brd7, brd9

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

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

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.

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].

BD-IN-1, a pan bromodomain (BD) inhibitor, exhibits K_D values of 250 nM for BRD4(1), 420 nM for CBP, 130 nM for BRPF1B, 430 nM for BRD7, 67 nM for BRD9, 240 nM for BRDT(1), and 970 nM for CECR2, respectively. This compound demonstrates antiproliferative activity [1].

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

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].

VZ185 is an effective and selective dual BRD7 9 PROTAC degrader (DC50s: 4.5 and 1.8 nM, respectively).

BRD7-IN-2 (compound 2-77) is a potent, selective inhibitor of bromodomain-containing protein 7 (BRD7) with an IC50 of 5.4 μM and exhibits significant anti-proliferative activity in prostate cancer cells, while demonstrating weak inhibition of BRD9 with an IC50 of >300 μM.

BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7 and BRD9, with half-maximal inhibitory concentrations (IC50s) of 1.6 μM for BRD7 and 2.7 μM for BRD9, respectively [1].

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

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.

NVS-CECR2-1 is a selective cat eye syndrome chromosome region candidate 2 (CECR2) inhibitor with antitumor activity and inhibits chromatin binding of CECR2 BRD. NVS-CECR2-1 is cytotoxic and can induce apoptosis.