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52

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T12345 CBP/p300-IN-3

P300/CBP-IN-3

Histone Acetyltransferase Chromatin/Epigenetic
CBP/p300-IN-3 (P300/CBP-IN-3) 是一种组蛋白乙酰转移酶抑制剂。
T40144 CBP/p300 ligand 2

CBP/p300 ligand 2 is a selective ligand that binds to the target protein for PROTAC of dCBP-1, a potent and selective heterobifunctional degrader of p300/CBP.
T40143 PROTAC CBP/P300 Degrader-1

PROTAC CBP/P300 Degrader-1

PROTAC CBP/P300 Degrader-1 is an effective compound that degrades CBP/P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines.
T40142 Thalidomide-NH-CBP/p300 ligand 2

Thalidomide-NH-CBP/p300 ligand 2

Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based compound designed to degrade CBP and p300, acting as a functional antagonist (WO2020173440).
T12346 CBP/p300-IN-5

P300/CBP-IN-5

Epigenetic Reader Domain Chromatin/Epigenetic
P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).
T39826 CBP/p300-IN-8

CBP/p300-IN-8

CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains . CBP/p300-IN-8 inhibits CBP ( IC 50 =0.01-0.1 μΜ) and BRD4 ( IC 50 =1-1000 μΜ) activity.
T40344 CBP/p300-IN-14

CBP/p300-IN-14

CBP/p300-IN-14, efficiently inhibits CBP/EP300 (lysine acetyltransferase) with an IC50 value of 3.3 nM.
T10702 CBP/p300-IN-2

CBP/EP300-IN-2

Epigenetic Reader Domain; c-Myc Cell Cycle/Checkpoint; Chromatin/Epigenetic
CBP/EP300-IN-2 is an inhibitor of CBP/EP300 (IC50s: 1.07 nM and 5.96 nM for CBP/HTRF and Myc).
T9370 dCBP-1

Epigenetic Reader Domain; Ligand for E3 Ligase Chromatin/Epigenetic; PROTAC
dCBP-1 是基于Cereblon 配体的p300/CBP 的选择性双功能降解剂。dCBP-1可以有效的杀死多发性骨髓瘤细胞,并降低驱动 MYC 表达的致癌增强子活性。
T3635 IQ 1

IQ1,IQ-1

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
IQ 1 有多种作用,如保持小鼠ESCs 的多功能性、降低Wnt 刺激的磷酸化、阻止PP2A/Nkd 的相互作用等等。
T8778 TTK21

Epigenetic Reader Domain Chromatin/Epigenetic
TTK21 是 CBP/p300 组蛋白乙酰转移酶活性的激活剂,与葡萄糖基碳纳米球结合时,可通过血脑屏障,对成人大脑神经发生和长期记忆功能有益。
T8658 NEO2734

EP31670

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
NEO2734 (EP31670) 是一种具有口服活性的选择性 p300/CBP 和 BET 溴结构域抑制剂,其 IC50值均小于30 nM,可用于前列腺癌的研究。
T9373 DCH36_06

(5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

Apoptosis; Epigenetic Reader Domain; Histone Acetyltransferase Apoptosis; Chromatin/Epigenetic
DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione) 是一种选择性p300/CBP 抑制剂,介导 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化,有抗肿瘤活性,对p300CBP 的IC50分别为 0.6 μM 和 3.2 μM。
T62415 CBP/p300-IN-17

CBP/p300-IN-17 (compound 7) 是一种 EP300/CBP HAT 的有效抑制剂,能够作用于 HAT EP300 (IC50: 0.18 μM) 和 LK2 H3K27 (IC50: 0.69 μM)。
T79395 CBP/p300-IN-21

Epigenetic Reader Domain Chromatin/Epigenetic
CBP/p300-IN-21 (Compound 5d) 作为一种选择性CBP/p300抑制剂,展现出对p300CBP具有差异性的IC50值,分别为0.07 μM和1.755 μM。该化合物能有效降低H3K18Ac的水平,并抑制小鼠4T1肿瘤的生长。
T62700 CBP/p300-IN-16

CBP/p300-IN-16 (compound 1) 是一种 EP300/CBP HAT 的有效抑制剂,作用于 HAT EP300 (IC50: 0.61 μM) 和 LK2 H3K27 (IC50: 2.24 μM)。
T63110 CBP/p300-IN-15

