bromodomain in 1

Bromodomain IN-1 is an inhibitor of Bromodomain.

CBP EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor targeting the bromodomain receptors of CBP EP300, demonstrating nanomolar-level binding affinity with proteins possessing bromodomains.

P300 bromodomain-IN-1 is a potent inhibitor of p300 (EP300) bromodomain (IC50: 49 nM). p300 bromodomain-IN-1 blocks c-Myc expression and induces cell cycle arrest at G1 G0 phase and apoptosis in OPM-2 cells. apoptosis).

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1, a BET bromodomain inhibitor, which acts on BRD4(1 2) with IC50 values of 77 nM and 33 nM in a cell-free assay.

GSK097 is a highly potent and selective inhibitor of the second bromodomain (BD2) found in bromodomain and extra-terminal domain (BET) proteins. It exhibits a remarkable 2000-fold selectivity for BD2 over BD1, as indicated by BRD4 data. Additionally, GSK097 demonstrates solubility of over 1 mg/mL in FaSSIF media.

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP p300, exhibiting half-maximal degradation concentration (DC50) values of 0.05 nM for CBP and 0.2 nM for p300. The compound comprises lenalidomide (the cereblon ligand), a connecting linker, and GNE-207 (the bromodomain inhibitor). JET-209 is utilized in cancer research [1].

GSK217 is a potent and selective inhibitor of the bromo and extraterminal domain (BET) second bromodomain (BD2) with high solubility, utilized in oncology and immune inflammation research [1].

Bromodomain inhibitor-9 is an inhibitor of Bromodomains that selectively inhibits the activity of BRD4-1 with a Kd value of 12 nM. Bromodomain inhibitor-9 can be used in studies of diseases related to systemic or lipid metabolism, tissue inflammation, fibrosis, or chronic autoimmune diseases.

PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells. 1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021)

RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell

iBRD4-BD1 diTFA is a selective BRD4 bromodomain inhibitor with an IC50 value of 12 nM. It can be used for research in inflammation and oncology [1].

GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

FHD-609, an inhibitor and degrader of BRD9 (bromodomain-containing protein 9), targets the ncBAF complex and is useful for researching a broad spectrum of cancers with mutations in a BAF complex subunit. When used alongside Telomelysin or INO5401, FHD-609 could be effective in treating adrenocortical carcinoma (ACC) [1] [2].

BET-IN-16 (Comp I), a bromodomain and extra-terminal (BET) inhibitor, demonstrates anticancer activity by impeding the growth of prostate cancer cells. It exhibits potent inhibitory effects with half-maximal inhibitory concentration (IC50) values of 0.043 μM for LNCaP cells and 0.034 μM for 22Rv1 cells [1].

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

CBP EP300-IN-1 is a CBP EP300 bromodomain inhibitor.

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].

Y08262, a potent and selective inhibitor of the CBP bromodomain, demonstrates inhibitory action with an IC50 value of 73.1 nM. This compound is utilized in the study of acute myeloid leukemia (AML) [1].

PBRM1-BD2-IN-1 is a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibiting a binding affinity (Kd) of 0.7 μM and an inhibitory efficacy (IC50) of 0.2 μM, and is used in cancer research.

BET Bromodomain Inhibitor 3 is a BET bromodomain inhibitor with an inhibitory Ki value of >40 µM against BrdT. It is utilized in research related to contraception, cancer, and heart disease [1].