Search Result
Results for "
EP300/CBP inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100726
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- HY-111420
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- HY-136285
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Histone Acetyltransferase
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Cancer
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CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity .
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- HY-160261S
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Epigenetic Reader Domain
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Cancer
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EP300/CBP-IN-2 is a potent EP300/CBP inhibitor that has good activity in vivo. EP300/CBP-IN-2 can be used for the research of cancer .
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- HY-160260
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC50s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells .
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- HY-128761
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Epigenetic Reader Domain
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Cancer
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CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM and 5.96 nM for CBP/HTRF and Myc, respectively. CBP/EP300-IN-2, example 25, is extracted from patent WO2017205538A1 .
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- HY-143441
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Histone Acetyltransferase
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Cancer
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CBP/p300-IN-17 (compound 7) is a potent EP300/CBP HAT inhibitor with IC50s of 0.18, 0.69 µM for HAT EP300 and LK2 H3K27, respectively .
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- HY-143442
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Histone Acetyltransferase
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Cancer
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CBP/p300-IN-18 (compound 8) is a potent EP300/CBP HAT inhibitor with IC50s of 0.056, 0.46 µM for HAT EP300 and LK2 H3K27, respectively .
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- HY-143440
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Histone Acetyltransferase
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Cancer
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CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC50s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively .
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- HY-164005
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- HY-100482
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- HY-145386
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Others
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Cancer
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(S,S)-CPI-1612 is the isomer of CPI-1612 (HY-136285), and can be used as an experimental control. CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity .
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- HY-136285A
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Others
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Cancer
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(R,R)-CPI-1612 is the isomer of CPI-1612 (HY-136285), and can be used as an experimental control. CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity .
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- HY-139861
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- HY-143443
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Histone Acetyltransferase
Histone Demethylase
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Cancer
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DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research .
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- HY-152241
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Histone Acetyltransferase
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Cancer
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DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research .
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- HY-161958
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PROTACs
Histone Acetyltransferase
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Cancer
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dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961) [1] .
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- HY-151812
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- HY-155229
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- HY-146277
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Histone Acetyltransferase
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Cancer
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CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity .
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- HY-161495
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- HY-146277A
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Histone Acetyltransferase
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Cancer
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CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity .
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- HY-136920
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Epigenetic Reader Domain
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Cancer
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CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC50=0.01-0.1 µΜ) and BRD4 (IC50=1-1000 µΜ) activity .
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- HY-161483
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Epigenetic Reader Domain
Histone Acetyltransferase
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Neurological Disease
Cancer
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CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .
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- HY-111422
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Epigenetic Reader Domain
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Cancer
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PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
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- HY-132197
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450 .
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- HY-128876
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- HY-19541
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- HY-139108
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Histone Acetyltransferase
Apoptosis
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Cancer
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DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity .
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- HY-107455
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- HY-143339
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC50 values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC50 values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research .
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- HY-100132
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Histone Acetyltransferase
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Cancer
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P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM .
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- HY-19999A
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Epigenetic Reader Domain
Histone Acetyltransferase
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Neurological Disease
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PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with?IC50?of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β,?IL-6?and?IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates?RGS4?expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al .
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- HY-123758
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- HY-136938
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NEO2734
1 Publications Verification
EP31670
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains . NEO2734 is active in SPOP mutant and wild-type prostate cancer .
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- HY-147261
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Histone Acetyltransferase
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Cancer
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B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines .
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- HY-139148
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- HY-100697
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- HY-161494
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PROTACs
Epigenetic Reader Domain
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Cancer
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XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496)) .
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- HY-161498
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PROTACs
Epigenetic Reader Domain
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Cancer
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XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))
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- HY-15826
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Epigenetic Reader Domain
Histone Acetyltransferase
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Inflammation/Immunology
Cancer
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SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects .
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- HY-161369
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PROTACs
Histone Acetyltransferase
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Cancer
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CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
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- HY-P10238
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Apoptosis
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Cancer
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MYBMIM is an inhibitor for assembly of the molecular MYB:CBP/P300 complex. MYBMIM inhibits growth of leukemia cells .
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- HY-111784
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CCS1477
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Epigenetic Reader Domain
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Cancer
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Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .
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- HY-141546
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Histone Acetyltransferase
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Cancer
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Pocenbrodib (compound II) is a CBP/p300 family of bromodomain inhibitor. Pocenbrodib has the potential for cancer research .
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- HY-124696
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PU139
3 Publications Verification
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Histone Acetyltransferase
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Cancer
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PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively .
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- HY-154984
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Histone Acetyltransferase
PROTACs
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Cancer
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JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 contains Lenalidomide (HY-A0003) (the cereblon ligand), a linker and GNE-207 (HY-120028) (bromodomain Inhibitor). JET-209 is used for cancer research .
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- HY-124722
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM .
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- HY-110263
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- HY-115539
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Wnt
β-catenin
Histone Acetyltransferase
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Cancer
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Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP .
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- HY-162259
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PROTACs
Histone Acetyltransferase
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Cancer
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QC-182 is a potent PROTAC degrader of p300/CBP. QC-182 reduces p300 protein in the SK-HEP-1 cells (DC50 = 93nM). QC-182 potently and effectively inhibits cell growth in the SK-HEP-1 and JHH7 cell lines with IC50 values of 0.733 and 0.477 μM, respectively. QC-182 can be used for the research of hepatocellular carcinoma (HCC) .
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- HY-101125A
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L-45 dihydrochloride
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Epigenetic Reader Domain
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Cancer
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L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM .
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- HY-101125
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L-Moses
2 Publications Verification
L-45
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Epigenetic Reader Domain
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Cancer
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L-Moses (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM .
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- HY-19541A
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Epigenetic Reader Domain
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Cancer
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I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
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- HY-161250
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PROTACs
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Cancer
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Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader, which contains a CRBN ligands Pomalidomide, a 24-atom linker with 6 PEG units and a HAT inhibitor CPI-1612. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 exhibits antiproliferative effects in cells multiple myeloma cells LP1 (with a DC50 of 1.2 μM), MM1S and various cancer cell lines, especially the leukemia cells .
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- HY-120290
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Histone Acetyltransferase
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Cancer
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PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity .
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- HY-147290
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Histone Acetyltransferase
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Cancer
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NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer .
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- HY-14428
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β-catenin
Apoptosis
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Cancer
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ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
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- HY-101125B
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D-45
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Others
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Cancer
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D-Moses (D-45) is an enantiomer of L-Moses (HY-101125). L-Moses (L-45) is a potent and selective p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor. D-Moses shows no observable binding for PCAF Brd. D-Moses can be used as an inactive control compound to L-Moses .
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- HY-158113
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Histone Acetyltransferase
PROTACs
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Cancer
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CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10238
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Apoptosis
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Cancer
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MYBMIM is an inhibitor for assembly of the molecular MYB:CBP/P300 complex. MYBMIM inhibits growth of leukemia cells .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-160261S
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EP300/CBP-IN-2 is a potent EP300/CBP inhibitor that has good activity in vivo. EP300/CBP-IN-2 can be used for the research of cancer .
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