CBP/p300-IN-15 (compound 13a) 是一种有效的 p300 (IC50: 2.5 nM) 和 CBP (IC50: 28.0 nM) 抑制剂。CBP/p300-IN-15 能够较好的抑制 OVCAR-3 细胞 (EC50: 0.865 μM) 和 A2780 细胞 (EC50: 2.71 μM)。 CBP/p300-IN-15 能够用于研究卵巢癌。
T72815 CBP/p300-IN-10

CBP/p300-IN-10 是一种高效的组蛋白乙酰转移酶 EP300和CREBBP 的抑制剂,IC50分别为 26 nM 和 39 nM。
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。
T62720 CBP/p300-IN-18

CBP/p300-IN-18 (compound 8) 是一种 EP300/CBP HAT 的有效抑制剂,能够作用于 HAT EP300 (IC50: 0.056 μM) 和 LK2 H3K27 (IC50: 0.46 μM)。
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。
T14073 A-485

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
A-485 是 p300/CBP 的一种选择性催化抑制剂,对 p300CBP 组蛋白乙酰转移酶的 IC50值分别为 9.8 和 2.6 nM。
T15216 EML 425

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
EML425 是一种有效的选择性 CREB ​​结合蛋白 (CBP)/p300 抑制剂,IC50为 2.9 和 1.1 μM。
T3969 I-CBP112

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
I-CBP112 是一种特异性的乙酰赖氨酸竞争性蛋白质-蛋白质相互作用抑制剂,靶向 CBP/p300 溴结构域,增强 p300 的乙酰化作用。
T10717 Inobrodib

CBP-IN-1

Epigenetic Reader Domain Chromatin/Epigenetic
Inobrodib (CBP-IN-1) 是一种口服活性的强选择性p300/CBP 抑制剂,与 p300CBP 结合,Kd 值为 1.3 和 1.7 nM。它抑制前列腺癌细胞系的细胞增殖并降低雄激素受体和 C-MYC 调节的基因表达。
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)、CBPp300,IC50 分别为 8.39、9.74、2.49 和 5.35 μM。
T9194 UMB298

Epigenetic Reader Domain Chromatin/Epigenetic
UMB298 是一种有效的选择性 CBP/P300 溴结构域抑制剂,抑制 BRD4,IC50 为 5193nM。
T10641 C-82

Epigenetic Reader Domain; Wnt/beta-catenin Chromatin/Epigenetic; Cytoskeletal Signaling; Stem Cells
C-82 是一种特异性 CBP/β-catenin 拮抗剂。它抑制 β-catenin 和 CBP 之间的结合,并增加 β-catenin 和 p300 之间的结合。
T6113 ICG-001

Apoptosis; Epigenetic Reader Domain; Wnt/beta-catenin Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Stem Cells
ICG001 是β-catenin/TCF 介导的一种转录抑制剂,选择性地阻断 β-catenin/CBP 相互作用而不干扰 β-catenin/p300 相互作用。它可特异性结合 CREB 蛋白,IC50为3 μM。
T69691 Pocenbrodib

FT-7051,P-300

Epigenetic Reader Domain Chromatin/Epigenetic
Pocenbrodib (FT-7051) 是一种有效的 CBP/p300 家族的溴结构域抑制剂,具有潜在的抗肿瘤活性,可口用于研究癌症。
T2237 ICG001

Epigenetic Reader Domain; Wnt/beta-catenin Chromatin/Epigenetic; Cytoskeletal Signaling; Stem Cells
ICG001 (PRI-724 isomer) 拮抗 Wnt/β-catenin/TCF 介导的转录,并特异性结合元件结合蛋白(CREB) 结合蛋白 (CBP),IC50 为 3 μM,但不是相关的转录共激活因子 p300
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。
T6668 SGC-CBP30

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
SGC-CBP30 是高选择性CBP/p300溴结构域的有效抑制剂,对CBPp300的Kd 值分别为 21 和 32 nM。它强烈减少 Th17 细胞中 IL-17A 的分泌,具有抗炎作用。
T4247 I-CBP112 hydrochloride

Epigenetic Reader Domain Chromatin/Epigenetic
I-CBP112 hydrochloride 是含溴结构域转录因子的选择性抑制剂,靶向 CBP/p300 溴结构域。在体内外,它以剂量依赖性方式显着降低 MLL-AF9(+) 急性髓细胞白血病细胞的白血病起始潜力,还增加 BET 溴结构域抑制剂 JQ1 以及阿霉素的细胞毒活性。
T3217 PF-CBP1 hydrochloride

PF-CBP1 HCl

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
PF-CBP1 hydrochloride (PF-CBP1 HCl) 是 CREB 结合蛋白溴结构域的一种高选择性抑制剂,抑制 CREBBP 和 EP300溴结构域的 IC50分别为 125 和 363 nM。它降低 LPS 诱导的巨噬细胞中炎症因子的表达,也可下调皮质神经元 RGS4 的表达,可用于癫痫和帕金森病等神经疾病的研究。
T2452 C646

