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シグナル伝達経路

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阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
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-06405761) <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
S8297 ARV-825 <1 mg/mL 100 mg/mL 3 mg/mL
S8846 compound 3i (666-15) <1 mg/mL 100 mg/mL 3 mg/mL
S8739 PLX51107 <1 mg/mL 88 mg/mL <1 mg/mL
S8296 dBET1 ˂1 mg/mL 100 mg/mL 39 mg/mL
S8753 INCB054329(INCB-054329; INCB-54329) ˂1 mg/mL 70 mg/mL 70 mg/mL
S8762 dBET6 <1 mg/mL 100 mg/mL 42 mg/mL
S8714 INCB057643 <1 mg/mL 83 mg/mL <1 mg/mL
S5916 GSK 5959 <1 mg/mL 6 mg/mL 3 mg/mL
S8763 ZL0420 <1 mg/mL 59 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
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
S8409 KG-501 (2-naphthol-AS-E-phosphate) <1 mg/mL 20 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
S8723 ABBV-744 <1 mg/mL 98 mg/mL <1 mg/mL
S7088 UNC1215 <1 mg/mL 100 mg/mL 100 mg/mL

Epigenetic Reader Domain製品

新Epigenetic Reader Domain製品
製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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-06405761)

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

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.

S8574

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

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.

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.

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.

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).

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.

S8753

INCB054329(INCB-054329; INCB-54329)

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.

S8762

dBET6

dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.

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.

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.

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.

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.

S8179

BI-7273

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

S8190

CPI-637

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

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.

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.

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.

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

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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-06405761)

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

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.

S8574

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

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.

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.

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.

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).

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.

S8753

INCB054329(INCB-054329; INCB-54329)

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.

S8762

dBET6

dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.

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.

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.

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.

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.

S8179

BI-7273

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

S8190

CPI-637

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

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.

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.

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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

2018, 98(12):1627-1641