Epigenetic Reader Domain

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Epigenetic Reader Domain Products

All (57) Epigenetic Reader Domain Inhibitors (53) Epigenetic Reader Domain Activators (1) Epigenetic Reader Domain Antagonists (1) Epigenetic Reader Domain Modulators (1)

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cancer Cell, 2020, 37(3):340-353 Mol Cell, 2020, 10.1016/j.molcel.2020.01.023 Nat Commun, 2020, 29;11(1):2086
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.	Nat Genet, 2020, 52(4):408-417 Adv Sci (Weinh), 2020, 16;7(7):1902926 Nat Commun, 2020, 29;11(1):2086	The BET protein inhibitor JQ1 reduces c-Myc expression and attenuates primary MCC cell proliferation. A, decreased c-Myc expression in MCC-3 and MCC-5 treated with JQ1 (800 nmol/L) for 72 hours by qRT-PCR and immunoblotting. The mRNA expression of target genes was normalized to that of MRPS2 and a value of 1.0 was assigned to the mRNA expression of target genes in the control group (means+SEM; **, P < 0.01 vs. control); b-actin was used as a loading control for immunoblotting.
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.	Nat Commun, 2020, 14;11(1):1833 Int J Cancer, 2020, 10.1002/ijc.33000 J Mol Cell Biol, 2020, 11;12(5):359-371	OVTOKO and OVCA420 cells were treated with DMSO, JQ1 (1 μM) or I-BET151 (1 μM). Cell lysates were immunoblotted with indicated antibodies.
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.	J Mol Cell Biol, 2020, 11;12(5):359-371 Front Immunol, 2019, 1.1243055556 World J Urol, 2019, 37(2):343-349
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.	Nat Commun, 2020, 14;11(1):1833 Signal Transduct Target Ther, 2020, 4;5(1):20 Aging (Albany NY), 2020, 12(10):9240-9259	PECAPJ49 parental and cetuximab-resistant clones were treated with 100 nmol/L cetuximab ± 800 nmol/L I-BET-762(IBET) for 72 hours. Cells were stained with crystal violet and quantified as described in Materials and Methods (n = 3; *, P < 0.02). Figures are representative of three independent experiments.
S3239^New	Emetine Dihydrochloride Emetine Dihydrochloride, 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 Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
S7853^New	CPI-0610 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.
S9648^New	NEO2734 NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.
S8968^New	PRI-724 PRI-724 is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.	Cell, 2020, 182(5):1232-1251.e22 Cancers (Basel), 2020, 12(9)E2556 Cell Death Dis, 2020, 11(8):673
S8961^New	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.
S0137^New	dBET57 dBET57 is a novel, potent and selective degrader of BRD4_BD1 based on the PROTAC technology with DC_50/5h of 500 nM. dBET57 is inactive on BRD4_BD2.
S8948^New	SRX3207 SRX3207 is a novel dual Syk-PI3K inhibitor 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 can relieve tumor immunosuppression.
S6758^New	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.
S8574^New	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.
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.	Cancer Res, 2020, canres.530.2020 J Mol Cell Biol, 2020, 11;12(5):359-371 Cell Rep, 2019, 27(11):3331-3344	Bromodomain 1 or 2 of BET family proteins is involved in 3T3-L1 adipogenesis. (A) LY294002, RVX208 and JQ1 were applied to differentiating 3T3-L1 from day 2 to day 6. Phenyl acetate (PA), known as a PPAR-γ agonist was used as a positive control. Cells were labeled with ORO (Bar=50nm). (B) Schematic representation of specificity of each chemical inhibitor for Bromodomain BD1 and 2 and quantitative analysis of ORO staining. The IDMR treatment without drugs (CTL) was used to define 100%. Data are reported as means ± sd (n=3); *** p<0.001 vs IDM control; ### p<0.001 vs IDMR control (-)-JQ1); +++ p<0.01 vs IDM of each condition; ns, non significant.
S7152	C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.	Autophagy, 2020, 15:1-13 Cell Rep, 2020, 26;31(8):107690 Oncogene, 2020, 39(18):3754-3773	Phosphorylation of STAT6 in butyrate-treated M2-BMDMs. Western blotting was performed with anti-phospho-STAT6, STAT6, and β-actin. Data are representative of three independent experiments. M2:M2 macrophage; But:butyrate.
