brd7

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].

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].

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

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.

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

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].

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.

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

BRD7116 competitively binds to bacterial DNA gyrase, exhibiting cell-non-autonomous anti-leukemia activity.

BRD7539B is a Dihydroorotate dehydrogenase (DHODH) inhibitor . RD7539 shows to target PfDHODH (IC50 = 0.033 μM) selectively over human (Hs) DHODH (IC50 > 50 μM).

BRD73954, an effective and specific HDAC inhibitor, which is with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

BRD7552 is an inducer of transcription factor PDX1, which increases insulin expression. BRD7552 increases PDX1 expression in mouse αTC cells but not βTC cells.

BRD7929 is a multistage antimalarial inhibitor for single-dose treatment of malaria in mouse models.

BRD73842 is an inhibitor of Plasmodium PI4K.

BRD7586 is a cell-permeable small molecule inhibitor of SpCas9 that enhances SpCas9 specificity.

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

SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.

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.

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.

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].

BMS-986202 is a novel Tyk2 inhibitor, binding to Tyk2 JH2, showing efficacies for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.

ARL-67085 is a P2T (P2YADP) purinoceptor antagonist.

BRD-7880 is a potent and highly specific inhibitor of aurora kinases B and C.