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92

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。
T7264 CBP/EP300-IN-1

Epigenetic Reader Domain Chromatin/Epigenetic
CBP/EP300-IN-1是一种 CBP/EP300 溴结构域抑制剂。
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 p300 和 CBP 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。
T24197 XDM-CBP

XDMCBP,XDM CBP

XDM-CBP is an effective and selective CBP/p300 bromodomain inhibitor.
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.
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.
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).
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。
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).
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.
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。
T68895 CBP-93872

CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy.
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).
T3973 PF-CBP1

Epigenetic Reader Domain Chromatin/Epigenetic
PF-CBP1 是一种高选择性的 CREB ​​结合蛋白 (CREBBP) 溴结构域抑制剂。它抑制 CREBBP (IC50: 125 nM) 和 p300 溴结构域 (IC50: 363 nM)。
T26962 CBP-307

CBP307

CBP-307 is a selective second generation S1P1 (a G-protein coupled receptor -GPCR) modulator.
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.
T12537 β-catenin/CBP-IN-1

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
β-catenin/CBP-IN-1 is a potent and selective inhibitor of CBP/β-catenin
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CBP 和p300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。
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。
T81314 Rademikibart

CBP-201

Rademikibart (CBP-201) 是一款针对IL-4Rα的人源化单克隆抗体,其与人IL-4Rα的结合亲和力KD值为20.7 pM。该抗体不与其他物种的IL-4Rα发生交互作用。Rademikibart 能够抑制PBMC中IL-4及IL-13介导的STAT6信号通路、TF-1细胞的增殖以及TARC的产生,显示出其在中到重度Th2型炎症性疾病研究中的应用潜力。
T79168 CBP-IN-1

Epigenetic Reader Domain Chromatin/Epigenetic
CBP-IN-1(化合物12)是一种高效CBP抑制剂,其IC50为1.5 nM。此外,该化合物对CBP BRET和BRD4(1)的抑制作用,其IC50分别达到690 nM和3100 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.
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p300和CBP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)。
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)。
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。
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。
T7856 Naphthol AS-E

色酚 AS-E,nAS-E

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
Naphthol AS-E (nAS-E) 是一种具有细胞渗透性的KIX-KID 相互作用的抑制剂,可用于癌症研究。它直接结合 CBP 的 KIX 域,Kd 为 8.6 µM,阻断 KIX 域和 KID 域的相互作用,IC50为 2.26 µM。
T69091 CBP501

CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle.
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p300和CBP 的IC50分别为 0.6 μM 和 3.2 μM。
T80132 CBP501 Affinity Peptide

CBP501 Affinity Peptide为Chk激酶抑制剂,具有消除DNA损伤剂诱导的G2停滞作用,主要应用于癌症研究领域。
T78455 Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2

Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 是一款钌基化合物,既可作为量子点 (QDs) 荧光猝灭剂,也适用于捕获病毒抗原EV71的探针。此外,该化合物还用于作为灵敏的电致化学发光 (ECL) 试剂,用于基质金属蛋白酶 (MMP)[2] 的检测。
T81250 Ru(bpy)2(dcbpy)NHS dihexafluorophosphate

Ru(bpy)2(dcbpy)NHS (dihexafluorophosphate)与金纳米颗粒结合, 可构建用于电化学发光检测溶菌酶的扩增系统。
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。
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。
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 p300和 CBP 组蛋白乙酰转移酶的 IC50值分别为 9.8 和 2.6 nM。
T6811 CPI-637

CPI 637

Epigenetic Reader Domain; Histone Acetyltransferase Chromatin/Epigenetic
CPI-637 是一种选择性和细胞活性的苯二氮卓 CBP/EP300 溴结构域抑制剂,其对 CBP、EP300和 BRD4 BD-1的 IC50值分别为 0.03、0.051 和 11.0 μM,对 CBP 的 EC50值为 0.3 μM。
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。
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。
T16154 MS417

GTPL7512

Epigenetic Reader Domain; HIV Protease Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome
MS417 (GTPL7512) 是一种 BET 特异性 BRD4 抑制剂,与 BRD4-BD1 和 BRD4-BD2 结合,Kd 值分别为 36.1和25.4 nM,IC50值分别为 30和46 nM。它对 CBP BRD 的选择性较低,IC50值为 32.7 μM。
T15405 GNE-781