S1848	Curcumin Curcumin (Diferuloylmethane) 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 transcription factor 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.	Front Microbiol, 2020, 15;10:3016 Protein Sci, 2020, 29(6):1366-1372 Pharm Biol, 2020, 58(1):25-34
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.	Cell Biol Int, 2020, 4 Sci Transl Med, 2019, 9(415) Nat Commun, 2019, 10(1):5713	H3K27ac change. SMMC-7721 cells were treated with EPZ-6438 (1 μM) alone or in combination with histone acetyltransferase inhibitors C646 (5 μM) or SGC-CBP30 (5 μM) for 6 days. H3K27ac was examined by immunoblotting.
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.	Int J Parasitol Drugs Drug Resist, 2018, 8(2):189-193 Oncotarget, 2017, 8(55):94104-94116
S7360	Birabresib (OTX015) OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1.	Nat Commun, 2020, 22;11(1):1935 Nat Commun, 2020, 14;11(1):1833 Clin Cancer Res, 2020, 20 pii: clincanres	A. Growth inhibition IC50 values of CUDC-907 and three BET inhibitors (I-BET-762, JQ1, and OTX015) in three BRD–NUT fusion-positive NMC cell lines. Cell viability after 72-hour incubation was assessed by the CellTiter-Glo assay. Growth inhibition IC50 values for each compound were determined by GraphPad Prism 5.
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 Lab Invest, 2018, 98(12):1627-1641
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.
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
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.
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.	Genome Med, 2020, 12(1):63
S7304	CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.	Aging (Albany NY), 2020, 12(5):4547-4557 EBioMedicine, 2019, 43:201-210 Biochem Pharmacol, 2019, 164:237-251
S7305	MS436 MS436 is a selective BET bromodomain inhibitor with K_i of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.	Cell Physiol Biochem, 2018, 50(2):640-653 Nucleic Acids Res, 2017, 45(14):8403-8410	BRD4 inhibitors facilitate Palomid 529-induced 786-O cell apoptosis. 786-O cells were pretreated for 30 min with JQ1 (1 μM), MS436 (50 nM) or CPI203 (100 nM), followed by Palomid 529 (“P529”, 5 μM) treatment, cells were then cultured for the applied time, cell survival was tested by the MTT assay (A); Cell apoptosis was tested by the assays mentioned in the text (B and C). For each assay, n=5. * p< 0.05 vs. “Ctrl” cells. # p< 0.05 vs. “Palomid 529” only cells. In this figure, experiments were repeated four times, and similar results were obtained each time.
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.
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.
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
S7231	GSK2801 GSK2801 is a selective bromodomains BAZ2A/B inhibitor with K_D of 257 nM and 136 nM, respectively.	Epigenetics, 2019, 10.1080/15592294.2019.1656156
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.
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.	J Exp Clin Cancer Res, 2019, 38(1):383
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
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.
S7315	PFI-3 PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.	Front Genet, 2020, 11:80 Cell Death Dis, 2020, 11(7):549 Front Cell Dev Biol, 2020, 8:569	Western blot analysis of Brg1, α-SMA and Col1a1 expression in the presence of PFI-3(0uM, 5uM, 10uM,20uM,40uM,80uM) for 48 h in the indicated concentration in LX-2 cells.
S8409	KG-501 (2-naphthol-AS-E-phosphate) KG-501 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.	Cereb Cortex, 2020, 5 pii: bhaa062 Biomolecules, 2020, 9;10(4) pii: E580 J Cell Mol Med, 2020, 10.1111/jcmm.15723
S7582	Anacardic Acid Anacardic 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.	Oncogene, 2020, 39(18):3754-3773 Free Radic Biol Med, 2020, 10.1016/j.freeradbiomed.2020.01.016 Chemosphere, 2020, 247:125825	Western blot analysis of α-SMA expression in whole-lung lysates. Data are expressed as means ± SEM, *P < 0.05 versus vehicle and #P < 0.05 versus PQ (n = 4-6).
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.	Blood Cancer J, 2019, 9(2):4 Leuk Res, 2019, 77:42-50
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.
