pcaf

Garcinol 是一种从印度藤黄提取的聚异戊二烯基二苯甲酮，对乙酰胆碱酯酶和丁酰胆碱酯酶具有抗胆碱酯酶的特性，IC50分别为 0.66 µM 和 7.39 µM。它还抑制组蛋白乙酰转移酶和 p300 CPB 相关因子，具有抗炎和抗癌活性。

L002 是一种细胞可渗透的，可逆特定性乙酰转移酶 p300(KAT3B)抑制剂，IC50为 1.98 μM。 它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域，阻断组蛋白乙酰化和 p53 乙酰化，且抑制 STAT3 激活，有用于高血压引起的心脏肥大和纤维化的研究潜力。

PCAF-IN-2 (compound 17) 是一种有效的 PCAF 抑制剂(IC50 = 5.31 µM)。PCAF-IN-2 具有抗肿瘤活性。PCAF-IN-2 诱导细胞凋亡并且阻滞细胞周期在 G2 M 期。

PCAF-IN-1是一种高选择性的PCAF（p300 CBP-associated factor）抑制剂，具有潜在的抗肿瘤、抗炎、抗心脏疾病作用。抑制PCAF可以减轻心肌梗死后的心脏重塑，减少M1型巨噬细胞的极化，减轻自身免疫性关节炎。

GSK 4027 is a PCAF GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

Delphinidin chloride 是一种花青素，是一种可从浆果和红酒中分离得到的天然植物色素，是某些花青素的前体。Delphinidin chloride 诱导血管内皮释放一氧化氮，引起血管松弛。在1 ~ 40 μM 剂量下，对上皮生长因子受体的信号传导和雌激素受体α的表达有抑制作用，与细胞凋亡和自噬有关。Delphinidin chloride 能调节 JAK STAT3 和 MAPKinase 信号传导。Delphinidin 还能抑制 p300 CBP 的组蛋白乙酰转移酶活性(IC50 在约为30 μM)

Anacardic Acid (6-pentadecylsalicylic Acid) 是从腰果壳中提取液中分离到的酸类物质，是一种组蛋白乙酰转移酶抑制剂，对 p300 和 PCAF 的 IC50值分别为 ∼8.5 μM 和 ∼5 μM。

NSC 694623 是一种有效的组蛋白乙酰转移酶 (HAT) 抑制剂，对重组 HAT p300 CBP 相关因子 (PCAF) 具有抑制作用，IC50 为 15.9 μM。NSC 694623 对部分癌细胞展示出抗增殖活性，可用于研究抗癌。

BRD-IN-3 is a highly potent PCAF bromodomain (BRD) inhibitor (IC50: 7 nM). It also exhibits activity against GCN5 and FALZ.

GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF GCN5 bromodomain chemical probe. The pIC50 of GSK4028 is 4.9 in a TR-FRET assay.

CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300 CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid . At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.

NSC 694621是一种PCAF和组蛋白乙酰转移酶（ histone acetyltransferase，HAT）抑制剂，与PCAF的活性位点Cys574形成共价键，从而不可逆地抑制其乙酰转移酶活性，能够抑制SK-N-SH 和HCT116细胞增殖，具有抗癌潜力。

CBP p300-IN-19 是一种 p300 CBP HAT 的有效抑制剂，能够作用于 p300-HAT (IC50: 1.4 μM)、CBP-HAT (IC50: 2.2 μM)、PCAF (IC50>100 μM)、Myst3 (IC50>100 μM)。CBP p300-IN-19 具有抗肿瘤活性。

CBP p300-IN-19 hydrochloride 是选择性的、有效的 p300 CBP HAT 抑制剂，能够作用于 p300-HAT (IC50: 1.4 μM)、CBP-HAT (IC50: 2.2 μM)、PCAF (IC50>100 μM)、Myst3 (IC50>100 μM)。CBP p300-IN-19 hydrochloride 具有抗肿瘤作用。

CCT077791 是一种有效的 p300 和 PCAF 组蛋白乙酰转移酶活性抑制剂，可用于研究癌症。

L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300 CBP-associated factor (PCAF) (Kd: 126±15 nM).

APA-APA-MPO is a PCAF bromodomain/Tat-AcK50 association inhibitor.

APA-H-MPO is a PCAF bromodomain Tat-AcK50 association inhibitor.

PU139 是一种有效的泛组蛋白乙酰转移酶 (HAT) 抑制剂。PU139 阻断 HATs Gcn5、p300 CBP 相关因子 (PCAF)、CBP 和 p300，IC50 分别为 8.39、9.74、2.49 和 5.35 μM。

GSK699 is a potent, cell penetrant PCAF GCN5 PROTAC.

High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID:27966810

Selective p300 histone acetyltransferase (HAT) inhibitor (IC50 = 50-500 nM). Exhibits approximately 100-fold selectivity for p300 over PCAF (IC50 = 200 μM). Inhibits p300-dependent transcription. Active in vivo. Lau et al (2000) HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol.Cell. 5 589 PMID:10882143 |Liu et al (2008) The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 451 846 PMID:18273021 |Burns et al (2005) Iso-coenzyme A. J.Biol.Chem. 280 16550 PMID:15708855 |Cebrat et al (2003) Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg.Med.Chem. 11 3307 PMID:12837541

YF-2 hydrochloride is a potent histone acetyltransferase activator that exhibits high selectivity and can pass through the blood-brain barrier. It specifically acetylates H3 in the hippocampus, with EC50 values of 2.75 μM, 29.04 μM, and 49.31 μM for CBP, PCAF, and GCN5, respectively. Notably, it does not affect HDAC activity. Moreover, YF-2 hydrochloride demonstrates promising anti-cancer and anti-Alzheimer's disease properties.

YF-2 是一种高选择性，可透过血脑屏障的组蛋白乙酰转移酶激动剂，能够在海马区乙酰化 H3，对 CBP、PCAF 和 GCN5 的EC50值分别为 2.75、29.04 和 49.31 μM，具有抗肿瘤和抗阿尔滋海默症的活性。