Epigenetic Reader Domain
Catalog No. | Inhibitor Name | Epigenetic Reader Domain |
---|---|---|
A12729 | (*)-JQ1 | *** |
A11783 | I-BET151 | * |
A12545 | PFI-1 | ** |
A11440 | I-BET-762 | *** |
A13956 | RVX-208 | * |
A13227 | SGC-CBP30 | **** |
A13163 | Bromosporine | **** |
A13890 | OTX015 | **** |
A12948 | UNC1215 | ** |
A13717 | UNC669 | * |
A14133 | GSK1324726A | *** |
A13749 | MS436 | ** |
A13068 | CPI-203 | *** |
A13957 | PFI-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.
-
CD235
Catalog No. A19115 BET bromodomain inhibitorCD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor. Learn More -
BI-7273
Catalog No. A16068 BRD9 BD InhibitorBI-7273 is a selective, and cell-permeable BRD9 BD inhibitor. Learn More -
BI-9564
Catalog No. A16196 BRD7/9 inhibitorBI-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). Learn More -
VZ185
Catalog No. A18685 dual BRD7/9 PROTAC degraderVZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively. Learn More -
ZXH-3-26
Catalog No. A18399 PROTAC BRD4 degraderZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM. Learn More -
(E)-ZL0420
Catalog No. A20136 BRD4 inhibitorZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. Learn More -
ZL0454
Catalog No. A20123 BRD4 inhibitorZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2. Learn More -
BMS-986158
Catalog No. A19442 Bromodomain inhibitorBMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. Learn More -
MS417
Catalog No. A19433 BRD4 inhibitorMS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). Learn More -
MZP-54
Catalog No. A19426 BRD3/4 degraderMZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2. Learn More -
MZP-55
Catalog No. A19415 BRD3/4 degraderMZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. Learn More -
dBET57
Catalog No. A19133 BRD4BD1degraderdBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. Learn More -
PFI-1
Catalog No. A12545 BET inhibitorPFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. Learn More -
BETd-246
Catalog No. A18913 BRD inhibitorBETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity. Learn More -
Bromodomain IN-1
Catalog No. A18845 Bromodomain inhibitorBromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . Learn More -
BRD4 Inhibitor-10
Catalog No. A18679 BRD4-BD1 inhibitorBRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM. Learn More -
GSK9311
Catalog No. A12453 inhibitor of the BRPF bromodomainGSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively. Learn More -
BET-IN-1
Catalog No. A12141 Bromodomain inhibitorBET-IN-1 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 Learn More -
GS-626510
Catalog No. A13305 BET family bromodomains inhibitorGS-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. Learn More -
(Rac)-BAY1238097
Catalog No. A21598 BET inhibitor(Rac)-BAY1238097 is a BET inhibitor, with an IC50 of 1.02 μM for BRD4. Used in cancer research. Learn More -
INCB054329 Racemate
Catalog No. A21609 -
CPI-0610 carboxylic acid
Catalog No. A21714 BET inhibitorCPI-0610 carboxylic acid is a potent bromodomain and extra-terminal (BET) protein inhibitor. CPI-0610 carboxylic acid has the potential in the therapy of multiple myeloma. Learn More -
AZD5153 6-Hydroxy-2-naphthoic acid
Catalog No. A21852 BET/BRD4 bromodomain inhibitorAZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. Learn More -
Molibresib besylate
Catalog No. A21855 BET bromodomain inhibitorMolibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. Learn More -
I-CBP112
Catalog No. A13165 CBP/p300 bromodomain inhibitorI-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). Learn More -
I-BRD9
Catalog No. A15872 Selective BRD9 inhibitorI-BRD9 is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4. Learn More -
MS436
Catalog No. A13749 BRD4 inhibitorMS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM. Learn More -
UNC1215
Catalog No. A12948 L3MBTL3 inhibitorUNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity. Learn More -
OTX015
Catalog No. A13890 BET inhibitorOTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM). Learn More -
SGC-CBP30
Catalog No. A13227 CBP/p300 bromodomain inhibitorSGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators. Learn More -
(+)-JQ1
Catalog No. A12729 BET Inhibitor(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor. Learn More -
UNC 669
Catalog No. A13717 L3MBTL inhibitorUNC669 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) Learn More -
GSK 1210151A (I-BET151)
Catalog No. A11783 BET Bromodomain InhibitorGSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4. Learn More -
CPI-203
Catalog No. A13068 BET bromodomain InhibitorCPI203 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). Learn More -
GSK 525762A (I-BET-762)
Catalog No. A11440 BET inhibitorGSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family Learn More -
Bromosporine
Catalog No. A13163 bromodomain inhibitorBromosporine 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. Learn More -
(-)-JQ1
Catalog No. A14160 BET bromodomain inhibitorThe 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. Learn More -
UNC 926 hydrochloride
Catalog No. A15367 MBT Domain (L3MBTL1) InhibitorUNC 926 is a methyl lysine reader domain inhibitor. Learn More -
P300/CBP-IN-3
Catalog No. A18544 p300/CBP histone acetyltransferase inhibitorP300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. Learn More -
BRD-IN-3
Catalog No. A18454 BRD inhibitorBRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ. Learn More -
Apabetalone (RVX-208)
Catalog No. A13956 BET bromodomain inhibitorRVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 uM for BD2, about 170-fold selectivity over BD1. Learn More -
GNE-049
Catalog No. A20206 CBP inhibitorGNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. Learn More -
PFI-3
Catalog No. A13957 SMARCA bromodomains probePFI-3 is a selective chemical probe for SMARCA bromodomains. Learn More -
Anacardic Acid
Catalog No. A14226 KAT5 (Tip60), p300/PCAF inhibitorAnacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. Learn More -
GSK 525768A
Catalog No. A14134 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. Learn More -
GSK1324726A (I-BET726)
Catalog No. A14133 BET inhibitorGSK1324726A (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). Learn More -
ZEN-3219
Catalog No. A19367 BET inhibitorZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4. Learn More -
GSK2801
Catalog No. A14015 BAZ2A and BAZ2B inhibitorGSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins Learn More -
GNE-207
Catalog No. A18844 CBP bromodomain inhibitorGNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile. Learn More -
SF1126
Catalog No. A12704 Pan PI3K inhibitorSF1126 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. Learn More