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.
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.	J Mol Cell Biol, 2020, 11;12(5):359-371
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.	Nat Commun, 2020, 11(1):3018 J Med Chem, 2020, 31 Cell Stem Cell, 2019, 24(1):123-137
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.	Cancer Res, 2018, 78(2):436-450
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).	Leuk Res, 2019, 77:42-50
S8344	AZD5153 AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4.	Mol Cancer Ther, 2019, 18(8):1439-1450 Int J Biol Sci, 2019, 15(9):1942-1954 Cancer Cell, 2018, 33(3):401-416
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.	Genome Res, 2019, 29(10):1659-1672
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.	J Mol Cell Biol, 2020, 11;12(5):359-371 Nature, 2019, 10.1038/s41586-019-1472-0 Cancer Cell, 2018, 33(3):401-416
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.	Leuk Res, 2019, 77:42-50
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
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.
S7681	OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with K_d of 100 nM and 500 nM, respectively.	J Mol Cell Biol, 2020, 11;12(5):359-371
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.
S0022^New	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.
S7088	UNC1215 UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and K_d of 120 nM, 50-fold selective versus other members of the human MBT family.	Cell Death Dis, 2018, Lab Invest, 2018, 98(12):1627-1641
S8889^New	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 Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.
S8785^New	A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cancer Cell, 2020, 37(3):340-353 Mol Cell, 2020, 10.1016/j.molcel.2020.01.023 Nat Commun, 2020, 29;11(1):2086
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.	Nat Genet, 2020, 52(4):408-417 Adv Sci (Weinh), 2020, 16;7(7):1902926 Nat Commun, 2020, 29;11(1):2086	The BET protein inhibitor JQ1 reduces c-Myc expression and attenuates primary MCC cell proliferation. A, decreased c-Myc expression in MCC-3 and MCC-5 treated with JQ1 (800 nmol/L) for 72 hours by qRT-PCR and immunoblotting. The mRNA expression of target genes was normalized to that of MRPS2 and a value of 1.0 was assigned to the mRNA expression of target genes in the control group (means+SEM; **, P < 0.01 vs. control); b-actin was used as a loading control for immunoblotting.
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.	Nat Commun, 2020, 14;11(1):1833 Int J Cancer, 2020, 10.1002/ijc.33000 J Mol Cell Biol, 2020, 11;12(5):359-371	OVTOKO and OVCA420 cells were treated with DMSO, JQ1 (1 μM) or I-BET151 (1 μM). Cell lysates were immunoblotted with indicated antibodies.
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.	J Mol Cell Biol, 2020, 11;12(5):359-371 Front Immunol, 2019, 1.1243055556 World J Urol, 2019, 37(2):343-349
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.	Nat Commun, 2020, 14;11(1):1833 Signal Transduct Target Ther, 2020, 4;5(1):20 Aging (Albany NY), 2020, 12(10):9240-9259	PECAPJ49 parental and cetuximab-resistant clones were treated with 100 nmol/L cetuximab ± 800 nmol/L I-BET-762(IBET) for 72 hours. Cells were stained with crystal violet and quantified as described in Materials and Methods (n = 3; *, P < 0.02). Figures are representative of three independent experiments.
S3239^New	Emetine Dihydrochloride Emetine Dihydrochloride, 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 Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
S7853^New	CPI-0610 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.
S9648^New	NEO2734 NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.
S8968^New	PRI-724 PRI-724 is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.	Cell, 2020, 182(5):1232-1251.e22 Cancers (Basel), 2020, 12(9)E2556 Cell Death Dis, 2020, 11(8):673
S8961^New	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.
S0137^New	dBET57 dBET57 is a novel, potent and selective degrader of BRD4_BD1 based on the PROTAC technology with DC_50/5h of 500 nM. dBET57 is inactive on BRD4_BD2.
