BET Chemicals

Cat.No.	Product Name	Information	Product Use Citations
E1664	GNE-987	GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. This compound inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines.	BMC Cancer, 2024, 928 Carcinogenesis, 2024, 424-435
E1177	CFT8634	CFT8634 is a potent BRD9 degrader with DC50 of 3 nM. It forms a ternary complex with BRD9 and an E3 ligase, resulting in BRD9 ubiquitination. This compound is used in the treatment of SMARCB1-perturbed cancers.	Blood, 2025, blood.2025029429
E1994	DBr-1	DBr-1 is a DCAF1-BRD9 PROTAC, created by linking the BRD9 binder BI-956448 to the DCAF1 scaffold via a piperidine-aliphatic carbon linker. It is a potent and selective degrader of BRD9 with a DC50 of 90 nM. It overcomes intrinsic resistance to VHL-degraders, positioning DCAF1-PROTACs as a promising strategy to counter ligase-mediated resistance.
E1926	IBG1	IBG1 (PROTAC BRD4 Degrader-19) is a PROTAC-like degrader specifically targeting BET bromodomains with a DC50 of 0.15 nM for BRD4. It consists of the BET inhibitor JQ1 linked to E7820 and functions through CRL4-DCAF16.
E1683	DN02	DN02 is a selective probe of BRD8 bromodomain family. It exhibits potency against BRD8(1) with a Kd of 32 nM, and interestingly, demonstrated this activity to be selective over BRD8's second bromodomain (BRD8(2) with a Kd of >1000 nM)
S7315	PFI-3	PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.	bioRxiv, 2025, nan Cell Rep, 2023, 42(2):112097 J Transl Med, 2023, 21(1):639