Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T79527 |
BET BD2-IN-1
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BET BD2-IN-1(compound 45)为BETBD2选择性抑制剂,IC50值为1.6 nM,通过抑制STAT3与NF-κB活性,阻断Th17细胞的分化,适用于银屑病与炎症性肠病研究。 | |||
T9619 |
I-BET567
|
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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。 | |||
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。 | |||
T79610 |
BET-IN-17
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BET-IN-17(化合物16)作为BET家族的泛抑制剂,具有针对BETBD1和BETBD2的pIC50值,分别为7.8与7.6。 | |||
T39634 |
GSK097
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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. | |||
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。 | |||
T79018 |
GSK217
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
GSK217为一种针对(BET)第二溴化结构域(BD2)的强效、选择性及高溶解度抑制剂,应用于肿瘤及免疫炎症研究领域。 | |||
T63418 |
GSK040
|
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GSK040 是一种有效和具有选择性的BETBD2抑制剂,pIC50值为 8.3。GSK040 对 BETBD2的选择性比 BETBD1(pIC50=4.6) 高 5000 倍。GSK040 可用于肿瘤学和免疫学疾病的研究。 | |||
T36103 |
TW9
TW9 |
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TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistica... | |||
T36574 |
GW841819X
GW841819X |
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GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70... |