Cat. No. | Product Name | Target | Signaling Pathways |
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T61327 |
BRD4 Inhibitor-15
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BRD4 Inhibitor-15 (compound 13) is a highly potent and specific inhibitor of BRD4, effectively inhibiting it with an IC50 of 18 nM. By regulating the Bcl-2/Bax proteins and activating the caspase-3 signaling pathway, BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells. Additionally, it effectively down-regulates the c-Myc level in 22RV1 cells. Due to its properties, BRD4 Inhibitor-15 is a valuable compound for research related to prostate cancer [1]. | |||
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。 | |||
T64192 | BRD4 D1-IN-2 | ||
BRD4 D1-IN-2 (compound 26) 是一种选择性的、有效的 BRD4 D1 抑制剂,其 IC50 值小于 0.092 μM。BRD4 D1-IN-2 对 BRD4 D1 具有 15 nM 亲和力,对 BRD2 D1 和 BRD4 D2 具有 500 倍以上的选择性。 | |||
T18598 |
PROTAC BRD2/BRD4 degrader-1
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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]. | |||
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。 | |||
T38381 |
CAY17c
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CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,... |