Search Result
Results for "
CBP/EP300
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107455
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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-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-15826
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Epigenetic Reader Domain
Histone Acetyltransferase
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Inflammation/Immunology
Cancer
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SGC-CBP30, a chemical probe, 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-138539
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-
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- HY-100726
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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-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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- HY-138536
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines .
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- HY-100482
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- HY-134582
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PROTACs
Epigenetic Reader Domain
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Cancer
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dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression .
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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-19541
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- HY-136938
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NEO2734
4 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-124696
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PU139
4 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-128875
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Histone Acetyltransferase
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Cancer
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CBP/p300-IN-10 is a highly potent histone acetyltransferase EP300 and CREBBP with IC50 values of 26 nM and 39 nM, respectively. CBP/p300-IN-10 can be used to research anticancer .
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- HY-141546
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Histone Acetyltransferase
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Cancer
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Pocenbrodib is a P300/CBP inhibitor. Pocenbrodib blocks the function of P300/CBP and inhibits the acetylation of histones and non-histone proteins. Pocenbrodib may be used in research related to castration-resistant prostate cancer and other cancers .
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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), a chemical probe, 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-111420
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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-154984
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Histone Acetyltransferase
PROTACs
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Cancer
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JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia .
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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-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-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-128876
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- HY-173552
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Molecular Glues
Histone Acetyltransferase
BCL6
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Cancer
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TCIP3 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. TCIP3 redirects p300 and CBP to activate programmed cell death genes normally repressed by the oncogenic driver, BCL6. TCIP3 can be used for the study of diffuse large B cell lymphomas (DLBCLs). TCIP3 exhibits no toxicity in non-transformed tonsillar lymphocytes or fibroblasts .
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- HY-112359
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β-catenin
Wnt
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Cancer
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C-82 is a second-generation specific CBP/β-catenin antagonist, which inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300 .
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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-134591
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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-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-139148
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- HY-134592
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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-110263
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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-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-161959
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- HY-161960
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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EP300/CBP ligand 2 (compound S19) is a ligand targeting the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). EP300/CBP ligand 2 can be used as a target protein ligand in the PROTAC structure, and can be coupled to the E3 ubiquitin ligase ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, EP300/CBP ligand 2 can be coupled with the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc (HY-161961) to produce the PROTAC molecule dCE-2 (HY-161958) .
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- HY-164005
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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-139707
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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-100697
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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-139861
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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-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-176251
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Histone Acetyltransferase
Epigenetic Reader Domain
NF-κB
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Inflammation/Immunology
Cancer
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CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC50 of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.
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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-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-168201
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PROTACs
Histone Acetyltransferase
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Cancer
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MJP6412 is a potent degrader histone acetyltransferases p300/CBP, with DC50 of 1.6 and 1.2 nM for p300 and CBP, respectively. MJP6412 plays an important role in cancer research .
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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-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-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-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-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-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-136285A
-
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Histone Acetyltransferase
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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-145386
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Histone Acetyltransferase
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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-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-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-W877997
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E3 Ligase Ligand-Linker Conjugates
Drug Derivative
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Cancer
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Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer .
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- HY-151812
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- HY-155229
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- HY-161495
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- HY-161961
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-NH-C10-Boc (compound S20) is a conjugate of the E3 ubiquitinase ligand Thalidomide and PROTAC Linker, which can recruit Cereblon ubiquitinase. Thalidomide-NH-C10-Boc can couple the target protein ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, Thalidomide-NH-C10-Boc can couple with the ligand EP300/CBP ligand 2 (HY-161960) to produce the PROTAC molecule dCE-2 (HY-161958) .
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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-161711
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- HY-123758
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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-100726R
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Reference Standards
Histone Acetyltransferase
Epigenetic Reader Domain
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Cancer
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GNE-272 (Standard) is the analytical standard of GNE-272 (HY-100726). This product is intended for research and analytical applications. GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300 .
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- HY-161710
-
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PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)) .
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- HY-168464
-
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Epigenetic Reader Domain
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Cancer
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Y16526 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.03 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML) .
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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-173641
-
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Molecular Glues
Histone Acetyltransferase
BCL6
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Cancer
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MNN-02-155 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. MNN-02-155 induces potent activation of the BCL6-target reporter gene and cell death. MNN-02-155 can be used for the study of diffuse large B cell lymphomas (DLBCLs) .
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- HY-100482R
-
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Epigenetic Reader Domain
Reference Standards
Histone Acetyltransferase
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Cancer
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CPI-637 (Standard) is the analytical standard of CPI-637 (HY-100482). This product is intended for research and analytical applications. CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP .
