YDR1 is a potent, selective and orally bioavailable Cereblon-based PROTAC and a degrader of SMARCA2 with DC50 of 60 nM at 48 hours. It exhibits antitumor activity in SMARCA4-mutant lung cancer xenograft models and can be used in research on non-small cell lung cancer.

YD54 is a potent, selective and orally bioavailable PROTAC and a degrader of SMARCA2 with DC50 of 8.1 nM at 24 hours. It exhibits antitumor activity in SMARCA4-mutant lung cancer xenograft models and can be used in research on non-small cell lung cancer.

Y16526 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.03 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).

Y16524 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.01 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).

XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .

TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 and class I HDAC inhibitor CI994. TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine.

trans-BAY-850 is the trans isomer of BAY-850.

SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model.

PBRM1/SMARCA2,4 binder-1 is a binder of PBRM1, SMARCA2, and SMARCA4 (IC50: 0.083, 0.153, and 0.046 μM, respectively).

JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model.

iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models.

Hyp-dBET1 is a PROTAC degrader targeting BRD4. Hyp-dBET1 has an IC50 value of 3.4 μM in MDA-MB-231 cells. Hyp-dBET1 can be activated by hypoxia and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.

HRG038 is a selective covalent BRD4 degrader. HRG038 binds covalently to the E3 ubiquitin ligase CUL4 DCAF16, recruiting it to BRD4, leading to the ubiquitination and subsequent proteasomal degradation of BRD4. HRG038 is promising for research of cancers.

G-6599 is a SMARCA2/A4 target-anchored monovalent degrader with DC50 values of 0.018 nM and 0.056 nM, respectively. G-6599 has degradation activity and anti-proliferative effects in AR-dependent prostate cancer cell lines.

DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity.

Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.

Balomenib is the inhibitor for menin-MLL interaction, that inhibits the interaction between men1-MLL4-43 with an IC50 < 0.075 μM. Balomenib inhibits the growth of MV4-11 (CC50 < 0.1 μM), MOLM-13 (CC50 0.1~0.5 μM) and HEK293 (CC50 < 2 μM). Balomenib exhibits antineoplastic activity.

(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD).

UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM.

ET-JQ1-OH is an allele-specific BET inhibitor.

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

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

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

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.

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).

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.

Trotabresib (CC-90010) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.

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.

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

GNE-064 (compound 5) is a selective, oral and highly soluble inhibitor of the SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.