Epigenetic Reader Domain Chromatin/Epigenetic
GNE-781 是一种具有口服活性的选择性 CBP 抑制剂,在 TR-FRET 实验中 IC50为 0.94 nM。它还抑制BRET 和BRD4 (1),IC50分别为 6.2 和 5100 nM,有抗肿瘤活性。
T50014 2-methyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-4-one

Epigenetic Reader Domain Chromatin/Epigenetic
2-methyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-4-one 是 CBP 的配体。
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。

化合物

CBP/p300-IN-3
Cat.No: T12345
Synonym: P300/CBP-IN-3
Target: Histone Acetyltransferase
CBP/EP300-IN-1
Cat.No: T7264
Synonym:
Target: Epigenetic Reader Domain
Inobrodib
Cat.No: T10717
Synonym: CBP-IN-1
Target: Epigenetic Reader Domain
XDM-CBP
Cat.No: T24197
Synonym: XDMCBP,XDM CBP
Target:
CBP/p300-IN-14
Cat.No: T40344
Synonym: CBP/p300-IN-14
Target:
CBP/p300-IN-8
Cat.No: T39826
Synonym: CBP/p300-IN-8
Target:
CBP/p300-IN-5
Cat.No: T12346
Synonym: P300/CBP-IN-5
Target: Epigenetic Reader Domain
I-CBP112 hydrochloride
Cat.No: T4247
Synonym:
Target: Epigenetic Reader Domain
CBP/p300-IN-2
Cat.No: T10702
Synonym: CBP/EP300-IN-2
Target: Epigenetic Reader Domain, c-Myc
PROTAC CBP/P300 Degrader-1
Cat.No: T40143
Synonym: PROTAC CBP/P300 Degrader-1
Target:
I-CBP112
Cat.No: T3969
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
CBP-93872
Cat.No: T68895
Synonym:
Target:
Thalidomide-NH-CBP/p300 ligand 2
Cat.No: T40142
Synonym: Thalidomide-NH-CBP/p300 ligand 2
Target:
PF-CBP1
Cat.No: T3973
Synonym:
Target: Epigenetic Reader Domain
CBP-307
Cat.No: T26962
Synonym: CBP307
Target:
CBP/p300 ligand 2
Cat.No: T40144
Synonym:
Target:
β-catenin/CBP-IN-1
Cat.No: T12537
Synonym:
Target: Wnt/beta-catenin
SGC-CBP30
Cat.No: T6668
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
PF-CBP1 hydrochloride
Cat.No: T3217
Synonym: PF-CBP1 HCl
Target: Epigenetic Reader Domain, Histone Acetyltransferase
Rademikibart
Cat.No: T81314
Synonym: CBP-201
Target:
CBP-IN-1
Cat.No: T79168
Synonym:
Target: Epigenetic Reader Domain
MDK8228
Cat.No: T28004
Synonym: PF-CBP/BRD4,MDK-8228,MDK 8228
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-17
Cat.No: T62415
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:
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
Naphthol AS-E
Cat.No: T7856
Synonym: 色酚 AS-E,nAS-E
Target: Epigenetic Reader Domain, Histone Acetyltransferase
CBP501
Cat.No: T69091
Synonym:
Target:
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
CBP501 Affinity Peptide
Cat.No: T80132
Synonym:
Target:
Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2
Cat.No: T78455
Synonym:
Target:
Ru(bpy)2(dcbpy)NHS dihexafluorophosphate
Cat.No: T81250
Synonym:
Target:
ICG-001
Cat.No: T6113
Synonym:
Target: Apoptosis, Epigenetic Reader Domain, Wnt/beta-catenin
ICG001
Cat.No: T2237
Synonym:
Target: Epigenetic Reader Domain, Wnt/beta-catenin
A-485
Cat.No: T14073
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
CPI-637
Cat.No: T6811
Synonym: CPI 637
Target: Epigenetic Reader Domain, Histone Acetyltransferase
EML 425
Cat.No: T15216
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
YF-2
Cat.No: T5468
Synonym:
Target: Others, Epigenetic Reader Domain, Histone Acetyltransferase
MS417
Cat.No: T16154
Synonym: GTPL7512
Target: Epigenetic Reader Domain, HIV Protease
GNE-781
Cat.No: T15405
Synonym:
Target: Epigenetic Reader Domain
2-methyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-4-one
Cat.No: T50014
Synonym:
Target: Epigenetic Reader Domain
UMB298
Cat.No: T9194
Synonym:
Target: Epigenetic Reader Domain
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
共92条,每页50条 1 2
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