Epigenetic Reader Domain

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Epigenetic Reader Domain Signaling Pathway Map

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Products

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Catalog No. Product Name Information Product Use Citations Product Validations
E0449New SGC-SMARCA-BRDVIII

SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

E1095New ODM-207 ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.
S0137 dBET57 dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. dBET57 is inactive on BRD4BD2.
S0344 Y06036 Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM.
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Sci Adv, 2022, 8(5):eabk0221
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
J Med Chem, 2022, 65(5):4182-4200
S1161 Histone Acetyltransferase Inhibitor II

Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

S1216 PFI-1 (PF-6405761) PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.
Immunity, 2021, S1074-7613(21)00222-3
J Mol Cell Biol, 2020, 11;12(5):359-371
Front Immunol, 2019, 1.1243055556
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Adv Sci (Weinh), 2021, e2103360
Front Immunol, 2021, 12:656242
Aging (Albany NY), 2021, 13(10):13968-14000
S2662 Foscenvivint (ICG-001) Foscenvivint (ICG-001) antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.
Cell Death Dis, 2022, 13(3):265
PLoS Pathog, 2022, 18(3):e1010354
Int J Mol Sci, 2022, 23(5)2834
S2780 I-BET151 (GSK1210151A) I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.
Adv Biol (Weinh), 2022, e2101184
Acta Neuropathol, 2021, 10.1007/s00401-021-02341-z
Nat Commun, 2021, 12(1):1045
S2951 P300/​CBP-IN-3 P300/CBP-IN-3 is an inhibitor of p300/CBP histone acetyltransferase.
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
S3573 CC-90010 CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5262 UNC-926 UNC-926 is a L3MBTL1 domain inhibitor with Kd value of 3.9 μM for binding with the MBT domain of the L3MBTL1 protein.
S5916 GSK 5959 GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
S6758 I-CBP112 I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Blood, 2022, 139(1):73-86
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c20394
Am J Hematol, 2022, 10.1002/ajh.26461
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Cell Rep, 2022, 38(3):110250
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7189 Molibresib (I-BET-762) Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.
Bioengineered, 2022, 13(2):2536-2552
Mol Cell, 2021, S1097-2765(21)00995-3
Acta Neuropathol, 2021, 10.1007/s00401-021-02341-z
S7231 GSK2801 GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively.
Epigenetics, 2019, 10.1080/15592294.2019.1656156
Cancer Res, 2018, 78(20):5731-5740
S7233 Bromosporine 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.
J Med Chem, 2022, 65(5):4182-4200
Cancer Res, 2018, 78(20):5731-5740
Elife, 2018, 7e38519
S7256 SGC-CBP30 SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.
Nature, 2021, 10.1038/s41586-021-04116-8
Immunity, 2021, S1074-7613(21)00222-3
Sci Adv, 2021, 7(36):eabf9975
S7295 Apabetalone (RVX-208) Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.
Int J Mol Sci, 2021, 22(19)10204
Cancer Res, 2020, canres.530.2020
J Mol Cell Biol, 2020, 11;12(5):359-371