S8948^New	SRX3207 SRX3207 is a novel dual Syk-PI3K inhibitor 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 can relieve tumor immunosuppression.
S6758^New	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.
S8574^New	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.
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.	Cancer Res, 2020, canres.530.2020 J Mol Cell Biol, 2020, 11;12(5):359-371 Cell Rep, 2019, 27(11):3331-3344	Bromodomain 1 or 2 of BET family proteins is involved in 3T3-L1 adipogenesis. (A) LY294002, RVX208 and JQ1 were applied to differentiating 3T3-L1 from day 2 to day 6. Phenyl acetate (PA), known as a PPAR-γ agonist was used as a positive control. Cells were labeled with ORO (Bar=50nm). (B) Schematic representation of specificity of each chemical inhibitor for Bromodomain BD1 and 2 and quantitative analysis of ORO staining. The IDMR treatment without drugs (CTL) was used to define 100%. Data are reported as means ± sd (n=3); *** p<0.001 vs IDM control; ### p<0.001 vs IDMR control (-)-JQ1); +++ p<0.01 vs IDM of each condition; ns, non significant.
S7152	C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.	Autophagy, 2020, 15:1-13 Cell Rep, 2020, 26;31(8):107690 Oncogene, 2020, 39(18):3754-3773	Phosphorylation of STAT6 in butyrate-treated M2-BMDMs. Western blotting was performed with anti-phospho-STAT6, STAT6, and β-actin. Data are representative of three independent experiments. M2:M2 macrophage; But:butyrate.
S1848	Curcumin Curcumin (Diferuloylmethane) 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 transcription factor 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.	Front Microbiol, 2020, 15;10:3016 Protein Sci, 2020, 29(6):1366-1372 Pharm Biol, 2020, 58(1):25-34
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.	Cell Biol Int, 2020, 4 Sci Transl Med, 2019, 9(415) Nat Commun, 2019, 10(1):5713	H3K27ac change. SMMC-7721 cells were treated with EPZ-6438 (1 μM) alone or in combination with histone acetyltransferase inhibitors C646 (5 μM) or SGC-CBP30 (5 μM) for 6 days. H3K27ac was examined by immunoblotting.
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.	Int J Parasitol Drugs Drug Resist, 2018, 8(2):189-193 Oncotarget, 2017, 8(55):94104-94116
S7360	Birabresib (OTX015) OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1.	Nat Commun, 2020, 22;11(1):1935 Nat Commun, 2020, 14;11(1):1833 Clin Cancer Res, 2020, 20 pii: clincanres	A. Growth inhibition IC50 values of CUDC-907 and three BET inhibitors (I-BET-762, JQ1, and OTX015) in three BRD–NUT fusion-positive NMC cell lines. Cell viability after 72-hour incubation was assessed by the CellTiter-Glo assay. Growth inhibition IC50 values for each compound were determined by GraphPad Prism 5.
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 Lab Invest, 2018, 98(12):1627-1641
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.
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
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.
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.	Genome Med, 2020, 12(1):63
S7304	CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.	Aging (Albany NY), 2020, 12(5):4547-4557 EBioMedicine, 2019, 43:201-210 Biochem Pharmacol, 2019, 164:237-251
S7305	MS436 MS436 is a selective BET bromodomain inhibitor with K_i of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively.	Cell Physiol Biochem, 2018, 50(2):640-653 Nucleic Acids Res, 2017, 45(14):8403-8410	BRD4 inhibitors facilitate Palomid 529-induced 786-O cell apoptosis. 786-O cells were pretreated for 30 min with JQ1 (1 μM), MS436 (50 nM) or CPI203 (100 nM), followed by Palomid 529 (“P529”, 5 μM) treatment, cells were then cultured for the applied time, cell survival was tested by the MTT assay (A); Cell apoptosis was tested by the assays mentioned in the text (B and C). For each assay, n=5. * p< 0.05 vs. “Ctrl” cells. # p< 0.05 vs. “Palomid 529” only cells. In this figure, experiments were repeated four times, and similar results were obtained each time.
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.
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.
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
