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Histone Acetyltransferase
Histone Acetyltransferase製品
- All (32)
- Histone Acetyltransferase阻害剤 (28)
- Histone Acetyltransferase活性剤(3)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|---|
| 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. |
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| 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. |
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| 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. | ||
| 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. |
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| 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. |
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| S7641 | Remodelin Hydrobromide | Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor. | ||
| S7476 | MG149 | MG149 (Tip60 HAT inhibitor) is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively. | ||
| S8776 | WM-1119 | WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively. | ||
| 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. | ||
| S9432 | Ginkgolic Acid | Ginkgolic acid, toxic phenolic compounds present in the fruits and leaves of Ginkgo biloba L., is a potent sumoylation inhibitor also reported to inhibit histone acetylation transferase (HAT). | ||
| S8190 | CPI-637 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. | ||
| 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. | ||
| E1215 | JQAD1 | JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. | ||
| S2977 | EML 425 | EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively. | ||
| S9805 | WM-3835 | WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. | ||
| S1242 | CPTH2 | CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B. | ||
| 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. |
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| E1107 | CTB | CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol. | ||
| S7475 | NU9056 | NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. NU9056 demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells. | ||
| S6655 | WM-8014 | WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM. | ||
| E6080New | AUR1545 | AUR1545 is a potent and selective degrader of KAT2A and KAT2B. It exhibits an anti-proliferative effect and significantly inhibits tumor growth in an NCI-H1048 xenograft model. | ||
| E5885New | JG-2016 | JG-2016 is a potent and selective inhibitor of HAT1, with an IC50 of 14.8 μM and a binding KD of 22.5 μM for the HAT1:Rbap46 complex. It exhibits anti-proliferative activity with EC50 of 10.4 μM, 29.8 μM, and 1.9 μM in HCC1806, FICC1937, and A549 cells, respectively. JG-2016 significantly suppresses tumor growth in an A549 xenograft model. | ||
| E5829New | PU139 | PU139 is a potent inhibitor of pan-histone acetyltransferase (HAT) that blocks Gcn5, PCAF, CBP, and p300 with IC50 values of 8.39 μM, 9.74 μM, 2.49 μM, and 5.35 μM, respectively. It significantly impairs Smp14 promoter activity, suggesting that targeting SmGCN5 and SmCBP1 is a novel strategy to control S. mansoni egg development, it also exhibits anticancer activity. | ||
| 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. | ||
| E0068 | NiCur | NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter. | ||
| E1387 | Butyrolactone 3 | Butyrolactone 3 is a non-irreversible inhibitor of the histone acetyltransferase Gcn5, with an IC50 of 100 μM. It selectively targets the Gcn5/PCAF family exhibiting weak inhibition of CBP HAT with an IC50 of 0.5 mM and also inhibits pre-mRNA splicing in vitro before catalysis, with an IC50 of 0.5 mM. | ||
| E1654 | CTPB | CTPB is a synthetic activator of the p300 histone acetyltransferase (HAT) enzyme, which promotes transcription by increasing the H3 and H4 acetylation in nucleosomes. | ||
| S6886 | 1-Aminobenzotriazole | 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT). | ||
| S9445 | Ginkgolic Acid (C13:0) | Ginkgolic Acid (C13:0) is a natural anticariogenic agent in Ginkgo biloba L. that exhibits antimicrobial activity against S. mutans and suppresses the specific virulence factors associated with its cariogenicity. Ginkgolic acid is a potent sumoylation inhibitor and reported to inhibit histone acetylation transferase (HAT). | ||
| E7170 | KAT8-IN-1 | KAT8-IN-1 is an inhibitor of lysine acetyltransferase 8 (KAT8)> with IC50 values of 141 μM, 221 μM and 106 μM for KAT8, KAT2B, KAT3B respectively. By inhibiting histone acetyltransferases (HATs), it helps investigate their role in disease and holds potential as a therapeutic agent for cancer and inflammatory conditions. | ||
| E5782 | Remodelin | Remodelin is a potential inhibitor of the acetyltransferase NAT10. It enhances nuclear shape and cellular fitness in both progeric cells and cells depleted of Lamin A/C by inhibiting NAT10. Remodelin exhibits anti-proliferation activity and significantly inhibits tumour growth and tumour cell proliferation in the PDX model of HNSCC. | ||
| E0146 | PF-9363 (CTx-648) | PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumor activity in ER+ breast cancer models. | ||
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| S7641 | Remodelin Hydrobromide | Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor. | ||