S7304 CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Mol Cancer Ther, 2021, molcanther.0809.2020
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831
Antimicrob Agents Chemother, 2021, AAC0047021
S7305 MS436 MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.
Cancer Res, 2018, 78(20):5731-5740
Cell Physiol Biochem, 2018, 50(2):640-653
Nucleic Acids Res, 2017, 45(14):8403-8410
S7315 PFI-3 PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.
Mol Cell, 2020, 80(6):1104-1122.e9
Front Genet, 2020, 11:80
Cell Death Dis, 2020, 11(7):549
S7360 Birabresib (OTX015) Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Haematologica, 2021, 10.3324/haematol.2020.267096
Cancer Lett, 2021, S0304-3835(21)00532-2
S7373 UNC669 UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor with IC50 of 6 μM for L3MBTL1, 5- and 11-fold selective over L3MBTL3 and L3MBTL4.
J Med Chem, 2020, 31
Cancer Res, 2018, 78(20):5731-5740
Lab Invest, 2018, 98(12):1627-1641
S7525 XMD8-92 XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.
Sci Rep, 2022, 12(1):7
Nature, 2021, 595(7869):730-734
Cell Rep, 2021, 37(1):109782
S7582 Anacardic Acid Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity, prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
J Pharmacol Exp Ther, 2021, 379(3):303-309
S7620 GSK1324726A (I-BET726) GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
Front Oncol, 2021, 11:773186
J Mol Cell Biol, 2020, 11;12(5):359-371
Nature, 2019, 10.1038/s41586-019-1472-0
S7681 OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.
Cell Rep, 2021, 35(11):109233
J Mol Cell Biol, 2020, 11;12(5):359-371
Cancer Res, 2018, 78(20):5731-5740
S7835 I-BRD9 I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
Cell Death Dis, 2021, 12(11):962
Cancer Discov, 2020, CD-20-0735
Transpl Int, 2020, 33(2):229-243
S7853 Pelabresib (CPI-0610) Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Mol Cancer Ther, 2021, 20(4):691-703
Mol Cancer Ther, 2021, molcanther.0809.2020
bioRxiv, 2021, 10.1101/2021.10.11.464007
S7906 PFI-4 PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
J Mol Cell Biol, 2020, 11;12(5):359-371
S8113 BI-9564 BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.
Mol Cancer Res, 2019, 17(7):1503-1518
S8179 BI-7273 BI-7273 is a potent, selective, and cell-permeable BRD9 BD inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7 respectively in alpha assay.
Cancer Res, 2018, 78(20):5731-5740
S8180 PF-CBP1 HCl PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
Nat Aging, 2021, 1(2):165-178
Cancer Res, 2018, 78(2):436-450
Cancer Res, 2018, 78(20):5731-5740
S8190 CPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
S8265 GSK6853 GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.
Front Oncol, 2021, 11:766656
J Mol Cell Biol, 2020, 11;12(5):359-371
S8296 dBET1 dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment.
Methods Mol Biol, 2021, 2365:3-20
S8297 ARV-825 ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
Mol Oncol, 2022, 10.1002/1878-0261.13195
Methods Mol Biol, 2021, 2365:3-20
J Exp Clin Cancer Res, 2019, 38(1):383
S8344 AZD-5153 6-hydroxy-2-naphthoic acid AZD-5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD-5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.
Mol Cancer Ther, 2022, molcanther.MCT-21-0646-A.2021
Cancer Lett, 2022, 528:31-44
Cell Rep, 2021, 34(7):108750
