About 12 results found for searched term "BRD7-IN-2" (0.122 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M41648 | BRD7-IN-2 | Epigenetic Reader Domain |
| BRD7-IN-2 is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. | ||
| M5200 | BRD73954 | HDAC |
| BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively. | ||
| M8397 | BRD4770 | Histone Methyltransferase |
| BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 inhibited the dimethylation and trimethylation of H3K9, EC50 was 5 µM, and had little effect on H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 activates the ataxic telangiectasia mutation (ATM) pathway and induces cell senescence. | ||
| M10531 | BRD3731 | GSK-3 |
| BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. | ||
| M27706 | RVX-297 | Epigenetic Reader Domain |
| RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models. | ||
| M28903 | (2S,3R)-LP99 | Epigenetic Reader Domain |
| (2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion. | ||
| M29172 | TP-472 | Epigenetic Reader Domain |
| TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells. | ||
| M29291 | GSK973 | Epigenetic Reader Domain |
| GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5). | ||
| M29339 | SB-284851-BT | p38 MAPK |
| SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET). | ||
| M29492 | VZ185 | PROTAC |
| VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively. | ||
| M30012 | BRD7389 | S6 Kinase |
| BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells. | ||
| M41650 | BRD4 Inhibitor-27 | Epigenetic Reader Domain |
| BRD4 Inhibitor-27 is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. | ||
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