Histone Acetyltransferases
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cell permeable p300 inhibitor
Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5 ?M; Histone Acetyltransferase Inhibitor II can be used in cancer research.
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CBP/p300 bromodomain 抑制剂
SGC-CBP30是一种有效且选择性的CREBBP(CBP)和EP300抑制剂,无细胞试验中IC50分别为21 nM和38 nM。它们是一般的转录共激活因子。
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CBP/p300 bromodomain 抑制剂
I-CBP112是一种高效且选择性的p300/CBP溴结构域抑制剂(对于CBP,IC50为?0.14-0.17 uM,对于p300为?0.625 uM)。
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CBP/P300 benzoxazepine bromodomain inhibitor
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
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CBP inhibitor
GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
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CBP/beta-catenin 拮抗剂
PRI-724是ICG-001的异构体或对映异构体,是一种强力的特异性抑制剂癌症干细胞中的Wnt信号通路具有潜在的抗肿瘤活性。
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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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CBP/p300 抑制剂
EML 425是一种可逆且非竞争性的CBP/p300抑制剂,具有细胞渗透性(IC50值分别为1.1和2.9 uM)。
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CBP/EP300 bromodomain 抑制剂
CPI-637是一种选择性的,具有细胞活性的苯并二氮杂酮CBP/EP300溴结构域抑制剂。
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p300 HAT activator
CTPB is an activator of p300 HAT (histone acetyltransferase) without PCAF (p300/CBP-associated factor) HAT activities.
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p300/CBP 抑制剂
A-485是p300/CBP的强效选择性HAT抑制剂,在p300 TR-FRET分析中的IC50为10 nM,在CBP TR-FRET分析中的IC50为3 nM,选择性是紧密相关的HAT的1000倍以上。
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CBP/beta-catenin modulator
E-7386是一种活性CBP /β-catenin调节剂。
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CBP bromodomain inhibitor
GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile.
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histone acetyltransferase activator
YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
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acetyl-transferase protein NAT10 inhibitor
Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
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p300/CBP histone acetyltransferase inhibitor
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor.
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lysine acetyltransferase KAT6A 抑制剂
WM-1119是赖氨酸乙酰基转移酶KAT6A的高效选择性抑制剂,IC50为0.25 uM。它对KAT6A的活性分别是对KAT5或KAT7的1100倍和250倍。
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KAT5 (Tip60) HAT 抑制剂
MG149是一种有效的组蛋白乙酰转移酶抑制剂,对Tip60和MOF的IC50为74 uM和47 uM。
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NAT10 抑制剂
Remodelin Hydrobromide是一种有效的乙酰转移酶NAT10抑制剂。
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KAT5 (Tip60), p300/PCAF 抑制剂
Anacardic Acid是p300和p300/CBP相关因子组蛋白乙酰转移酶的有效抑制剂。
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KAT5 (Tip60) HAT 抑制剂
NU9056是一种选择性KAT5(Tip60)HAT抑制剂。对于KAT5,p300,pCAF和GCN5,IC50值分别为<2、60、36和> 100μM。抑制前列腺癌细胞系和蛋白质块中的蛋白质乙酰化。
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p300/CBP 抑制剂
C646是选择性的p300/CREB结合蛋白(CBP)抑制剂(Ki = 400 nM)。
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- Zhifeng Zhang, .et al. XRCC5 cooperates with p300 to promote cyclooxygenase-2 expression and tumor growth in colon cancers, PLoS One, 2017, 12(10): e0186900 PMID: 29049411
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HAT 抑制剂
藤黄酚是从印度藤黄中分离的聚异戊二烯基二苯甲酮衍生物。 在体外和体内,它都是有效的组蛋白乙酰转移酶(HATs)p300(IC50 = 7?M)和PCAF(IC50 = 5?M)抑制剂。
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