S8400 Mivebresib (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), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
J Cancer Res Clin Oncol, 2022, 10.1007/s00432-021-03885-z
Sci Rep, 2022, 12(1):7
Bioorg Chem, 2021, 115:105238
S8409 KG-501 (2-naphthol-AS-E-phosphate) KG-501 (2-naphthol-AS-E-phosphate) is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.
Cell Death Discov, 2022, 8(1):36
Sci Immunol, 2021, 6(61)eabg9698
Oncogene, 2021, 10.1038/s41388-021-01845-y
S8496 EED226 EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED.
Cell Death Dis, 2022, 13(2):155
Mol Cell, 2021, 81(10):2183-2200.e13
Nat Commun, 2021, 12(1):6985
S8574 BI 894999 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.
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Oncotarget, 2017, 8(58):98471-98481
S8665 GNE-781 GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.
S8714 INCB057643 INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.
S8723 ABBV-744 ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers.
J Cancer Res Clin Oncol, 2022, 10.1007/s00432-021-03885-z
bioRxiv, 2021, 2021.01.19.427194
bioRxiv, 2021, 2021.11.14.468537
S8739 PLX51107 PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).
Cancers (Basel), 2021, 13(6)1376
Cell Rep, 2020, 32(12):108166
Oncol Rep, 2020, 44(6):2475-2486
S8740 A-485 A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.
Nat Cell Biol, 2022, 24(3):384-399
EMBO J, 2022, e109463
Mol Cell, 2021, S1097-2765(21)00051-4
S8753 INCB054329 INCB054329 (INCB-054329, INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.
Cell, 2021, S0092-8674(21)00354-8
bioRxiv, 2021, 10.1101/2020.08.23.258574
Oncol Rep, 2020, 44(6):2475-2486
S8762 dBET6 dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.
Sci Adv, 2021, 7(23)eabg4126
Bioorg Chem, 2021, 115:105238
bioRxiv, 2021, 2021.01.19.427194
S8763 ZL0420 ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
S8785 A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
S8846 compound 3i (666-15) Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
J Leukoc Biol, 2022, 10.1002/JLB.2A0421-221R
Cell Prolif, 2021, 54(4):e13003
J Cell Sci, 2021, 134(5)jcs254268
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
EMBO Mol Med, 2022, e14990
Sci Rep, 2022, 12(1):7
mBio, 2021, 12(6):e0279221
S9648 NEO2734 NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.
S9659 UNC6852 UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
S9667 Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
S9684 GSK046 GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity.
S9685 GSK620 GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.
S9691New BMS-986158 BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
S9889New dCBP-1 dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.
A5014 CREB Rabbit Recombinant mAb CREB Rabbit Recombinant mAb detects endogenous levels of total CREB.
S0022 YF-2 YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, YF-2 has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. YF-2 also increases p300 activity.
J Exp Clin Cancer Res, 2022, 41(1):77
S7088 UNC1215 UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family.
Cell Death Differ, 2021, 10.1038/s41418-021-00769-0
Cell Death Differ, 2021, 28(8):2536-2551
Cancer Sci, 2020, 112(1):133-143
S8889 MZ-1 MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2.
Cancers (Basel), 2021, 13(16)4118
E0449New SGC-SMARCA-BRDVIII

SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

E1095New ODM-207 ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.
S0137 dBET57 dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. dBET57 is inactive on BRD4BD2.
S0344 Y06036 Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM.
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Sci Adv, 2022, 8(5):eabk0221
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
J Med Chem, 2022, 65(5):4182-4200
S1161 Histone Acetyltransferase Inhibitor II

Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

S1216 PFI-1 (PF-6405761) PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.
Immunity, 2021, S1074-7613(21)00222-3
J Mol Cell Biol, 2020, 11;12(5):359-371
Front Immunol, 2019, 1.1243055556
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Adv Sci (Weinh), 2021, e2103360
Front Immunol, 2021, 12:656242
Aging (Albany NY), 2021, 13(10):13968-14000
S2662 Foscenvivint (ICG-001) Foscenvivint (ICG-001) antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.
Cell Death Dis, 2022, 13(3):265
PLoS Pathog, 2022, 18(3):e1010354
Int J Mol Sci, 2022, 23(5)2834
S2780 I-BET151 (GSK1210151A) I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.
Adv Biol (Weinh), 2022, e2101184
Acta Neuropathol, 2021, 10.1007/s00401-021-02341-z
Nat Commun, 2021, 12(1):1045
S2951 P300/​CBP-IN-3 P300/CBP-IN-3 is an inhibitor of p300/CBP histone acetyltransferase.
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
S3573 CC-90010 CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5262 UNC-926 UNC-926 is a L3MBTL1 domain inhibitor with Kd value of 3.9 μM for binding with the MBT domain of the L3MBTL1 protein.
S5916 GSK 5959 GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
S6758 I-CBP112 I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Blood, 2022, 139(1):73-86
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c20394
Am J Hematol, 2022, 10.1002/ajh.26461
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Cell Rep, 2022, 38(3):110250
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7189 Molibresib (I-BET-762) Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.
Bioengineered, 2022, 13(2):2536-2552
Mol Cell, 2021, S1097-2765(21)00995-3
Acta Neuropathol, 2021, 10.1007/s00401-021-02341-z
S7231 GSK2801 GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively.
Epigenetics, 2019, 10.1080/15592294.2019.1656156
Cancer Res, 2018, 78(20):5731-5740
S7233 Bromosporine 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.
J Med Chem, 2022, 65(5):4182-4200
Cancer Res, 2018, 78(20):5731-5740
Elife, 2018, 7e38519
S7256 SGC-CBP30 SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively.
Nature, 2021, 10.1038/s41586-021-04116-8
Immunity, 2021, S1074-7613(21)00222-3
Sci Adv, 2021, 7(36):eabf9975
S7295 Apabetalone (RVX-208) Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.
Int J Mol Sci, 2021, 22(19)10204
Cancer Res, 2020, canres.530.2020
J Mol Cell Biol, 2020, 11;12(5):359-371
S7304 CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Mol Cancer Ther, 2021, molcanther.0809.2020
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831
Antimicrob Agents Chemother, 2021, AAC0047021
S7305 MS436 MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.
Cancer Res, 2018, 78(20):5731-5740
Cell Physiol Biochem, 2018, 50(2):640-653
Nucleic Acids Res, 2017, 45(14):8403-8410
S7315 PFI-3 PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.
Mol Cell, 2020, 80(6):1104-1122.e9
Front Genet, 2020, 11:80
Cell Death Dis, 2020, 11(7):549
S7360 Birabresib (OTX015) Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Haematologica, 2021, 10.3324/haematol.2020.267096
Cancer Lett, 2021, S0304-3835(21)00532-2
S7373 UNC669 UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor with IC50 of 6 μM for L3MBTL1, 5- and 11-fold selective over L3MBTL3 and L3MBTL4.
J Med Chem, 2020, 31
Cancer Res, 2018, 78(20):5731-5740
Lab Invest, 2018, 98(12):1627-1641
S7525 XMD8-92 XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively.
Sci Rep, 2022, 12(1):7
Nature, 2021, 595(7869):730-734
Cell Rep, 2021, 37(1):109782
S7582 Anacardic Acid Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity, prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
J Pharmacol Exp Ther, 2021, 379(3):303-309
S7620 GSK1324726A (I-BET726) GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
Front Oncol, 2021, 11:773186
J Mol Cell Biol, 2020, 11;12(5):359-371
Nature, 2019, 10.1038/s41586-019-1472-0
S7681 OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.
Cell Rep, 2021, 35(11):109233
J Mol Cell Biol, 2020, 11;12(5):359-371
Cancer Res, 2018, 78(20):5731-5740
S7835 I-BRD9 I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
Cell Death Dis, 2021, 12(11):962
Cancer Discov, 2020, CD-20-0735
Transpl Int, 2020, 33(2):229-243
S7853 Pelabresib (CPI-0610) Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Mol Cancer Ther, 2021, 20(4):691-703
Mol Cancer Ther, 2021, molcanther.0809.2020
bioRxiv, 2021, 10.1101/2021.10.11.464007
