Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T13915L |
PROTAC BRD9-binding moiety 1 hydrochloride
PROTAC BRD9-binding moiety 1 hydrochloride (2097512-23-5 free base) |
Others | Others |
PROTAC BRD9-binding moiety 1 hydrochloride binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC. | |||
T12560 |
PROTAC BRD9 Degrader-1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM. | |||
T13915 |
PROTAC BRD9-binding moiety 1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC. | |||
T82821 | BRD9 Degrader-1 | Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD9Degrader-1为一种BRD9降解剂,表现出对BRD9微摩尔级的结合亲和力,并对BRD9与VCB形成的三元复合体具有纳摩尔级别的亲和力。 | |||
T81385 |
PROTAC BRD9 Degrader-2
|
PROTACs | PROTAC |
PROTACBRD9 Degrader-2是针对癌症研究的BRD9双功能性降解剂。 | |||
T77936 |
PROTAC BRD9 Degrader-4
|
PROTACs | PROTAC |
PROTACBRD9 Degrader-4 是一种针对BRD9的双功能降解剂,用于癌症研究。 | |||
T81383 |
PROTAC BRD9 Degrader-5
|
PROTACs | PROTAC |
PROTACBRD9 Degrader-5为针对BRD9的专一性靶向降解PROTAC,具备选择性地介导BRD9蛋白的降解能力。 | |||
T81382 | PROTAC BRD9 Degrader-7 | PROTACs | PROTAC |
PROTACBRD9Degrader-7 是具有口服活性的BRD9选择性降解剂,DC50 值为 1.02 nM,表现出较好的口服生物利用度,其Cmax 达到 3436.95 ng/mL。 | |||
T81384 |
PROTAC BRD9 Degrader-3
|
PROTACs | PROTAC |
PROTACBRD9 Degrader-3为BRD9靶向的双功能降解剂,用于癌症研究。 | |||
T77975 |
PROTAC BRD9 Degrader-6
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTACBRD9Degrader-6,作为BRD9降解剂,表现出高效率(IC50=0.13 nM),主要应用于BAF复合物相关疾病的研究领域。 | |||
T15441 |
GSK8573
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
GSK8573 是 GSK2801 的非活性对照化合物。它与BRD9具有结合活性,Kd 值为 1.04 μM。 | |||
T74256 | PROTAC BRD9-binding moiety 5 | ||
PROTACBRD9-binding moiety 5 是一种选择性 BRD9结合剂,IC50为 4.20 μM,可用于合成 PROTACs。PROTACBRD9-binding moiety 5 对癌细胞具有抗增殖活性。 | |||
T31221L |
dBRD9 HCl
dBRD9 HCl(2170679-45-3 Free base) |
Epigenetic Reader Domain | Chromatin/Epigenetic |
dBRD9 HCl 是一种PROTAC,包含cereblon E3连接酶配体与BRD9抑制剂BI 7273。dBRD9 HCl 是有效和选择性的BRD9降解剂,在MOLM-13细胞中IC50的为56.6nM。dBRD9 HCl 在浓度高达5μM 时不会降解BRD4或BRD7。dBRD9 HCl 在人AML 细胞系中显示出抗增殖作用。 | |||
T31221 |
dBRD9
dBRD-9,dBRD 9 |
PROTACs | PROTAC |
dBRD9是一种 PROTAC。dBRD9是一种双重作用的分子,一部分连接 Bromodomain-containing protein 9 (BRD9)的溴域,另一部分招募小脑 E3泛素连接酶的配体(ligand that recruits the cereblon E3 ubiquitin ligase)。dBRD9对 MOLM-13细胞中 BRD9具有抑制作用,可使其降解,IC50为104 nM。 | |||
T8342 |
BRD9876
6-叔丁基-2,3-二氰基萘 |
Others; Kinesin; Microtubule Associated | Cytoskeletal Signaling; Others |
BRD9876 是一种 MM1S 生长的选择性抑制剂,可将驱动蛋白 5 锁定在增强微管结合的状态,从而导致 MT 的捆绑和稳定。它特异性靶向微管结合的 Eg5,选择性抑制 CD34 细胞的骨髓瘤,有用于多发性骨髓瘤的研究潜力。 | |||
T7378 |
BRD9539
|
Histone Methyltransferase | Chromatin/Epigenetic |
BRD9539 是一种组蛋白甲基转移酶G9a 抑制剂,IC50为 6.3 μM,还抑制PRC2活性。 | |||
T35480 |
dBRD9-A
dBRD9-A |
||
Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model. | |||
T30584 |
BRD9092
BRD 9092,BRD-9092 |
||
BRD9092 is an enhancer of reactive oxygen species that are nontoxic or cause genotype-selective cell death. | |||
T14780 | BRD9185 | Dehydrogenase | Metabolism |
BRD9185 is an inhibitor of Dihydroorotate dehydrogenase (DHODH) with an EC50 of 16 nM against multidrug-resistant blood-stage parasites in vitro. | |||
T60603 |
BRD9500
|
||
BRD9500 是一种具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂,对PDE3A 和PDE3B 的IC50分别为 10 和 27 nM。BRD9500 在黑色素瘤细胞系 SK-MEL-3 癌症异种移植模型中具有活性。 | |||
T27423 |
GNE-375
GNE375,GNE 375 |
Epigenetic Reader Domain; Carboxypeptidase; CDK | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Proteases/Proteasome |
