brd9

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.

PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.

PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.

VZ185 is a potent, fast-acting, and selective von Hippel–Lindau–based dual degrader probe targeting BRD9 and BRD7 with DC50 values of 4.5 nM and 1.8 nM, respectively. VZ185 displays marked cytotoxicity in EOL-1 and A-402 cell lines with EC50 values of 3 nM and 40 nM, enabling advanced studies of chromatin remodeling, targeted protein degradation, and cancer cell dependency on SWI/SNF complex components.

BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7/9 with DC50 values of 4.5 and 1.8 nM, respectively [1].

CFT8634 is an orally active and selective degrader targeting BRD9, with effects on the proliferation of SMARCB1-deficient cancer cell lines. CFT8634 induces the formation of a ternary complex with BRD9 and E3 ligase, inducing BRD9 ubiquitination and subsequent degradation by the proteasome.

BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), interacts with a VHL ligand via a linker to form the PROTAC VZ185 (targeting BRD7/9 with DC50 values of 4.5 and 1.8 nM, respectively)[1].

BRD9 ligand-7 acts as the target protein ligand for PROTAC (Ligand for Target Protein for PROTAC) and is utilized in the synthesis of BRD9 Degrader-1.

PROTACBRD9 Degrader-8 (compound E5) is a PROTAC-based BRD9 degrader with a DC50 value of 16 pM. It exhibits antiproliferative effects in MV4–11 cells with an IC50 of 0.27 nM and in OCI-LY10 cells with an IC50 of 1.04 nM.

PROTAC BRD9 Degrader-4 is a bifunctional degrader that targets BRD9, specifically designed for applications in cancer research.

PROTAC BRD9 Degrader-6, with an IC50 value of 0.13 nM, is a potent degrader of BRD9 suitable for research on BAF complex-related disorders [1].

PROTAC BRD9 Degrader-7 is a selective and orally active BRD9 degrader with a DC50 of 1.02 nM and demonstrates superior pharmacokinetics, evidenced by a Cmax of 3436.95 ng/mL [1].

PROTAC BRD9 Degrader-5 is a proteolysis targeting chimera (PROTAC) designed to specifically degrade Bromodomain-containing protein 9 (BRD9).

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, used in cancer research.

PROTAC BRD9 Degrader-2 is a bifunctional compound engineered for the targeted degradation of BRD9 (Bromodomain containing 9) in cancer research applications.

BRD9 Degrader-1 functions as a BRD9 degrader, demonstrating micromolar binding affinity towards BRD9 and nanomolar affinity for the ternary complex involving BRD9 and VCB [1].

BRD9 Degrader-2 (Compound B11), a potent BRD9 degrader (DC50≤1.25nM; Dmax≥75%), is applicable in cancer research.

BRD9 Ligand-5 (Compound 172-11) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CFT8634.

BRD9 ligand-6 serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of FHD-609.

PROTAC BRD9-binding moiety 5, a selective binder of BRD9 with an IC50 value of 4.20 μM, is utilized in PROTAC synthesis and exhibits antiproliferative activity against cancer cells [1].

BRD9 Degrader-3 (compound B20) is a molecular glue for BRD9 with a DC50 of less than 1.25 nM.

BRD9 Degrader-4 (BRD9c) is a bifunctional molecule that acts as an effective BRD9 degrader with a DC50 value of ≤25 nM. It exhibits anticancer properties.

dBRD9 is a PROTAC. dBRD9 is a double-acting molecule, partially containing Bromodomain-containing protein 9 (BRD9), ligand that recruits the cereblon E3 ubiquitin ligase. Ligand that recruits the cereblon E3 ubiquitin ligase. dBRD9 can inhibit the degradation of BRD9 in MOLM-13 cells, and the IC50 is 104 nM.