Epigenetic Reader Domain

Cat. No.

A12729

CAS No.

1268524-70-4

(+)-JQ1

(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.

Cat. No.

A11783

CAS No.

1300031-49-5

GSK 1210151A (I-BET151)

Synonyms: I-BET151

GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.

Cat. No.

A12545

CAS No.

1403764-72-6

PFI-1

PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.

Cat. No.

A13068

CAS No.

1446144-04-2

CPI-203

CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).

Cat. No.

A13227

CAS No.

1613695-14-9

SGC-CBP30

SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.

Cat. No.

A14133

CAS No.

1300031-52-0

GSK1324726A (I-BET726)

Synonyms: I-BET726

GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).

Cat. No.

A15856

CAS No.

1422253-38-0

Foscenvivint (PRI-724)

Synonyms: PRI 724

PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.

Cat. No.

A20579

CAS No.

202592-23-2

JQ1 (carboxylic acid)

JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.

Cat. No.

A11440

CAS No.

1260907-17-2

Molibresib (GSK 525762A, I-BET-762)

Synonyms: GSK-525762A; I-BET-762

GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family

Cat. No.

A12141

CAS No.

1422554-34-4

I-BET282

I-BET282 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0. IC50 value: 6.0 - 7.0 (plC50) Target: bromodomain

Cat. No.

A12453

CAS No.

1923851-49-3

GSK9311

GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.

Cat. No.

A12474

CAS No.

1936428-93-1

GNE-272

GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.

Cat. No.

A12655

CAS No.

2018300-62-2

TPOP146

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

Cat. No.

A12704

CAS No.

936487-67-1

SF1126

SF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities.

Cat. No.

A12764

CAS No.

1629277-36-6

PNZ5

PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).

Cat. No.

A13163

CAS No.

1619994-69-2

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.

Cat. No.

A13165

CAS No.

1640282-31-0

I-CBP112

I-CBP112 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.14-0.17 uM for CBP and ~0.625 uM for p300).

Cat. No.

A13305

CAS No.

1637770-13-8

GS-626510

GS-626510 is a potent, and orally bioavailable BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively.

Cat. No.

A13383

CAS No.

1800477-30-8

IACS-9571

Synonyms: ASIS-P040

IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

Cat. No.

A13451

CAS No.

900305-37-5

PF-4

PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4.

Cat. No.

A13749

CAS No.

1395084-25-9

MS436

MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.

Cat. No.

A13890

CAS No.

202590-98-5

Birabresib (OTX015)

Synonyms: OTX 015

OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).

Cat. No.

A13956

CAS No.

1044870-39-4

Apabetalone (RVX-208)

Synonyms: RVX-000222; RVX-208

RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 uM for BD2, about 170-fold selectivity over BD1.

Cat. No.

A14015

CAS No.

1619994-68-1

GSK2801

GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins

Cat. No.

A14134

CAS No.

1260530-25-3

GSK 525768A

GSK 525768A is the enantiomer compound of GSK 525762A, which is a potent small molecule inhibitor that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4); GSK 525768A has NO activity towards BET.