GNE-375 是一种具有选择性和高效性的 BRD9 抑制剂,(IC50:5 nM)。GNE-375 抑制 BRD4、TAF1 和 CECR2,可用于研究表观遗传学耐药性。 | |||
T15784 |
LP99
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
LP99 是一种表观遗传探针,可破坏 BRD7 和 BRD9 与细胞中染色质的结合。它是一种选择性的 BRD7 和 BRD9 溴结构域抑制剂,对 BRD9 的 Kd 为 99 nM。 | |||
T6786 |
BI-9564
BI 9564,BI9564 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
BI-9564 是一种选择性的且可透过细胞的 BRD9/BRD7溴结构域抑制剂,IC50分别为 75 和 3.4 μM,Kd 为 14 和 239 nM。它对 BET 家族的 IC50值大于 100 μM。 | |||
T6783 |
BI-7273
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BI7273 是一种选择性的可细胞透过BRD9抑制剂,IC50和Kd 分别为 19 和 0.75 nM。它对 BRD7 的作用较强,IC50和Kd 值分别为 117 和 0.3 nM。 | |||
T73425 |
CFT8634
|
||
CFT8634 是一种靶向 BRD9的降解剂,可用于滑膜肉瘤和 SMARCB1 缺失实体瘤的研究。 | |||
T13190 |
TP-472
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
TP-472 is a selective inhibitor of BRD9 (Kd: 33 nM). | |||
T78660 | (S,R)-CFT8634 | Epigenetic Reader Domain | Chromatin/Epigenetic |
(S,R)-CFT8634为选择性与口服活性BRD9蛋白降解剂,潜在用途覆盖BRD9介导疾病研究,包含细胞增殖异常等。 | |||
T77680 |
BRD7-IN-3
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD7-IN-3 (compound 1-78) 作为BRD7/BRD9的双抑制剂,其IC50s分别是1.6 μM和2.7 μM。 | |||
T79889 |
DBr-1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
DBr-1为一高效BRD9降解剂。 | |||
T41202 | TP 472N | ||
TP 472N is a negative control forTP 472. Inactive against other bromodomains (>20μM against BRD9). | |||
T82603 | DCAF1 binder 2 | ||
DCAF1 binder 2 是 E3 Ligase 的配体,涉及 BRD9、激酶和选择性 BTK 降解。 | |||
T39524 |
Thalidomide-NH-PEG2-C2-NH-Boc
Thalidomide-NH-PEG2-C2-NH-Boc |
||
Thalidomide-NH-PEG2-C2-NH-Boc, a synthesized E3 ligase ligand-linker conjugate, combines the cereblon-targeting Thalidomide ligand with a PEG linker for the synthesis of dBRD9 (compound 6). This selective BRD9 probe PROTAC degrader is utilized in researching BAF complex biology. | |||
T40055 | TP-238 hydrochloride | ||
TP-238 hydrochloride is a highly potent and selective dual CECR2/BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases. | |||
T78801 |
BRD7-IN-2
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD7-IN-2(化合物2-77)是针对前列腺癌细胞的有效BRD7抑制剂,具有对BRD7的选择性但不选择性抑制BRD9,IC50分别为5.4 μM和>300 μM。 | |||
T74919 | QA-68 | ||
QA-68 (QA-68-ZU81) 为一种高效BRD9降解剂。该化合物抑制细胞周期进展与细胞集落生成,对急性髓系白血病(AML)细胞系展现出抗增殖能力。 | |||
T34907 |
TP-238
TP 238 |
||
TP-238 是一种有效的,选择性的CECR2/BPTF 双重探针,IC50值分别为 30 nM 和 350 nM。TP-238 还抑制BRD9,pIC50为 5.9,并且对其他 338 激酶的活性较低。 | |||
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。 | |||
T75135 | FHD-609 | ||
FHD-609 为含溴结构域蛋白BRD9的抑制剂及降解剂,针对ncBAF,适用于研究含BAF复合亚基突变的多种癌症。FHD-609与Telomelysin或INO5401联用,或对肾上腺皮质癌(ACC)的研究具有潜在作用。 | |||
T6255 |
Bromosporine
|
Epigenetic Reader Domain; CDK | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Bromosporine 是广谱 BRD2/4/9 和 CECR2 溴结构域抑制剂,IC50为0.41、0.29、0.122和0.017 μM。 | |||
T16321 |
NI-42
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
NI-42 是一种用于 BRPF 的结构正交化学探针,是有偏向性的BRPFs 溴结构域 (BRD)抑制剂,BRPF1、2和3的IC50为7.9、48和260 nM; BRPF1、2和3的Kd 值为40、210和940 nM,与非分类 IV BRD 蛋白相比具有很好的选择性。 | |||
T17249 |
VZ185
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
VZ185 is an effective and selective dual BRD7/9 PROTAC degrader (DC50s: 4.5 and 1.8 nM, respectively). | |||
T37151 |
NVS-CECR2-1
NVS-CECR2-1 |
||
NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 μM by Alpha screen, Kd = 0.80 μM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has n... |