S7906 PFI-4 PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
J Mol Cell Biol, 2020, 11;12(5):359-371
S8113 BI-9564 BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.
Mol Cancer Res, 2019, 17(7):1503-1518
S8179 BI-7273 BI-7273 is a potent, selective, and cell-permeable BRD9 BD inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7 respectively in alpha assay.
Cancer Res, 2018, 78(20):5731-5740
S8180 PF-CBP1 HCl PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
Nat Aging, 2021, 1(2):165-178
Cancer Res, 2018, 78(2):436-450
Cancer Res, 2018, 78(20):5731-5740
S8190 CPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
S8265 GSK6853 GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.
Front Oncol, 2021, 11:766656
J Mol Cell Biol, 2020, 11;12(5):359-371
S8296 dBET1 dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment.
Methods Mol Biol, 2021, 2365:3-20
S8297 ARV-825 ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
Mol Oncol, 2022, 10.1002/1878-0261.13195
Methods Mol Biol, 2021, 2365:3-20
J Exp Clin Cancer Res, 2019, 38(1):383
S8344 AZD-5153 6-hydroxy-2-naphthoic acid AZD-5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD-5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes.
Mol Cancer Ther, 2022, molcanther.MCT-21-0646-A.2021
Cancer Lett, 2022, 528:31-44
Cell Rep, 2021, 34(7):108750
S8400 Mivebresib (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), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
J Cancer Res Clin Oncol, 2022, 10.1007/s00432-021-03885-z
Sci Rep, 2022, 12(1):7
Bioorg Chem, 2021, 115:105238
S8409 KG-501 (2-naphthol-AS-E-phosphate) KG-501 (2-naphthol-AS-E-phosphate) is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.
Cell Death Discov, 2022, 8(1):36
Sci Immunol, 2021, 6(61)eabg9698
Oncogene, 2021, 10.1038/s41388-021-01845-y
S8496 EED226 EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED.
Cell Death Dis, 2022, 13(2):155
Mol Cell, 2021, 81(10):2183-2200.e13
Nat Commun, 2021, 12(1):6985
S8574 BI 894999 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.
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Oncotarget, 2017, 8(58):98471-98481
S8665 GNE-781 GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.
S8714 INCB057643 INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones.
S8723 ABBV-744 ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers.
J Cancer Res Clin Oncol, 2022, 10.1007/s00432-021-03885-z
bioRxiv, 2021, 2021.01.19.427194
bioRxiv, 2021, 2021.11.14.468537
S8739 PLX51107 PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).
Cancers (Basel), 2021, 13(6)1376
Cell Rep, 2020, 32(12):108166
Oncol Rep, 2020, 44(6):2475-2486
S8740 A-485 A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.
Nat Cell Biol, 2022, 24(3):384-399
EMBO J, 2022, e109463
Mol Cell, 2021, S1097-2765(21)00051-4
S8753 INCB054329 INCB054329 (INCB-054329, INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.
Cell, 2021, S0092-8674(21)00354-8
bioRxiv, 2021, 10.1101/2020.08.23.258574
Oncol Rep, 2020, 44(6):2475-2486
S8762 dBET6 dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.
Sci Adv, 2021, 7(23)eabg4126
Bioorg Chem, 2021, 115:105238
bioRxiv, 2021, 2021.01.19.427194
S8763 ZL0420 ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
S8785 A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
S8846 compound 3i (666-15) Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
J Leukoc Biol, 2022, 10.1002/JLB.2A0421-221R
Cell Prolif, 2021, 54(4):e13003
J Cell Sci, 2021, 134(5)jcs254268
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
EMBO Mol Med, 2022, e14990
Sci Rep, 2022, 12(1):7
mBio, 2021, 12(6):e0279221
S9648 NEO2734 NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.
S9659 UNC6852 UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
S9667 Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
S9684 GSK046 GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity.
S9685 GSK620 GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.
S9691New BMS-986158 BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
S9889New dCBP-1 dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.
A5014 CREB Rabbit Recombinant mAb CREB Rabbit Recombinant mAb detects endogenous levels of total CREB.
S0022 YF-2 YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, YF-2 has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. YF-2 also increases p300 activity.
J Exp Clin Cancer Res, 2022, 41(1):77
S7088 UNC1215 UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family.
Cell Death Differ, 2021, 10.1038/s41418-021-00769-0
Cell Death Differ, 2021, 28(8):2536-2551
Cancer Sci, 2020, 112(1):133-143
S8889 MZ-1 MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2.
Cancers (Basel), 2021, 13(16)4118
E0449New SGC-SMARCA-BRDVIII

SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

E1095New ODM-207 ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.
S9691New BMS-986158 BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
S9889New dCBP-1 dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.