Bromodomains are a family of evolutionarily conserved protein modules of approximately 110 amino acids that have been found in chromatin-associated proteins as well as nuclear histone acetyltransferases (HATs). Besides its role in chromatin remodeling, recent studies have identified that bromodomains, as acetyl-lysine binding domains, are able to recognize and bind ε–N-acetylated lysine residues in histone and non-histone proteins. The nuclear magnetic resonance (NMR) spectroscopic analysis reveals that the chemical structure of bromodomains, consisting of four left-handed α-helices (including αZ, αA, αB and αC) connected by two loops (ZA and BC loops), forms a deep hydrophobic cavity serving as the acetyl-lysine recognition site.
Cat. No. | Product Name | CAS No. | Information |
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H9639 |
BRD8 inhibitor DN02 |
BRD8 inhibitor DN02 is a first-in-class selective and cellularly active probe for NuA4 factor BRD8 (BD1) with AlphaScreen IC50 of 48 nM, and Kd of 34 nM, displays IC50 of 0.64 uM in-cell engagement within BRET displacement assays, shows no affinity for BRD8 (BD2), CBP, and p300 (IC50>10 uM). |
|
H9529 |
Amredobresib |
1610044-98-8 | Amredobresib is a potent inhibitor of BET,Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription; Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer |
H9481 |
Inobrodib |
2222941-37-7 | Inobrodib(CCS-1477) is an orally, potent and selective p300/CBP bromodomain inhibitor, is targeted & differentiated from BET inhibitors in prostate cancer cell lines in vitro. |
H9235 |
XS018661 |
878415-59-9 | XS018661 is the first-in-class dual inhibitor of ENL with Kd of 754 ± 45 nM and its paralog AF9 with Kd of 523 ± 53 nM. |
H9195 |
GSK778 |
2451862-42-1 | GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively; GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. |
H9191 |
NVS-CECR2-1 |
1992047-61-6 | NVS-CECR2-1 is a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM); NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism. |
H9108 |
(+)-JQ-1-aldehyde |
(+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains. |
|
H8855 |
Pelabresib |
1380087-89-7 | Pelabresib(CPI-0610)is a potent, selective, and cell-active BET inhibitor. CPI-0610 inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC. |
H8709 |
NHWD-870 |
2115742-03-3 | NHWD-870 is a potent BRD4 inhibitor with IC50 of IC50 = 2 or 1.6 nM , and is about 50-fold more potent than JQ1.NHWD-870 is an oral bet inhibitor, which has good permeability in lung and SCLC tumors. |
H8523 |
GSK046 |
2474876-09-8 | GSK046 (iBET-BD2) is a potent, selective and orally active bromodomain inhibitor of BD2 of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. |
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