GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media.

GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases.

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.

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.

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.

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-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).

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

Ziftomenib is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).

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.

I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

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

SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity.

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.

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

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).

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.

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).

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.

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.

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.