Epigenetic Reader Domain

Sigaling 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 RVX-208 <1 mg/mL 74 mg/mL <1 mg/mL
S8400 Mivebresib(ABBV-075) <1 mg/mL 91 mg/mL <1 mg/mL
S7853 CPI-0610 <1 mg/mL 73 mg/mL 12 mg/mL
S8190 CPI-637 <1 mg/mL 27 mg/mL <1 mg/mL
S8113 BI-9564 <1 mg/mL 3 mg/mL 16 mg/mL
S8179 BI-7273 <1 mg/mL 70 mg/mL 70 mg/mL
S7835 I-BRD9 <1 mg/mL 99 mg/mL <1 mg/mL
S8180 PF-CBP1 HCl 100 mg/mL 100 mg/mL 100 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
S7088 UNC1215 <1 mg/mL 100 mg/mL 100 mg/mL
S7360 OTX015 <1 mg/mL 98 mg/mL 98 mg/mL
S7373 UNC669 <1 mg/mL 11 mg/mL 68 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
S7315 PFI-3 <1 mg/mL 64 mg/mL <1 mg/mL
S7620 GSK1324726A (I-BET726) <1 mg/mL 86 mg/mL 86 mg/mL
S7681 OF-1 <1 mg/mL 76 mg/mL <1 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.

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.

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.

S7295

RVX-208

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.

S8400New

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).

S7853New

CPI-0610

CPI-0610 is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor and currently undergoing human clinical trials for hematological malignancies.

S8190New

CPI-637

CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.

S8113New

BI-9564

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.

S8179New

BI-7273

BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor.

S7835New

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.

S8180New

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.

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.

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.

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.

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.

S7315

PFI-3

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

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.

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.

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.

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.

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.

S7295

RVX-208

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.

S8400New

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).

S7853New

CPI-0610

CPI-0610 is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor and currently undergoing human clinical trials for hematological malignancies.

S8190New

CPI-637

CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.

S8113New

BI-9564

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively.

S8179New

BI-7273

BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor.

S7835New

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.

S8180New

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.

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.

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.

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.

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.

S7315

PFI-3

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

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.

S7681

OF-1

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

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 Kd of 120 nM, 50-fold selective versus other members of the human MBT family.