (MK-8628) 是一种 BRD2/3/4抑制剂,IC50值为 92 到 112 nM 之间,具有潜在的抗肿瘤活性。 | |||
T2442 |
CPI203
CPI 203,CPI-203 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
CPI203 (CPI 203) 是一种有效的 BET 溴结构域抑制剂(BRD4 的 IC50:37 nM)。 | |||
T12338 |
OXFBD04
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
OXFBD04 是有效的、选择性的 BRD4 抑制剂(IC50= 166 nM)。OXFBD04 是有效的 BET 溴结构域配体,具有对 CREBBP 溴结构域额外的适度亲和力。OXFBD04 显示出抗癌活性。 | |||
T2480 |
Apabetalone
RVX-208,RVX000222,阿帕他隆 |
Epigenetic Reader Domain; HIV Protease | Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome |
Apabetalone (RVX000222) 是一种 BET 溴结构域抑制剂,用于研究治疗糖尿病、动脉粥样硬化和冠状动脉疾病。 | |||
T4697 |
ABBV-744
ABBV744 |
Epigenetic Reader Domain; HIV Protease | Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome |
ABBV-744 是一种 BDII 选择性 BET 溴结构域抑制剂,可抑制 BRD2/3/4。 它可研究炎症性疾病、癌症和艾滋病。 | |||
T17311 |
(+)-JQ1 PA
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
(+)-JQ1 PA 是一种溴结构域和末端外 (BET) 抑制剂 JQ1 的衍生物,IC50 为 10.4 nM。 | |||
T3504 |
AZD5153 6-Hydroxy-2-naphthoic acid
AZD5153,AZD5153结晶体(API形式),AZD-5153 HNT salt |
Epigenetic Reader Domain | Chromatin/Epigenetic |
AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) 是 AZD5153的6-羟基-2-萘甲酸盐形式。AZD5153是一种有口服活性的选择性 BET/BRD4溴结构域抑制剂,对BRD4的IC50值为1.7nM。 | |||
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。 | |||
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。 | |||
T19935 |
XD14
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
XD14 是BET 抑制剂,其与 BRD2、BRD3 和 BRD4 的结合常数分别为 170 nM、380 nM 和 160 nM。它具有抗肿瘤活性。 | |||
T13363 |
Y06137
|
Epigenetic Reader Domain; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
Y06137 是一种有效的特异性 BET 抑制剂,对 BRD4(1) 溴结构域的 Kd 为 81 nM。 Y06137可用于去势抵抗性前列腺癌治疗的研究。 | |||
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。 | |||
T3712 |
Mivebresib
ABBV-075,米维布塞 |
Apoptosis; Epigenetic Reader Domain | Apoptosis; Chromatin/Epigenetic |
Mivebresib (ABBV-075) 是一种有效的,口服活性的溴结构域和末端结构域 (BET) 抑制剂,结合BRD4的Ki 值是 1.5 nM。 | |||
T27392 |
FT001
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
FT001是一种有效的、选择性的和具有口服活性的 BET Bromodomain 抑制剂,具有抗肿瘤活性。FT001抑制 MYC 的表达,IC50为0.46 μM。FT001对 MV-4-11具有有效的抗增殖作用,并在体外和体内显著抑制 MYC mRNA 水平。 | |||
T8932 |
GSK046
iBET-BD2 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
GSK046 (iBET-BD2) 是一种选择性和具有口服活性的 BET 蛋白 BD2溴结构域的抑制剂,对 BRD2 BD2、BRD3 BD2、BRD4 BD2 和 BRDT BD2的 IC50值为 264、98、49 和 214 nM,具有免疫调节活性。 | |||
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。 | |||
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。 | |||
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。 | |||
T12660L |
BAY1238097
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BAY1238097 是一种具有有效性和选择性的溴结构域和末端外基序(BET)抑制剂,具有抗癌活性,在AML (急性髓性白血病) 和MM (多发性骨髓瘤) 模型中表现出较强的抗增殖活性 。BAY1238097 可用于研究晚期难治性恶性肿瘤。 | |||
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。 | |||
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。 | |||
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。 | |||
T22845 |
I-BET151 dihydrochloride
I-BET 151 hydrochloride |
Others | Others |
I-BET 151 dihydrochloride is a BET bromodomain inhibitor that prevents BET from recruiting to chromatin. | |||
T10720 |
CD235
|
Others | Others |
CD235 is a structurally similar analog of CD161. CD161 is an orally bioavailable inhibitor of BET bromodomain. | |||
T10621 | Bromodomain inhibitor-8 | Others | Others |
Bromodomain inhibitor-8 is an inhibitor of BET bromodomain used to treat autoimmune and inflammatory diseases. | |||
T26780 | BETi-211 | ||
BETi-211 is a selective inhibitor BET bromodomain. | |||
T62055 | NVS-BET-1 | ||
NVS-BET-1 是 BET 溴结构域抑制剂。NVS-BET-1可以调节角质形成细胞可塑性。 | |||
T12558 | PROTAC BET-binding moiety 2 | Others | Others |
PROTAC BET-binding moiety 2 is an BET bromodomain inhibitor. | |||
T11472L |
Molibresib besylate
I-BET 762 besylate,GSK 525762C |
CCR | Immunology/Inflammation; Microbiology/Virology |
Molibresib besylate is an inhibitor of BET bromodomain (IC50: 32.5-42.5 nM). | |||
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. | |||
T10517 |
BET-BAY 002 (S enantiomer)
|
Others | Others |
BET-BAY 002 S enantiomer为BET-BAY 002的S型对映异构体,属于BET小分子抑制剂。 | |||
T27469 |
GSK2820151
GSK-2820151,GSK 2820151 |
||
GSK2820151 is an orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential antineoplastic activity. | |||
T15627 |
(S)-JQ-35
TEN-010 |
Others | Others |
(S)-JQ-35 (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins. It has a potential antineoplastic activity. | |||
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 | |||
T28630 |
RX-37
RX37 |
||
RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell | |||
T62024 | GSK852 | ||
GSK852 是有效的 BD2 选择性 BET 抑制剂,pIC50为 7.9。 | |||
T14549 | BETd-246 | Others | Others |
BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity. | |||
T70702 |
JQ1-Acid HCl
|
||
(+)-JQ-1 carboxylic acid is a potent bromodomain and extra terminal domain (BET) inhibitor. (+)-JQ-1 carboxylic has potential to be used as a precursor to synthesize PROTACs and other conjugates. | |||
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. |