PBRM1-BD2-IN-4 (compound 15) is a potent PBRM1 Bromodomain inhibitor with Kd values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.2 μM for PBRM1-BD2. PBRM1-BD2-IN-4 can be used to research anticancer[1].
BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively.
BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC50 of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases[1].
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins.
OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50value of 382 nM[1].
I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that targets the CBP/p300 bromodomains.
Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia[1].
GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively[1].
I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].
A novel a potent, selective inhibitor of BRD4 with Kd of 550 nM, cellular IC50 of 724 nM; also potently binds to the TAF1 (560 nM) and TAF1L (1.3 uM) bromodomains; significantly induces HIV-1 reactivation.
BRM/BRG1 ATP Inhibitor-4 is a BRG1/BRM inhibitor. BRM/BRG1 ATP Inhibitor-4 can be used for the research of cancers and BAF complex-related disorders[1].
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1[1].
A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4; shows an excellent selectivity over other non-BET bromodomain-containing proteins with the exception of CREBBP (Kd=670 nM); potently and selectively inhibits cell growth in human acute leukemia cell lines harboring the rearranged MLL1 gene (IC50=20 nM for MV4;11 cells).
BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM[1].
HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6[1].
A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer[1].
E3 Ligase Ligand-Linker Conjugates 21 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
Target Protein-binding moiety 4 is a BRD4(1) inhibitor with an IC50 of 7.9 μM.
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.
PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition[1].
CBP-IN-1 (compound 12) is a potent CBP inhibitor, with an IC50 of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4(1), with IC50 values of 690 and 3100 nM, respectively[1].
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
CPI-0610 is a potent, selective, and cell-active BET bromodomain inhibitor CPI-0610 inhibits BRD4-BD1 with IC50 of 39 nM in time-resolved fluorescence energy transfer (TR-FRET ) binding assay. IC50 value: 39 nMTarget: Bromodomains in vitro: CPI-0610 is about 6 times more potent against BET BD-2 than against BET BD-1. When tested on other members of the bromodomain family, CPI-0610 is remarkably selective, displaying essentially no activity in TR-FRET- or AlphaLisa-based assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 of >20 μM, >80 μM, >20 μM, >20 μM, >20 μM, >80 μM, >20 μM, and >15 μM, respectively), among others. In a CEREP express panel of about 50 GPCRs, ion channels, and transporters, the compound displayed no meaningful inhibition. CPI-0610 also displays negligible inhibition of cytochrome P450 activity when tested at 10 μM against a number of common isoforms, and it also showed no time-dependent inhibition.[1] in vivo: The t1/2 of CPI-0610 for the rat and dog is 0.93 and 9 h, respectively.[1]
EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
DZNep (3-Deazaneplanocin A) is a potent histone methyltransferase EZH2 inhibitor.