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.
SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts[1][2].
PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT[1].
ZXH-3-26 is a selective BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM[1].
UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM[1].
PLX51107 is a potent and selective BET inhibitor, with Kds of 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; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.
BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC50 of 14.1 µM[1].
UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM[1].
GNE-375 is a potent, selective BRD9 inhibitor with IC50 of 5 nM, displays >480-fold selectivity over BRD4, CECR2, and TAF1; decreases BRD9 binding to chromatin, and decreases expression of ALDH1A1, a gene previously shown to be important in drug tolerance; shows remarkable potency in preventing the emergence of a drug tolerant population in EGFR mutant PC9 cells treated with EGFR inhibitors.
QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].
ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.
E-7386 is an orally active CBP/beta-catenin modulator.
BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively)[1].
Curcumin D6 (Diferuloylmethane D6) is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
BET-IN-7 (Compound 1) is a potent inhibitor of BET with a Ki and Kd of 12.27 and 89.3 μM, respectively. BET-IN-7 has the potential for the research of sepsis[1].
MS417 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).
XD14 is a BET bromodomain inhibitor with Kd values of 160, 170, 380, 490, 830 and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2) respectively.
HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is a PROTAC BET degrader. Antitumor activity[1].
ZEN-2759 is BRD4(BD1) inhibitor.
LP99 is the first potent and selective BRD7/9 bromodomain inhibitor with Kd of 99 nM for BRD9; inhibits IL‐6 secretion from THP‐1 cells in a dose‐dependent manner; decreases BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose‐dependent manner, with cellular IC50 values in the low micromolar range for both histones.
CFT8634 is a degrader targeting BRD9 extracted from patent WO2021178920A1 compound 173. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors[1].
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity[1][2].
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation[1].
Menin-MLL inhibitor 21(example 9) is a specific irreversible inhibitor of Menin-MLL interactions and can be used in the study of autoimmune diseases, alloimmune diseases, cancer and other diseases dependent on menin-MLL[1].
GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) andgreater than 1600-fold selectivity over all other bromodomainstested.target: BRPF1.[1]In vivo: The ip route of administration would be suitable for dosing GSK6853 in potential PK/PD models. [1]
6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways[1]. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons[2].