Apoptosis; Epigenetic Reader Domain; Histone Acetyltransferase; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic
C646 是一种竞争性组蛋白乙酰转移酶 p300选择性抑制剂,Ki 值为 400 nM,对其他乙酰转移酶作用较小。
T24197 XDM-CBP

XDMCBP,XDM CBP

XDM-CBP is an effective and selective CBP/p300 bromodomain inhibitor.
T26758 BDOIA383

BDOIA383 is a novel inhibitor of CBP/p300 Bromodomains.
T63940 B026

B026 是选择性的、口服具有活力的 p300/CBP 组蛋白乙酰转移酶 (p300/CBP HAT) 抑制剂,能够作用于 p300 (IC50: 1.8 nM) 和 CBP (IC50: 9.5 nM)。B026 对雄激素受体阳性 (AR+) 前列腺癌细胞表现出抗癌效果。
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).
T28004 MDK8228

PF-CBP/BRD4,MDK-8228,MDK 8228

MDK8228 is an inhibitor of CBP/p300 and BRD4 bromodomain. MDK8228 downregulates IL-6, IL-ß and IFN-ß in macrophages.
T17147 TPOP146

Epigenetic Reader Domain Chromatin/Epigenetic
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor (Kd: 134 nM and 5.02 μM for CBP and BRD4).
T73566 OHM1

OHM1 是HIF1α CTAD 的类似物,抑制其与 p300/CBP 的结合。OHM1 靶向 CH1 结构域,亲和力为 0.53 μM。
T79230 JET-209

PROTACs PROTAC
JET-209为高效PROTAC CBP/p300降解剂,DC50分别为CBPp300的0.05 nM与0.2 nM。该化合物融合了Lenalidomide (cereblon配体)、连接子以及GNE-207 (溴结构域抑制剂)。JET-209主要应用于癌症研究领域。
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)。
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。
T78715 MS78

MS78为一种乙酰化靶向嵌合体(AceTAC),其功能是招募组蛋白乙酰转移酶p300/CBP以乙酰化p53肿瘤抑制蛋白的p53Y220C突变体。通过该作用,MS78能够上调TRAIL凋亡基因,同时下调DNA损伤反应信号通路。此化合物结构包含CBP/p300结合物、p53Y220C结合物及linker。
T40036 Thalidomide-NH-PEG4-COOH

Thalidomide-NH-PEG4-COOH

Thalidomide-NH-PEG4-COOH is a conjugate comprising an E3 ligase ligand-linker, utilized in the synthesis of dCBP-1. dCBP-1 itself functions as a powerful and selective heterobifunctional degrader targeting p300/CBP.
T39352 Piperidine-GNE-049-N-Boc

Piperidine-GNE-049-N-Boc is a ligand that specifically binds to the target protein dCBP, enabling it to be degraded by a selective and potent heterobifunctional degrader, p300/CBP.
T72013 Epigenetic Multiple Ligand

Epigenetic Multiple Ligand is a cell-permeable inhibitor of substrate processing by several chromatin-associated enzymes, including SIRT1/2, H3/SET7, H3/p300/CBP, H4/RmtA, PABP1/CARM1, and H4/PRMT1. It acts by inducing either apoptosis or granulocytic differentiation.

