About 31 results found for searched term "BRD4-IN-4" (0.114 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M41667 | BRD4-IN-4 | Epigenetic Reader Domain |
| BRD4-IN-4 is a BRD4 inhibitor (IC50=6.83 μM). | ||
| M2167 | (+)-JQ1 | Epigenetic Reader Domain |
| JQ1 | ||
| (+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. | ||
| M5258 | Mivebresib | Epigenetic Reader Domain |
| ABBV-075 | ||
| Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4) | ||
| M6206 | ARV-825 | Epigenetic Reader Domain |
| ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, 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. | ||
| M9026 | AZD-5153 HNT salt | Epigenetic Reader Domain |
| AZD5153 | ||
| AZD-5153 HNT salt is a potent, selective and orally available BET/BRD4 bromodomain inhibitor, disrupts BRD4 with an IC50 of 1.7 nM. | ||
| M9237 | dBET1 | Epigenetic Reader Domain |
| dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 linked to NSC 527179 with a linker. | ||
| M9396 | A1874 | PROTAC |
| A1874 is a BRD4-degrading PROTAC which inhibits many cancer cell lines proliferation, with DC50 of 32 nM (induce BRD4 degradation in cells). | ||
| M9515 | MS417 | Epigenetic Reader Domain |
| GTPL7512 | ||
| MS417 (also known as GTPL7512) is a potent and selective BRD4 inhibitor, which binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30 and 46 nM, respectively. | ||
| M10380 | dBET57 | PROTAC |
| dBET-57 | ||
| dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC) which exhibits significant and selective degradation of BRD4 BD1 but is inactive on BRD4 BD2. | ||
| M10862 | MS645 | Epigenetic Reader Domain |
| MS645 is a BET bromodomains (BrD) inhibitor for K of BRD4-BD1/BD2i The value is 18.4 nM. MS645 spatially limits the divalent inhibition of BRD4 BrDs, resulting in sustained inhibition of BRD4 transcriptional activity in solid tumor cells. | ||
| M10908 | ZL0420 | Epigenetic Reader Domain |
| ZL0420 is a potent and selective BET bromine domain 4 (BRD4) inhibitor of BRD4 BD1 and BRD4 BD2 IC50 27 nM and 32 nM, respectively. | ||
| M21109 | Inobrodib | Epigenetic Reader Domain |
| CCS1477; CBP-IN-1; CBP/p300-IN-4 | ||
| Inobrodib (CCS1477, CBP-IN-1) is an orally active, potent and selective p300/CBP inhibitor. inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM and has a 170/130 fold selectivity compared to BRD4 with a Kd of 222 nM. Inobrodib (CCS1477) acts by inhibiting the expression and function of androgen receptor (AR) and by inhibiting c-Myc. | ||
| M21426 | BRD-K98645985 | HIV Protease |
| BRD-K98645985 is a mammalian SWI/SNF transcriptional repressor inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complex, prevents nucleosome localization, effectively reverses HIV-1 latency, and has no T-cell toxicity. | ||
| M25513 | GNE-207 | Epigenetic Reader Domain |
| GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4(1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells. | ||
| M25521 | OXFBD04 | Epigenetic Reader Domain |
| OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity. | ||
| M28413 | OXFBD02 | Epigenetic Reader Domain |
| OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM. | ||
| M28737 | UMB-32 | Epigenetic Reader Domain |
| UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor. | ||
| 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. | ||
| M29228 | BRD4 degrader AT1 | PROTAC |
| BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in 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). | ||
| M29385 | ZL0454 | Epigenetic Reader Domain |
| ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2. | ||
| M29389 | ZL0590 | Epigenetic Reader Domain |
| ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities. | ||
| M29443 | TD-106 | Ligand for E3 Ligase |
| TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation. | ||
| 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. | ||
| M29501 | PROTAC BRD4 Degrader-3 | PROTAC |
| PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4. | ||
| M29518 | TD-428 | PROTAC |
| TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation. | ||
| M29804 | XY-06-007 | PROTAC |
| XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies. | ||
| M29810 | BRD4-BD1-IN-1 | Epigenetic Reader Domain |
| BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM. | ||
| M29811 | BRD4-BD1-IN-2 | Epigenetic Reader Domain |
| BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC50 of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases. | ||
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