PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.

(R,S)-CFT8634 is a selective and orally active BRD9 protein degrader. (R,S)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 176).

(R,R)-CFT8634 is a selective and orally active BRD9 protein degrader. (R,R)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 175).

FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70).

FHT-1205 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 67).

BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders.

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.

OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively.

UNC6864 (Kei), an ethylisopropyllysine (Kei)-containing ligand, binds to wild-type CBX5, with a KD of 3.3 μM.

UNC6349 (Ket2), a diethyllysine (Ket2)-containing ligand, binds to wild-type CBX5, with a KD of 3.2 μM.

UNC6212 (Kme2), a dimethyllysine (Kme2)-containing ligand, has a KD for CBX5 of 5.7 μM.

Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for BRD4.

BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.

BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.

BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2).

Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.

ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities.

Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer.

BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5).

ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.

Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1).

GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.

I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.

NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.

GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC50 = 7.9).

Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6).

L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.

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.

MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.

ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4.