Epigenetic Reader Domain

Inhibitory Selectivity
Catalog No.Inhibitor Name Epigenetic Reader Domain
A12729(*)-JQ1
***
A11783I-BET151
*
A12545PFI-1
**
A11440I-BET-762
***
A13956RVX-208
*
A13227SGC-CBP30
****
A13163Bromosporine
****
A13890OTX015
****
A12948UNC1215
**
A13717UNC669
*
A14133GSK1324726A
***
A13749MS436
**
A13068CPI-203
***
A13957PFI-3

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



38 Item(s)

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Catalog No. Product Name Application Product Information
A11783 SALE

GSK 1210151A (I-BET151)

BET Bromodomain Inhibitor
GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.
A16196 SALE

BI-9564

BRD7/9 inhibitor
BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 uM, respectively).
A16068

BI-7273

BRD9 BD Inhibitor
BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor.
A15872

I-BRD9

Selective BRD9 inhibitor
I-BRD9 is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
A13749

MS436

BRD4 inhibitor
MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.
A13165 SALE

I-CBP112

CBP/p300 bromodomain inhibitor
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).
A12948 SALE

UNC1215

L3MBTL3 inhibitor
UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.
A13890 SALE

OTX015

BET inhibitor
OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).
A13227

SGC-CBP30

CBP/p300 bromodomain inhibitor
SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
A12545 SALE

PFI-1

BET inhibitor
PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
A11440 SALE

GSK 525762A (I-BET-762)

BET inhibitor
GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family
A13068

CPI-203

BET bromodomain Inhibitor
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).
A13163 SALE

Bromosporine

bromodomain inhibitor
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.
A13717

UNC 669

L3MBTL inhibitor
UNC669 is a small-molecule antagonist of methyl-lysine (KMe) reader protein with selectivity for L3MBTL1 and L3MBTL3 (IC50 of 4.2μM and 3.1μM respectively)
A12729 SALE

(+)-JQ1

BET Inhibitor
(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
A15947

BAZ2-ICR

BAZ2 bromodomain inhibitor
BAZ2-ICR is an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.
A16000

OF-1

BRPF1B/BRPF2 bromodomain inhibitor
OF-1 is a chemical probe for BRPF bromodomains. OF-1 has been shown to bind to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 uM (ITC).
A16076

CPI 0610

BET bromodomain inhibitor
CPI 0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity.
A16092

GSK 5959

BRPF1 bromodomain inhibitor
GSK 5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
A16180

EML 425

CBP/p300 inhibitor
EML 425 is a reversible and non-competitive CBP/p300 inhibitor that is cell permeable (IC50 values are 1.1 and 2.9 uM, respectively).
A16330

GSK6853

BRPF1 bromodomain inhibitor
GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested.
A16355

CeMMEC13

TAF1 inhibitor
CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 μM).
A16366

OXF BD 02

BRD4 inhibitor
OXF BD 02, selective inhibitor of the first bromodomain of BRD4 (BRD4(1)) (IC50 = 382 nM). Exhibits 2-3-fold selectivity for BRD4(1) over the CBP bromodomain and has little affinity for a range of other bromodomains.
A16367

GW841819X

BET Inhibitor
GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring 3.
A16368

BET-BAY 002

BET inhibitor
BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
A15876

PF-CBP1

CREBBP inhibitor
PF-CBP1 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.
A13451

PF-4

BRPF1 bromodomain inhibitor
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.
A12704

SF1126

Pan PI3K inhibitor
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.
A12815

C646

p300/CBP inhibitor
C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
A14015 SALE

GSK2801

BAZ2A and BAZ2B inhibitor
GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins
A14160 SALE

(-)-JQ1

BET bromodomain inhibitor
The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes.
A14133 SALE

GSK1324726A

BET inhibitor
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).
A14134

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.
A14226

Anacardic Acid

KAT5 (Tip60), p300/PCAF inhibitor
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases.
A13957

PFI-3

SMARCA bromodomains probe
PFI-3 is a selective chemical probe for SMARCA bromodomains.
A13956 SALE

RVX-208

BET bromodomain inhibitor
RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 uM for BD2, about 170-fold selectivity over BD1.
A15367

UNC 926 hydrochloride

MBT Domain (L3MBTL1) Inhibitor
UNC 926 is a methyl lysine reader domain inhibitor.
A16470

CPI-637

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

38 Item(s)

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