| S7476 | MG149 | MG149 (Tip60 HAT inhibitor) is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively. | ||
| S8776 | WM-1119 | WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively. | ||
| 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. | ||
| S9432 | Ginkgolic Acid | Ginkgolic acid, toxic phenolic compounds present in the fruits and leaves of Ginkgo biloba L., is a potent sumoylation inhibitor also reported to inhibit histone acetylation transferase (HAT). | ||
| S8190 | CPI-637 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. | ||
| S2977 | EML 425 | EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively. | ||
| S9805 | WM-3835 | WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. | ||
| S1242 | CPTH2 | CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B. | ||
| 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. |
||
| S7475 | NU9056 | NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. NU9056 demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells. | ||
| S6655 | WM-8014 | WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM. | ||
| E6080New | AUR1545 | AUR1545 is a potent and selective degrader of KAT2A and KAT2B. It exhibits an anti-proliferative effect and significantly inhibits tumor growth in an NCI-H1048 xenograft model. | ||
| E5885New | JG-2016 | JG-2016 is a potent and selective inhibitor of HAT1, with an IC50 of 14.8 μM and a binding KD of 22.5 μM for the HAT1:Rbap46 complex. It exhibits anti-proliferative activity with EC50 of 10.4 μM, 29.8 μM, and 1.9 μM in HCC1806, FICC1937, and A549 cells, respectively. JG-2016 significantly suppresses tumor growth in an A549 xenograft model. | ||
| E5829New | PU139 | PU139 is a potent inhibitor of pan-histone acetyltransferase (HAT) that blocks Gcn5, PCAF, CBP, and p300 with IC50 values of 8.39 μM, 9.74 μM, 2.49 μM, and 5.35 μM, respectively. It significantly impairs Smp14 promoter activity, suggesting that targeting SmGCN5 and SmCBP1 is a novel strategy to control S. mansoni egg development, it also exhibits anticancer activity. | ||
| 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. | ||
| E0068 | NiCur | NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter. | ||
| E1387 | Butyrolactone 3 | Butyrolactone 3 is a non-irreversible inhibitor of the histone acetyltransferase Gcn5, with an IC50 of 100 μM. It selectively targets the Gcn5/PCAF family exhibiting weak inhibition of CBP HAT with an IC50 of 0.5 mM and also inhibits pre-mRNA splicing in vitro before catalysis, with an IC50 of 0.5 mM. | ||
| S6886 | 1-Aminobenzotriazole | 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT). | ||
| S9445 | Ginkgolic Acid (C13:0) | Ginkgolic Acid (C13:0) is a natural anticariogenic agent in Ginkgo biloba L. that exhibits antimicrobial activity against S. mutans and suppresses the specific virulence factors associated with its cariogenicity. Ginkgolic acid is a potent sumoylation inhibitor and reported to inhibit histone acetylation transferase (HAT). | ||
| E7170 | KAT8-IN-1 | KAT8-IN-1 is an inhibitor of lysine acetyltransferase 8 (KAT8)> with IC50 values of 141 μM, 221 μM and 106 μM for KAT8, KAT2B, KAT3B respectively. By inhibiting histone acetyltransferases (HATs), it helps investigate their role in disease and holds potential as a therapeutic agent for cancer and inflammatory conditions. | ||
| E5782 | Remodelin | Remodelin is a potential inhibitor of the acetyltransferase NAT10. It enhances nuclear shape and cellular fitness in both progeric cells and cells depleted of Lamin A/C by inhibiting NAT10. Remodelin exhibits anti-proliferation activity and significantly inhibits tumour growth and tumour cell proliferation in the PDX model of HNSCC. | ||
| E0146 | PF-9363 (CTx-648) | PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumor activity in ER+ breast cancer models. | ||
| 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. | ||
| E1107 | CTB | CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol. | ||
| E1654 | CTPB | CTPB is a synthetic activator of the p300 histone acetyltransferase (HAT) enzyme, which promotes transcription by increasing the H3 and H4 acetylation in nucleosomes. | ||
| E6080New | AUR1545 | AUR1545 is a potent and selective degrader of KAT2A and KAT2B. It exhibits an anti-proliferative effect and significantly inhibits tumor growth in an NCI-H1048 xenograft model. | ||
| E5885New | JG-2016 | JG-2016 is a potent and selective inhibitor of HAT1, with an IC50 of 14.8 μM and a binding KD of 22.5 μM for the HAT1:Rbap46 complex. It exhibits anti-proliferative activity with EC50 of 10.4 μM, 29.8 μM, and 1.9 μM in HCC1806, FICC1937, and A549 cells, respectively. JG-2016 significantly suppresses tumor growth in an A549 xenograft model. | ||
| E5829New | PU139 | PU139 is a potent inhibitor of pan-histone acetyltransferase (HAT) that blocks Gcn5, PCAF, CBP, and p300 with IC50 values of 8.39 μM, 9.74 μM, 2.49 μM, and 5.35 μM, respectively. It significantly impairs Smp14 promoter activity, suggesting that targeting SmGCN5 and SmCBP1 is a novel strategy to control S. mansoni egg development, it also exhibits anticancer activity. |
Histone Acetyltransferaseシグナル伝達経路
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間