About 14 results found for searched term "Bromodomain inhibitor-8" (0.124 seconds)
Cat.No. | Name | Target |
---|---|---|
M21943 | Bromodomain inhibitor-8 | Others |
Bromodomain inhibitor-8 | ||
M25394 | BPTF-IN-1 | Epigenetic Reader Domain |
compound AU1 | ||
BPTF-IN-1 (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. BPTF-IN-1 shows to be selective for BPTF over BRD4 bromodomain. | ||
M5064 | PFI-4 | Epigenetic Reader Domain |
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. PFI-4 (1.25 µM; 7 or 11 days) inhibits differentiation of human osteoclasts. | ||
M5258 | Mivebresib | Epigenetic Reader Domain |
ABBV-075 | ||
Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4) | ||
M10822 | GNE-781 | Epigenetic Reader Domain |
GNE-781 (compound 19) is a highly potent, orally active, selective bromodomain inhibitor against cyclic adenosine monophosphate response element binding protein (CBP). The IC50 value is 0.94 nM (in TR-FRET assay). GNE-781 also suppresses BRET and BRD4(1), with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 has antitumor activity. | ||
M10862 | MS645 | Epigenetic Reader Domain |
MS645 is a BET bromodomains (BrD) inhibitor for K of BRD4-BD1/BD2i The value is 18.4 nM. MS645 spatially limits the divalent inhibition of BRD4 BrDs, resulting in sustained inhibition of BRD4 transcriptional activity in solid tumor cells. | ||
M20549 | GSK 5959 | Epigenetic Reader Domain |
GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. | ||
M25523 | Y08284 | Epigenetic Reader Domain |
Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Y08284 has antitumor activity. | ||
M27706 | RVX-297 | Epigenetic Reader Domain |
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models. | ||
M28718 | CD161 | Epigenetic Reader Domain |
NKR-P1A | ||
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity. | ||
M28741 | GS-626510 | Epigenetic Reader Domain |
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively. | ||
M28788 | BAZ2-ICR | Epigenetic Reader Domain |
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe. | ||
M29089 | GSK8814 | Epigenetic Reader Domain |
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1. | ||
M29257 | NHWD-870 | Epigenetic Reader Domain |
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation. |
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