化合物

CBP/p300-IN-3
Cat.No: T12345
Synonym: P300/CBP-IN-3
Target: Histone Acetyltransferase
CBP/p300 ligand 2
Cat.No: T40144
Synonym:
Target:
PROTAC CBP/P300 Degrader-1
Cat.No: T40143
Synonym: PROTAC CBP/P300 Degrader-1
Target:
Thalidomide-NH-CBP/p300 ligand 2
Cat.No: T40142
Synonym: Thalidomide-NH-CBP/p300 ligand 2
Target:
CBP/p300-IN-5
Cat.No: T12346
Synonym: P300/CBP-IN-5
Target: Epigenetic Reader Domain
CBP/p300-IN-8
Cat.No: T39826
Synonym: CBP/p300-IN-8
Target:
CBP/p300-IN-14
Cat.No: T40344
Synonym: CBP/p300-IN-14
Target:
CBP/p300-IN-2
Cat.No: T10702
Synonym: CBP/EP300-IN-2
Target: Epigenetic Reader Domain, c-Myc
dCBP-1
Cat.No: T9370
Synonym:
Target: Epigenetic Reader Domain, Ligand for E3 Ligase
IQ 1
Cat.No: T3635
Synonym: IQ1,IQ-1
Target: Wnt/beta-catenin
TTK21
Cat.No: T8778
Synonym:
Target: Epigenetic Reader Domain
NEO2734
Cat.No: T8658
Synonym: EP31670
Target: Epigenetic Reader Domain, Histone Acetyltransferase
DCH36_06
Cat.No: T9373
Synonym: (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
Target: Apoptosis, Epigenetic Reader Domain, Histone Acetyltransferase
CBP/p300-IN-17
Cat.No: T62415
Synonym:
Target:
CBP/p300-IN-21
Cat.No: T79395
Synonym:
Target: Epigenetic Reader Domain
CBP/p300-IN-16
Cat.No: T62700
Synonym:
Target:
CBP/p300-IN-15
Cat.No: T63110
Synonym:
Target:
CBP/p300-IN-10
Cat.No: T72815
Synonym:
Target:
CBP/p300-IN-19
Cat.No: T63122
Synonym:
Target:
CBP/p300-IN-18
Cat.No: T62720
Synonym:
Target:
CBP/p300-IN-19 hydrochloride
Cat.No: T63565
Synonym:
Target:
A-485
Cat.No: T14073
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
EML 425
Cat.No: T15216
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
I-CBP112
Cat.No: T3969
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
Inobrodib
Cat.No: T10717
Synonym: CBP-IN-1
Target: Epigenetic Reader Domain
PU139
Cat.No: T28471
Synonym: PU 139,PU-139
Target: Histone Acetyltransferase
UMB298
Cat.No: T9194
Synonym:
Target: Epigenetic Reader Domain
C-82
Cat.No: T10641
Synonym:
Target: Epigenetic Reader Domain, Wnt/beta-catenin
ICG-001
Cat.No: T6113
Synonym:
Target: Apoptosis, Epigenetic Reader Domain, Wnt/beta-catenin
Pocenbrodib
Cat.No: T69691
Synonym: FT-7051,P-300
Target: Epigenetic Reader Domain
ICG001
Cat.No: T2237
Synonym:
Target: Epigenetic Reader Domain, Wnt/beta-catenin
NSC 694623
Cat.No: T60558
Synonym:
Target: Histone Acetyltransferase
SGC-CBP30
Cat.No: T6668
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
I-CBP112 hydrochloride
Cat.No: T4247
Synonym:
Target: Epigenetic Reader Domain
PF-CBP1 hydrochloride
Cat.No: T3217
Synonym: PF-CBP1 HCl
Target: Epigenetic Reader Domain, Histone Acetyltransferase
C646
Cat.No: T2452
Synonym:
Target: Apoptosis, Epigenetic Reader Domain, Histone Acetyltransferase, Autophagy
XDM-CBP
Cat.No: T24197
Synonym: XDMCBP,XDM CBP
Target:
BDOIA383
Cat.No: T26758
Synonym:
Target:
B026
Cat.No: T63940
Synonym:
Target:
L-Moses
Cat.No: T11796L
Synonym: L-45
Target: Others
MDK8228
Cat.No: T28004
Synonym: PF-CBP/BRD4,MDK-8228,MDK 8228
Target:
TPOP146
Cat.No: T17147
Synonym:
Target: Epigenetic Reader Domain
OHM1
Cat.No: T73566
Synonym:
Target:
JET-209
Cat.No: T79230
Synonym:
Target: PROTACs
L-Moses dihydrochloride
Cat.No: T62424
Synonym:
Target:
NSC 698600
Cat.No: T60479
Synonym:
Target:
MS78
Cat.No: T78715
Synonym:
Target:
Thalidomide-NH-PEG4-COOH
Cat.No: T40036
Synonym: Thalidomide-NH-PEG4-COOH
Target:
Piperidine-GNE-049-N-Boc
Cat.No: T39352
Synonym:
Target:
Epigenetic Multiple Ligand
Cat.No: T72013
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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。
TN1567 Delphinidin chloride

Estrogen Receptor/ERR; VEGFR Angiogenesis; Endocrinology/Hormones; Tyrosine Kinase/Adaptors
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)

天然产物

Anacardic Acid
Cat.No: T6389
Synonym: 漆树酸,6-pentadecylsalicylic Acid,Hydroginkgolic acid
Target: Others, Epigenetic Reader Domain, Histone Acetyltransferase, Antibacterial
Delphinidin chloride
Cat.No: TN1567
Synonym:
Target: Estrogen Receptor/ERR, VEGFR
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