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.

I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.

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

GNE-375 is a selective and potent BRD9 inhibitor (IC50: 5 nM).GNE-375 inhibits BRD4, TAF1, and CECR2, and can be used to study epigenetic resistance.

BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.

TP-472 is a selective inhibitor of BRD9 (Kd: 33 nM).

GSK8573 is an inactive control compound for GSK2801, with binding activity to BRD9 (Kd of 1.04 μM).

LP99 is an epigenetic probe. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. LP99 is an effective and selective inhibitor of the BRD7 and BRD9 bromodomains (Kd: 99 nM against BRD9).

NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM). It also has excellent selectivity over nonclass IV BRD protei

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].

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.

BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 μM.

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.