Epigenetic Reader Domain
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Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.
The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.
p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.
Products Related to Epigenetic Reader Domain(298)
- GC32863Target Protein-binding moiety 4CAS: 1300019-38-8Purity: >98.50%
Target Protein-binding moiety 4 (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. Target Protein-binding moiety 4 (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
- GC32980PROTAC BET degrader-2CAS: 2093388-33-9Purity: >98.50%
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
- GC33015FL-411 (BRD4-IN-1)CAS: 2118944-88-8Purity: >98.00%
FL-411 (BRD4-IN-1) is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).
- GC33017BRD4 degrader AT1CAS: 2098836-45-2Purity: >98.50%
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.
- GC33028CF53CAS: 1808160-52-2Purity: >98.00%
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
- GC33042IACS-9571 (ASIS-P040)CAS: 1800477-30-8Purity: >98.00%
IACS-9571 (ASIS-P040) is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
- GC33104BAY1238097CAS: 1564268-08-1Purity: >98.50%
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
- GC33109PROTAC BET Degrader-1CAS: 2093386-22-0Purity: >98.50%
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
- GC33183L-45 (L-Moses)CAS: 2079885-05-3Purity: >99.00%
L-45 (L-Moses) (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
- GC33198(S)-JQ-35 (TEN-010)CAS: 1349719-98-7Purity: >98.50%
(S)-JQ-35 (TEN-010) (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.
- GC33211HJB97CAS: 2093391-24-1Purity: >98.00%
HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity.
- GC33212GNE-207CAS: 2158266-58-9Purity: >96.00%
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.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC32812 | BMS-986158 | 1800340-40-2 | >98.50% | |
A BET bromodomain inhibitor | ||||
| GC32863 | Target Protein-binding moiety 4 | 1300019-38-8 | >98.50% | |
Target Protein-binding moiety 4 (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. Target Protein-binding moiety 4 (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1. | ||||
| GC32880 | TPOP146 | 2018300-62-2 | >99.50% | |
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. | ||||
| GC32960 | GNE-049 | 1936421-41-8 | >98.50% | |
GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. | ||||
| GC32980 | PROTAC BET degrader-2 | 2093388-33-9 | >98.50% | |
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. | ||||
| GC33015 | FL-411 (BRD4-IN-1) | 2118944-88-8 | >98.00% | |
FL-411 (BRD4-IN-1) is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1). | ||||
| GC33017 | BRD4 degrader AT1 | 2098836-45-2 | >98.50% | |
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. | ||||
| GC33026 | INCB054329 | 1628607-64-6 | >98.00% | |
INCB054329 is a potent BET inhibitor. | ||||
| GC33028 | CF53 | 1808160-52-2 | >98.00% | |
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo. | ||||
| GC33042 | IACS-9571 (ASIS-P040) | 1800477-30-8 | >98.00% | |
IACS-9571 (ASIS-P040) is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. | ||||
| GC33102 | MZP-54 | 2010159-47-2 | >98.00% | |
MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2. | ||||
| GC33104 | BAY1238097 | 1564268-08-1 | >98.50% | |
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM). | ||||
| GC33109 | PROTAC BET Degrader-1 | 2093386-22-0 | >98.50% | |
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration. | ||||
| GC33183 | L-45 (L-Moses) | 2079885-05-3 | >99.00% | |
L-45 (L-Moses) (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM. | ||||
| GC33198 | (S)-JQ-35 (TEN-010) | 1349719-98-7 | >98.50% | |
(S)-JQ-35 (TEN-010) (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity. | ||||
| GC33204 | GS-626510 | 1637770-13-8 | >99.50% | |
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively. | ||||
| GC33211 | HJB97 | 2093391-24-1 | >98.00% | |
HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity. | ||||
| GC33212 | GNE-207 | 2158266-58-9 | >96.00% | |
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. | ||||
| GC33217 | QCA570 | 2207569-08-0 | >99.50% | |
QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC50 of 10 nM for BRD4 BD1 Protein. | ||||
| GC33264 | Y06137 | 2226534-49-0 | >99.50% | |
Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM. | ||||
| GC33280 | A1874 | 2064292-12-0 | >98.00% | |
A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation. | ||||
| GC33285 | Y06036 | 1832671-96-1 | >99.00% | |
Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity. | ||||
| GC33324 | GSK9311 | 1923851-49-3 | >99.00% | |
GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively. | ||||
| GC33363 | MZP-55 | 2010159-48-3 | >99.00% | |
MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4BD2. | ||||