Epigenetic Reader Domain

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S7110 (+)-JQ1 <1 mg/mL 91 mg/mL 91 mg/mL
S2780 I-BET151 (GSK1210151A) <1 mg/mL <1 mg/mL 27 mg/mL
S1216 PFI-1 (PF-6405761) <1 mg/mL 69 mg/mL <1 mg/mL
S7189 I-BET-762 <1 mg/mL 84 mg/mL 42 mg/mL
S7295 Apabetalone (RVX-208) <1 mg/mL 74 mg/mL <1 mg/mL
S8723 ABBV-744 <1 mg/mL 98 mg/mL <1 mg/mL
S8409 KG-501 (2-naphthol-AS-E-phosphate) <1 mg/mL 20 mg/mL <1 mg/mL
S7256 SGC-CBP30 <1 mg/mL 100 mg/mL 100 mg/mL
S7233 Bromosporine <1 mg/mL 81 mg/mL <1 mg/mL
S7360 OTX015 <1 mg/mL 98 mg/mL 98 mg/mL
S7373 UNC669 <1 mg/mL 11 mg/mL 68 mg/mL
S8179 BI-7273 <1 mg/mL 70 mg/mL 70 mg/mL
S8190 CPI-637 <1 mg/mL 27 mg/mL <1 mg/mL
S7853 CPI-0610 <1 mg/mL 73 mg/mL 12 mg/mL
S7304 CPI-203 <1 mg/mL 79 mg/mL 5 mg/mL
S7305 MS436 <1 mg/mL 55 mg/mL 1 mg/mL
S7906 PFI-4 <1 mg/mL 17 mg/mL 5 mg/mL
S7231 GSK2801 <1 mg/mL 74 mg/mL 7 mg/mL
S8589 SF2523 <1 mg/mL 29 mg/mL 7 mg/mL
S7315 PFI-3 <1 mg/mL 64 mg/mL <1 mg/mL
S8400 Mivebresib(ABBV-075) <1 mg/mL 91 mg/mL <1 mg/mL
S8265 GSK6853 <1 mg/mL 81 mg/mL 81 mg/mL
S8496 EED226 <1 mg/mL 73 mg/mL <1 mg/mL
S8180 PF-CBP1 HCl 100 mg/mL 100 mg/mL 100 mg/mL
S8344 AZD5153 <1 mg/mL 100 mg/mL 27 mg/mL
S7835 I-BRD9 <1 mg/mL 99 mg/mL <1 mg/mL
S7620 GSK1324726A (I-BET726) <1 mg/mL 86 mg/mL 86 mg/mL
S8113 BI-9564 <1 mg/mL 3 mg/mL 16 mg/mL
S7681 OF-1 <1 mg/mL 76 mg/mL <1 mg/mL
S7088 UNC1215 <1 mg/mL 100 mg/mL 100 mg/mL
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.
Gastroenterology, 2014, 147(5):1119-33
Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-15-2448
Cancer Res, 2016, 76(11):3319-31
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.
Theranostics, 2016, 6(2):219-30
J Immunol, 2018, 201(9):2744-2752
Oncotarget, 2016, 7(3):2545-54
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.
S7189

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.
Cancer Res, 2018, 78(15):4331-4343
Oncotarget, 2016, 7(24):35753-35767
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.
Biochemical and Biophysical Research Communications, 2016, 10.1016/j.bbrc.2016.03.013
S8723New

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.
S8409New

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.
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, 2018, 175(1):186-199
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.
S7360

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.

Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1040
Clin Cancer Res, 2018, 24(16):3941-3954
J Exp Clin Cancer Res, 2018, 37(1):241
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.
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.

S7853

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.
S7304

CPI-203

CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.

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.

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 KD of 257 nM and 136 nM, respectively.

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.

S7315

PFI-3

PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.

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).
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.
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.
S8344

AZD5153

AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4.
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.
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.

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.
S7681

OF-1

OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.

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.