S7231	GSK2801 GSK2801 is a selective bromodomains BAZ2A/B inhibitor with K_D of 257 nM and 136 nM, respectively.	Epigenetics, 2019, 10.1080/15592294.2019.1656156
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.
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.	J Exp Clin Cancer Res, 2019, 38(1):383
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
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.
S7315	PFI-3 PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.	Front Genet, 2020, 11:80 Cell Death Dis, 2020, 11(7):549 Front Cell Dev Biol, 2020, 8:569	Western blot analysis of Brg1, α-SMA and Col1a1 expression in the presence of PFI-3(0uM, 5uM, 10uM,20uM,40uM,80uM) for 48 h in the indicated concentration in LX-2 cells.
S8409	KG-501 (2-naphthol-AS-E-phosphate) KG-501 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.	Cereb Cortex, 2020, 5 pii: bhaa062 Biomolecules, 2020, 9;10(4) pii: E580 J Cell Mol Med, 2020, 10.1111/jcmm.15723
S7582	Anacardic Acid Anacardic 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.	Oncogene, 2020, 39(18):3754-3773 Free Radic Biol Med, 2020, 10.1016/j.freeradbiomed.2020.01.016 Chemosphere, 2020, 247:125825	Western blot analysis of α-SMA expression in whole-lung lysates. Data are expressed as means ± SEM, *P < 0.05 versus vehicle and #P < 0.05 versus PQ (n = 4-6).
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.	Blood Cancer J, 2019, 9(2):4 Leuk Res, 2019, 77:42-50
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.
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.
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.	J Mol Cell Biol, 2020, 11;12(5):359-371
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.	Nat Commun, 2020, 11(1):3018 J Med Chem, 2020, 31 Cell Stem Cell, 2019, 24(1):123-137
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.	Cancer Res, 2018, 78(2):436-450
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).	Leuk Res, 2019, 77:42-50
S8344	AZD5153 AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4.	Mol Cancer Ther, 2019, 18(8):1439-1450 Int J Biol Sci, 2019, 15(9):1942-1954 Cancer Cell, 2018, 33(3):401-416
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.	Genome Res, 2019, 29(10):1659-1672
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.	J Mol Cell Biol, 2020, 11;12(5):359-371 Nature, 2019, 10.1038/s41586-019-1472-0 Cancer Cell, 2018, 33(3):401-416
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.	Leuk Res, 2019, 77:42-50
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
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.
S7681	OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with K_d of 100 nM and 500 nM, respectively.	J Mol Cell Biol, 2020, 11;12(5):359-371
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.

Catalog No.	Information	Product Use Citations	Product Validations
S0022^New	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.

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S0022^New

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.

Catalog No.	Information	Product Use Citations	Product Validations
S7088	UNC1215 UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and K_d of 120 nM, 50-fold selective versus other members of the human MBT family.	Cell Death Dis, 2018, Lab Invest, 2018, 98(12):1627-1641

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S7088

UNC1215

UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and K_d of 120 nM, 50-fold selective versus other members of the human MBT family.

Cell Death Dis, 2018,

Lab Invest, 2018, 98(12):1627-1641

Catalog No.	Information	Product Use Citations	Product Validations
S8889^New	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 Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.

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S8889^New

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 Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.

Catalog No.	Information	Product Use Citations	Product Validations
S8785^New	A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.

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S8785^New

A1874

A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.

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