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- HY-101125B
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D-45
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Epigenetic Reader Domain
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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-122081
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Histone Acetyltransferase
LAG-3
CTLA-4
PD-1/PD-L1
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Cancer
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CPI-644 is a selective EP300/CBP bromodomain inhibitor, with an IC50 of 0.18 µM against the CBP bromodomain. CPI-644 reduces the proportion of FOXP3 + cells and downregulates the expression of LAG-3, CTLA-4 and PD-1. CPI-644 can be used in cancer-related research .
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- HY-183802
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PROTACs
Histone Acetyltransferase
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Cancer
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PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC50 of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies .
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- HY-181852
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- HY-186064
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- HY-181758
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PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
c-Myc
Apoptosis
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Cancer
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PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
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- HY-181261
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- HY-181759
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers .
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- HY-107455R
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Reference Standards
Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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A-485 (Standard) is the analytical standard of A-485 (HY-107455). This product is intended for research and analytical applications. A-485, a chemical probe, is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively .
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- HY-183817
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- HY-183251
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL) .
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- HY-W173361
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Epigenetic Reader Domain
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Others
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CBP/p300-IN-24 (compound 1) is a CBP bromodomain inhibitor with an IC50 of 32 μM and selectivity over BRD4 BD-1 bromodomain.CBP/p300-IN-24 binds to the acetyl lysine binding pocket, forms hydrogen bonds with Asn1168 and a solvent-mediated hydrogen bond with Tyr1125, and forms hydrophobic interactions with Leu1120, Ile1122, and Val1174 .
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- HY-181957
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Epigenetic Reader Domain
Histone Acetyltransferase
Apoptosis
IKZF Family
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Cancer
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KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC50 values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma .
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- HY-100697R
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- HY-168463
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Epigenetic Reader Domain
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Cancer
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Y16524 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.01 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML) .
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- HY-184124
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Androgen Receptor
Histone Acetyltransferase
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Cancer
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JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer .
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- HY-P11829
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Histone Acetyltransferase
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Cancer
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ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer .
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- HY-180804
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Epigenetic Reader Domain
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Cancer
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CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research .
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- HY-165413
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HIF/HIF Prolyl-Hydroxylase
VEGFR
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Cancer
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KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC50 of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies .
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- HY-114510
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Discoidin Domain Receptor
Histone Acetyltransferase
Sirtuin
Fungal
Apoptosis
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Infection
Cancer
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PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .
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- HY-183818
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Ligands for E3 Ligase
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Cancer
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CRBN ligand-903 is a CRBN-binding ligand as well as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase). CRBN ligand-903 can be used to synthesize PROTAC CBP/P300 Degrader-4 (HY-183802) .
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- HY-10593
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Wnt
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Others
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IQ 1 is a Wnt/β-catenin/CBP signalling sustainer. IQ 1 maintains long-term expansion of Wnt/β-catenin-driven mouse embryonic stem cells (ESCs) and prevents spontaneous differentiation by enhancing β-catenin/CBP-mediated transcription and preventing conversion to β-catenin/p300-mediated transcription. IQ-1 regulates Wnt signalling by interacting with PR72/130. IQ 1 can be used in study of ESCs expansion .
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- HY-185009
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PROTACs
Histone Acetyltransferase
Interleukin Related
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Inflammation/Immunology
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GSK702, a PROTAC, is a the less active cis-(S,S)-enantiomer of GSK983 (P300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) PROTAC). GSK702 induces only a small decrease of PCAF protein levels. GSK702 binds to CRBN and causes a reduction of IL-1β in macrophages. GSK702 can be used for the study of inflammatory mediators .
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- HY-116673
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Histone Acetyltransferase
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Neurological Disease
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TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
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- HY-17663
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PARP
STAT
STING
IFNAR
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Cancer
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KMR-206 is a PARP7 inhibitor with an IC50 of 13.7 nM. KMR-206 relieves AHR-mediated transcriptional repression and enhances CYP1A1 expression in the presence of TCDD. KMR-206 induces the STING-dependent IFN-β signaling pathway and increases the levels of STAT1, pSTAT1 and nuclear PARP7 in cancer cells. KMR-206 reduces the viability of lung adenocarcinoma cells, enhances radiation-induced immunogenic signals, and induces the production of immunogenic signals in glioblastoma cancer stem cells. KMR-206 destabilizes FRA1 to increase IRF1 levels and promotes the IRF3-CBP/p300 interaction. KMR-206 can be used in studies related to lung adenocarcinoma and glioblastoma .
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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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- HY-P11829
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Histone Acetyltransferase
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Cancer
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ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer .
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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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