Epigenetic Reader Domain

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Epigenetic Reader Domain Products

All (43) Epigenetic Reader Domain Inhibitors (40) Epigenetic Reader Domain Antagonists (1) Epigenetic Reader Domain Chemicals (2) New Epigenetic Reader Domain Products

Catalog No.	Information	Product Use Citations	Product Validations
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 Aging (Albany NY), 2020, 12(5):4547-4557	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 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.	Front Immunol, 2019, 1.1243055556 World J Urol, 2019, 37(2):343-349 Nat Commun, 2017, 8:14802
S7189	Molibresib (I-BET-762) I-BET-762 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 J Hematol Oncol, 2019, 12(1):73 EBioMedicine, 2019, 43:201-210	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.
S7295	Apabetalone (RVX-208) Apabetalone (RVX-208) 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.	Cell Rep, 2019, 27(11):3331-3344 Oncogene, 2018, 37(49):6341-6356 J Virol, 2018, 92(10)	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.
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 BI894999 is a novel potent and selective BET inhibitor with IC50 values of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI894999 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.
S8766^New	AT1 AT1 is highly selective Brd4 degrader which is a designed molecule based on the crystal structures of MZ1 bound to BRD4 as well as models of VHL proteins.
S8846^New	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.
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.	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
S8762	dBET6 dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.
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.
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.
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.
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 Nat Commun, 2019, 10(1):1551 Genome Res, 2019, 29(10):1659-1672	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 Biochem Mol Toxicol, 2019, 33(7):e22333
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).	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.
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 Stem Cell, 2019, 24(1):123-137 Cancer Cell, 2019, 36(4):385-401 Int J Cancer, 2019, 145(2):415-426
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.	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
S7681	OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with K_d of 100 nM and 500 nM, respectively.
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.
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.	Lab Invest, 2018, 98(12):1627-1641
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.
S8297^New	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

Catalog No.	Information	Product Use Citations	Product Validations
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 Aging (Albany NY), 2020, 12(5):4547-4557	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 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.	Front Immunol, 2019, 1.1243055556 World J Urol, 2019, 37(2):343-349 Nat Commun, 2017, 8:14802
S7189	Molibresib (I-BET-762) I-BET-762 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 J Hematol Oncol, 2019, 12(1):73 EBioMedicine, 2019, 43:201-210	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.
S7295	Apabetalone (RVX-208) Apabetalone (RVX-208) 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.	Cell Rep, 2019, 27(11):3331-3344 Oncogene, 2018, 37(49):6341-6356 J Virol, 2018, 92(10)	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.
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 BI894999 is a novel potent and selective BET inhibitor with IC50 values of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI894999 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.
S8766^New	AT1 AT1 is highly selective Brd4 degrader which is a designed molecule based on the crystal structures of MZ1 bound to BRD4 as well as models of VHL proteins.
S8846^New	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.
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.	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
S8762	dBET6 dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.
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.
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.
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.
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 Nat Commun, 2019, 10(1):1551 Genome Res, 2019, 29(10):1659-1672	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 Biochem Mol Toxicol, 2019, 33(7):e22333
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).	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.
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 Stem Cell, 2019, 24(1):123-137 Cancer Cell, 2019, 36(4):385-401 Int J Cancer, 2019, 145(2):415-426
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.	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
S7681	OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with K_d of 100 nM and 500 nM, respectively.
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
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.	Lab Invest, 2018, 98(12):1627-1641

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.

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

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.
S8297^New	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

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.

S8297^New

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

Choose Your Country or Region

By Signaling Pathways

By product type

Epigenetic Reader Domain

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Epigenetic Reader Domain Products