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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC73268 GNE-234 GNE-234 is the negative control compound of the selective PBRM1(2) inhibitor GNE-235.
DC73269 GNE-235 GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.
DC73270 GSK023 GSK023 is a potent, selective BET BD1 domain inhibitor with pIC50 of 7.8 against BRD4 BD1, >100-fold selective over BD2.
DC73271 GSK761 GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function.
DC73272 HP-4833 HPI-1 is a high affinity BET bromodomain binder with low nM Kd for BRD2/3/4 and about 10-fold lower affinity for BRDT. HPI-1 shows much higher affinity to BD2 of BRD2 (17 nM), than to BD1 (540 nM), no apparent selectivity between BRD2/3/4.
DC73273 iBRD4-BD1 iBRD4-BD1 is a potent, selective inhibitor of the first BRD4 bromodomain with IC50 of 12 nM, shows 23- to 6200-fold intra-BET selectivity.
DC73274 IV-255 IV-255 is a next-generation selective inhibitor of BRG1 bromodomain, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.
DC73275 IV-275 IV-275 is a next-generation inhibitor of BRG1 and BRM bromodomains, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.
DC73276 PFI-6 PFI-6 is a selective small-molecule chemical probe inhibitor for the YEATS domain of MLLT1 and MLLT3 with IC50 of 140 nM and 160 nM, respectively.
DC73277 SJ1461 SJ1461 (SJ-1461) is a potent and orally bioavailable BET inhibitor with IC50 of 6.8/0.2 nM for BRD4 BD1/BD2, and 1.3/0.1 nM for BRD2 BD1/BD2, respectively.
DC73278 TDI-11055 TDI-11055 (TDI 11055) is a potent, selective and orally bioavailable inhibitor of the acyl-lysine reader ENL/AF9 YEATS domain with IC50 of 0.05 and 0.07 uM, respectively.
DC73279 XL-126 XL-126 (XL126) is a potent BD1-selective BET inhibitor with SPR binding KD value of 8.9 nM, has 185-fold BD1/BD2 selectivity.
DC73280 YEATS4 binder 4d YEATS4 binder 4d is a potent, selective small-molecule epigenetic reader YEATS4 binder with Ki of 33 nM, >10-fold selectivity over YEATS1, 2 and 3.
DC73281 YEATS4 binder 4e YEATS4 binder 4e is a potent, selective small-molecule epigenetic reader YEATS4 binder with Ki of 37 nM, >15-fold selectivity over YEATS1, 2 and 3.
DC73282 ZEN-3694 ZEN-3694 is a novel potent, orally bioavailable BET bromodomain inhibitor, selectively binds to both bromodomains of the BET proteins, inhibiting the interaction of acetylated histone peptide with IC50 values in low nM range.
DC73283 2,4-lutidine 2,4-lutidine is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (His6-TTD vs. H3K9me3) EC50E of 29.2 uM.
DC73284 F1957-0088 F1957-0088 is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (TTD vs. H3K9me3) EC50 of 45.1 uM.
DC73285 GSK3482364 Featured GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.
DC73287 A452 A452 is a potent and selective HDAC6 inhibitor, effectively inhibits the cell growth and viability of various cancer cell types, irrespective of p53 status.
DC73288 CM-1758 CM-1758 is a novel histone deacetylase (HDAC) inhibitor with IC50 of 5 nM and 126 nM for HDAC1 and HDAC6, respectively.
DC73289 GH8HA01 GH8HA01 is a highly potent, selective HDAC8 inhibitor with Ki of 0.67 nM, highly selective against HDAC8 compared to other HDACs.
DC73290 HO53 HO53 is a small moecule inducer of cathelicidin antimicrobial peptide gene (CAMP) expression in bronchial epithelium cells, HO53 is a histone deacetylase (HDAC) inhibitor, interacts directly with HDAC3.
DC73291 HR488B HR488B is a potent, selective HDAC1 inhibitor with IC50 of 1.24 uM, effectively inhibits the proliferation of CRC cells.
DC73292 KH-259 KH-259 is a potent, isozyme-selective and CNS-penetrant HDAC6 inhibitor with IC50 of 260 nM, shows weak activity against HDAC1 and HDAC4 (IC50>6 uM).
DC73293 KPZ560 KPZ560 is a potent, HDAC1/2-selective inhibitor with IC50 of 12/68 nM, respectively.
DC73294 Mz325 Mz325 is a potent, selective, dual inhibitor of Sirt2/HDAC6 with IC50 of 320/43 nM, respectively.
DC73295 NBM-T-L-BMX-OS01 NBM-T-L-BMX-OS01 (BMX, HDAC8 inhibitor) is a potent, selective and BB penetrant HDAC8 inhibitor with IC50 of 831 nM.
DC73296 NN-429 NN-429 (NN429) is a potent, selective second-generation inhibitor of HDAC6 with IC50 of 3.2 nM, >312-fold selectivityt over all HDAC isoforms.
DC73297 NT160 NT160 is a high affinity, selective class-IIa histone deacetylase (HDAC) inhibitor with IC50 of 80 nM (HDAC4), 600-fold selectivity over HDAC2 and 27-fold selectivity over HDAC8.
DC73298 PB118 PB118 is a potent, selective HDAC6 inhibitor with IC50 of 5.6 nM, shows >1000 times selectively towards HDAC1, reduces alzheimer's disease neuropathology.

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