| S2662 |
ICG-001
|
ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis. |
-
Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0629
-
Adv Sci (Weinh), 2025, 12(40):e05702
-
Cell Rep Med, 2025, 6(2):101927
|
|
| S7152 |
C646
|
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
-
Nat Commun, 2025, 16(1):4502
-
Nat Commun, 2025, 16(1):524
-
J Extracell Vesicles, 2025, 14(2):e70042
|
|
| S1848 |
Curcumin
|
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
-
J Biol Chem, 2025, 301(7):110305
-
Mol Pain, 2025, 21:17448069251323668
-
BMC Immunol, 2025, 26(1):67
|
|
| S7256 |
SGC-CBP30
|
SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. |
-
Mol Cell, 2025, 85(8):1525-1542.e10
-
Cell Death Dis, 2025, 16(1):193
-
Cell Rep, 2025, 44(4):115523
|
|
| S8968 |
PRI-724 (Foscenvivint)
|
Foscenvivint (PRI-724) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP. |
-
Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0629
-
Cell Death Dis, 2025, 16(1):466
-
Biomed Pharmacother, 2025, 188:118225
|
|
| S8740 |
A-485
|
A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets. |
-
Nat Genet, 2025, 57(10):2468-2481
-
Cancer Discov, 2025, 15(2):382-400
-
Nat Cell Biol, 2025, 10.1038/s41556-025-01658-1
|
|
| S9648 |
NEO2734 (EP31670)
|
NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
-
Cell Rep Med, 2024, 5(3):101471
-
Nat Cancer, 2023, 4(10):1508-1525
-
PLoS Pathog, 2023, 19(8):e1011598
|
|
| S8190 |
CPI-637
|
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. |
-
Mol Cell Proteomics, 2023, 22(3):100504
-
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
|
|
| S6758 |
I-CBP112
|
I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively. |
-
Hepatology, 2021, 10.1002/hep.32245
-
Hepatology, 2021, 10.1002/hep.32245
|
|
| S0022 |
YF-2
|
YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, YF-2 has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. YF-2 also increases p300 activity. |
-
J Extracell Vesicles, 2025, 14(2):e70042
-
J Exp Clin Cancer Res, 2022, 41(1):77
|
|
| S1161 |
Histone Acetyltransferase Inhibitor II
|
Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
|
-
Genetics, 2017, 205(3):1125-1137
|
|
| S3984 |
Nordihydroguaiaretic acid (NDGA)
|
Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis. |
-
Gut Microbes, 2025, 17(1):2518338
|
|
| S8625 |
GNE-049
|
GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively. |
-
Nat Genet, 2025, 57(10):2468-2481
|
|
| S7582 |
Anacardic Acid
|
Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity,
prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
|
-
Sci Adv, 2025, 11(9):eadq2881
-
J Transl Med, 2024, 22(1):995
-
Int J Mol Sci, 2024, 25(17)9600
|
|
| S6876 |
CPI-1612
|
CPI-1612 is a highly potent, orally active inhibitor of EP300/CBP histone acetyltransferase (HAT). It displays an IC50 of 8.0 nM for EP300 HAT. CPI-1612 suppresses H3K27 acetylation in vivo and exhibits efficacy in JEKO-1 mantle cell lymphoma xenograft at a low dose. CPI-1612 displays anticancer activity. |
|
|
| E1348 |
E7386
|
E-7386 is a selective inhibitor which inhibits interaction between CBP/beta-catenin with IC50 value of 0.0484 μM in HEK293 cells. |
-
Adv Sci (Weinh), 2024, 11(35):e2308417
-
Cell Rep, 2024, 43(8):114532
|
|
| S9667 |
Inobrodib (CCS-1477)
|
Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc. |
-
Nat Genet, 2025, 57(10):2468-2481
-
Nat Commun, 2025, 16(1):4133
-
PLoS Pathog, 2025, 21(9):e1013073
|
|
| S2966 |
TTK21
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. It activates CBP/p300 histone acetyltransferase activity in a concentration-dependent manner with a maximal effect at a concentration of 275 µM. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different brain parts when conjugated to glucose-based carbon nanosphere (CSP). |
-
Chin Med J (Engl), 2025, 10.1097/CM9.0000000000003567
|
|
| S7152 |
C646
|
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
- Nat Commun, 2025, 16(1):4502
- Nat Commun, 2025, 16(1):524
- J Extracell Vesicles, 2025, 14(2):e70042
|
|
| S1848 |
Curcumin
|
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
- J Biol Chem, 2025, 301(7):110305
- Mol Pain, 2025, 21:17448069251323668
- BMC Immunol, 2025, 26(1):67
|
|
| S7256 |
SGC-CBP30
|
SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. |
- Mol Cell, 2025, 85(8):1525-1542.e10
- Cell Death Dis, 2025, 16(1):193
- Cell Rep, 2025, 44(4):115523
|
|
| S8740 |
A-485
|
A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets. |
- Nat Genet, 2025, 57(10):2468-2481
- Cancer Discov, 2025, 15(2):382-400
- Nat Cell Biol, 2025, 10.1038/s41556-025-01658-1
|
|
| S9648 |
NEO2734 (EP31670)
|
NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
- Cell Rep Med, 2024, 5(3):101471
- Nat Cancer, 2023, 4(10):1508-1525
- PLoS Pathog, 2023, 19(8):e1011598
|
|
| S8190 |
CPI-637
|
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. |
- Mol Cell Proteomics, 2023, 22(3):100504
- Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
|
|
| S6758 |
I-CBP112
|
I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively. |
- Hepatology, 2021, 10.1002/hep.32245
- Hepatology, 2021, 10.1002/hep.32245
|
|
| S1161 |
Histone Acetyltransferase Inhibitor II
|
Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
|
- Genetics, 2017, 205(3):1125-1137
|
|
| S3984 |
Nordihydroguaiaretic acid (NDGA)
|
Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis. |
- Gut Microbes, 2025, 17(1):2518338
|
|
| S8625 |
GNE-049
|
GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively. |
- Nat Genet, 2025, 57(10):2468-2481
|
|
| S7582 |
Anacardic Acid
|
Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity,
prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
|
- Sci Adv, 2025, 11(9):eadq2881
- J Transl Med, 2024, 22(1):995
- Int J Mol Sci, 2024, 25(17)9600
|
|
| S6876 |
CPI-1612
|
CPI-1612 is a highly potent, orally active inhibitor of EP300/CBP histone acetyltransferase (HAT). It displays an IC50 of 8.0 nM for EP300 HAT. CPI-1612 suppresses H3K27 acetylation in vivo and exhibits efficacy in JEKO-1 mantle cell lymphoma xenograft at a low dose. CPI-1612 displays anticancer activity. |
|
|
| E1348 |
E7386
|
E-7386 is a selective inhibitor which inhibits interaction between CBP/beta-catenin with IC50 value of 0.0484 μM in HEK293 cells. |
- Adv Sci (Weinh), 2024, 11(35):e2308417
- Cell Rep, 2024, 43(8):114532
|
|
| S9667 |
Inobrodib (CCS-1477)
|
Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc. |
- Nat Genet, 2025, 57(10):2468-2481
- Nat Commun, 2025, 16(1):4133
- PLoS Pathog, 2025, 21(9):e1013073
|
|