About 30 results found for searched term "I-BRD9" (0.093 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M8567 | I-BRD9 | Epigenetic Reader Domain |
| I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9), thought to be a member of the chromatin remodelling SWI/SNF BAF complex, which plays a fundamental role in gene expression regulation. | ||
| M4818 | Bromosporine | Epigenetic Reader Domain |
| Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively. | ||
| 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. | ||
| M25608 | FHD-609 | PROTAC |
| FHD-609 is an inhibitor and a degrader of BRD9 (bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. | ||
| 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. | ||
| M8602 | BI-9564 | Epigenetic Reader Domain |
| BI-9564 is a cell permeable, potent and specific inhibitor of BRD9 and BRD7. | ||
| M8931 | BI-7273 | Epigenetic Reader Domain |
| BI-7273 is a potent and selective BRD9 inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7, respectively. | ||
| 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. | ||
| M9824 | MZ 1 | PROTAC |
| MZ1 | ||
| MZ 1 is a PROTAC BRD4 degrader, with Kd values of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively. | ||
| M10759 | GSK046 | Epigenetic Reader Domain |
| iBET-BD2 | ||
| GSK046 (iBET-BD2) is an effective, selective and orally active inhibitor of the BD2 bromine domain of the BET protein,IC50 The values are 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2), and 214 nM (BRDT BD2). GSK046 has immunomodulatory activity. | ||
| M10952 | BRD0639 | PRMTs |
| BRD0639 is a first-in-class inhibitor of PRMT5-substrate aptamer interactions.BRD0639 is a PRMT5-binding motif (PBM) competitor that supports studies of PBM-dependent PRMT5 activity. | ||
| M13435 | CFT8634 | Epigenetic Reader Domain |
| CFT-8634 | ||
| CFT8634 is an inhibitor of BRD9 for the study of brD9-dependent cancers, including synoviosarcomas and smarCB1-deficient cancers. | ||
| M13843 | BRD9539 | Histone Methyltransferase |
| BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1. | ||
| M20727 | BI 894999 | Epigenetic Reader Domain |
| BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1. | ||
| M20751 | BRD6989 | CDK |
| BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA). | ||
| 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. | ||
| 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. | ||
| M28241 | BRD5529 | E1/E2/E3 Enzyme |
| BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC). | ||
| M28344 | BRD0539 | CRISPR/Cas9 |
| BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay. | ||
| M28352 | BRD6688 | HDAC |
| BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model. | ||
| M28650 | BRD0209 | GSK-3 |
| BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases. | ||
| M28814 | GSK8573 | Epigenetic Reader Domain |
| GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments. | ||
| 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. | ||
| M28904 | LP99 | Epigenetic Reader Domain |
| LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. | ||
| M29027 | GNE-375 | Epigenetic Reader Domain |
| GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin. | ||
| 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. | ||
| M29234 | GNE-886 | Epigenetic Reader Domain |
| GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM. | ||
| 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). | ||
| M29324 | dBRD9 | PROTAC |
| dBRD9 is a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family. | ||
| 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. | ||
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