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28

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T60452	PCAF-IN-2
	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。
T60762	PCAF-IN-1
	PCAF-IN-1 是用于肿瘤治疗研究的抗肿瘤剂。PCAF-IN-1 是高度选择性的PCAF 抑制剂。
T60558	NSC 694623	Histone Acetyltransferase	Chromatin/Epigenetic
	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。
T5468	YF-2	Others; Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic; Others
	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。
T28471	PU139 PU 139,PU-139	Histone Acetyltransferase	Chromatin/Epigenetic
	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。
T10604	BRD-IN-3	Others	Others
	BRD-IN-3 is a highly potent PCAF bromodomain (BRD) inhibitor (IC50: 7 nM). It also exhibits activity against GCN5 and FALZ.
T11495L	GSK 4027	Others	Others
	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.
T71724	F2276-0099
	F2276-0099 is a PCAF/GCN5 BRD inhibitor
T71721	F2276-0106
	F2276-0106 is a PCAF/GCN5 BRD inhibitor
T71720	F2276-0104
	F2276-0104 is a PCAF/GCN5 BRD inhibitor
T11495	GSK4028	Others	Others
	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.
T32010	GSK699 GSK-699,GSK 699
	GSK699 is a potent, cell penetrant PCAF/GCN5 PROTAC.
T62424	L-Moses dihydrochloride
	L-Moses (L-45) dihydrochloride 是一个有效的、选择性 p300/CBP 相关因子 (PCAF) 溴结构域 (Brd) 抑制剂 (Kd: 126 nM)。
T23745	APA-APA-MPO APA APA MPO,APAAPAMPO
	APA-APA-MPO is a PCAF bromodomain/Tat-AcK50 association inhibitor.
T25215	CCT077791 CCT 077791,CCT-077791	Epigenetic Reader Domain; Histone Acetyltransferase	Chromatin/Epigenetic
	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。
T23746	APA-H-MPO APAHMPO
	APA-H-MPO is a PCAF bromodomain/Tat-AcK50 association inhibitor.
T38711	YF-2 hydrochloride
	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.
T71723	F2276-0008
	F2276-0008 is a PCAF/GCN5 BRD inhibitor.
T11796L	L-Moses L-45	Others	Others
	L-45 is the first potent and cell-active bromodomain (Brd) inhibitor of p300/CBP-associated factor (PCAF) (Kd: 126±15 nM).
T36109	L Moses dihydrochloride
	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 P...
T60018	NSC 694621
	NSC 694621 是一种有效的 PCAF 抑制剂，其IC50值为 5.71 μM (PCAF/H31-21)。NSC 694621 显示出良好的抗癌活性，能抑制癌细胞的增殖。
T11807	L002	Others; Histone Acetyltransferase; STAT	Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells
	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。
T60479	NSC 698600
	NSC 698600 是一种有效的 PCAF（p300/CBP 相关因子）抑制剂，IC50值为 6.51 μM，显示出良好的癌细胞增殖抑制活性。
T63122	CBP/p300-IN-19
	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。
T73951	Lys-CoA TFA
	Lys-CoA TFA为选择性p300组蛋白乙酰转移酶(HAT)抑制剂，IC50值介于50-500 nM。其对p300的选择性超过PCAF 100倍，PCAF的IC50值为200 μM。此外，Lys-CoA TFA能够抑制依赖p300-HAT活性的转录激活。
T36626	Lys-CoA
	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 (...
T35818	CAY10669
	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.
T63565	CBP/p300-IN-19 hydrochloride
	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。

化合物

Cat.No: T60452

Cat.No: T60762

Cat.No: T60558

Target: Histone Acetyltransferase

Cat.No: T5468

Target: Others, Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T28471

Synonym: PU 139,PU-139

Target: Histone Acetyltransferase

Cat.No: T10604

Target: Others

Cat.No: T11495L

Target: Others

Cat.No: T71724

Cat.No: T71721

Cat.No: T71720

Cat.No: T11495

Target: Others

Cat.No: T32010

Synonym: GSK-699,GSK 699

L-Moses dihydrochloride

Cat.No: T62424

Cat.No: T23745

Synonym: APA APA MPO,APAAPAMPO

Cat.No: T25215

Synonym: CCT 077791,CCT-077791

Target: Epigenetic Reader Domain, Histone Acetyltransferase

Cat.No: T23746

Synonym: APAHMPO

YF-2 hydrochloride

Cat.No: T38711

Cat.No: T71723

Cat.No: T11796L

Synonym: L-45

Target: Others

L Moses dihydrochloride

Cat.No: T36109

Cat.No: T60018

Cat.No: T11807

Target: Others, Histone Acetyltransferase, STAT

Cat.No: T60479

Cat.No: T63122

Cat.No: T73951

Cat.No: T36626

Cat.No: T35818

CBP/p300-IN-19 hydrochloride

Cat.No: T63565

Cat. No.	Product Name	Target	Signaling Pathways
T11366	Garcinol	Apoptosis; Endogenous Metabolite; Histone Acetyltransferase; AChR; AChE	Apoptosis; Chromatin/Epigenetic; Metabolism; Neuroscience
	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。
T6389	Anacardic Acid 漆树酸,6-pentadecylsalicylic Acid,Hydroginkgolic acid	Others; Epigenetic Reader Domain; Histone Acetyltransferase; Antibacterial	Chromatin/Epigenetic; Microbiology/Virology; Others
	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。

天然产物

Cat.No: T11366

Target: Apoptosis, Endogenous Metabolite, Histone Acetyltransferase, AChR, AChE

Cat.No: T6389

Synonym: 漆树酸,6-pentadecylsalicylic Acid,Hydroginkgolic acid

Target: Others, Epigenetic Reader Domain, Histone Acetyltransferase, Antibacterial

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