GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620

I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.

QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines.

PROTAC_ERRα is a potent and selective ERRα degrader. PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%.

(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion.

OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM.

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.

MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM.

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.

BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information.

BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.

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).