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25

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T5318 666-15

CREB inhibitor

Epigenetic Reader Domain Chromatin/Epigenetic
666-15 (CREB inhibitor) 是一种选择性CREB 抑制剂,IC50为 81 nM,可抑制乳腺癌异种移植模型中的肿瘤生长。
T8890 653-47 hydrochloride

Epigenetic Reader Domain Chromatin/Epigenetic
653-47 hydrochloride 是一种增强剂,能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。它也是 CREB 抑制剂,IC50为 26.3 μM。
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。
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)。
T24212 XX-650-23

XX65023,XX 650 23

Apoptosis; Epigenetic Reader Domain Apoptosis; Chromatin/Epigenetic
XX-650-23 是一种小分子 CREB 抑制剂,阻断 CREB 与其所需的共激活因子 CBP(CREB 结合蛋白)之间的关键相互作用,诱导AML细胞凋亡和细胞周期停滞,可用于研究急性髓系白血病 (AML)。
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。
T8774 MS7972

Epigenetic Reader Domain Chromatin/Epigenetic
MS7972 是一种小分子,能阻断人 p53 和 CREB 结合。它在50 μM 的时候几乎可以完全阻断 BRD 的相互作用。
T7297 KG-501

Naphthol AS-E phosphate,色酚AS-E磷酸盐

Epigenetic Reader Domain Chromatin/Epigenetic
KG-501 (Naphthol AS-E phosphate) 是一种 cAMP 反应元件结合蛋白抑制剂,IC50为6.89 μM。
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。
T27083 Crebinostat

Epigenetic Reader Domain; Histone Acetyltransferase; HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂,对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用, IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性,增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化,并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。
T64247 CREB-IN-1 TFA

CREB-IN-1 TFA 是一种有效的、口服具有活力的 CREB 抑制剂,其 IC50 值为 0.18 μM。CREB-IN-1 TFA 对乳腺癌细胞的生长表现出抑制作用。
T21131 NASTRp

Naphthol AS-TR phosphate

NASTRp, an inhibitor of CREB-CBP complex, possesses anti-cancer effects along with cell cycle regulation, autophagy suppression, and endoplasmic reticulum stress.
T28867 STF-038533

STF-038533 is an inhibitor of CREB target gene transcription.
T70736 NSC-45576

NSC-45576 is an inhibitor of CREB-CRE interaction.
T24501 MS2126

NSC 71584,NSC71584,MS 2126,MS-2126,NSC-71584

MS2126 is a Human p53 and CREB Binding Protein interaction inhibitor.
T24606 PDE7 inhibitor S14

PDE7 inhibitor-S14,S14

PDE7 inhibitor S14 is a cell-permeable PDE7 inhibitor that acts by targeting the cyclic adenosine monophosphate (cAMP)/cAMP-response element-binding protein (CREB) pathway.
T61314 DC-CPin7

DC-CPin7, a powerful inhibitor of the bromodomain of CREB-binding protein (CBP), exhibits an IC50 value of 2.5 μM [1].
T63041 DS01080522

DS01080522 是一种 PRKACA 的抑制剂。DS01080522 对 PRKACA 激酶的活性 (IC50: 0.8 nM) 以及 CREB 磷酸化 (IC50: 66 nM) 具有抑制作用。DS0108052 能够用于研究癌症。
T61719 DC-CPin711

DC-CPin711, a potent and selective inhibitor of the bromodomain of CREB-binding protein (CBP) with an IC50 of 0.0626 μM, effectively halts the cell cycle at the G1 phase and promotes apoptosis [1].
T76597 Prolylserine

Prolylserine 是一种二肽,是 Mel-Ab 细胞中黑色素生成的抑制剂。Prolylserine 降低小眼相关转录因子 (MITF) 和酪氨酸酶的表达,诱导ERK 的磷酸化,但不诱导 cAMP 反应元件结合蛋白 (CREB)。
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.
T61617 Hcyb1

Hcyb1 is a potent and specific inhibitor of phosphodiesterase 2 (PDE2). It exhibits a high degree of selectivity for inhibiting PDE2A with an IC50 value of 0.57 μM. In addition, Hcyb1 displays over 250-fold selectivity against other recombinant members of the PDE family. Moreover, its pharmacological actions include neuroprotective and antidepressant-like effects, which are believed to be mediated through the cAMP/cGMP-CREB-BDNF signaling pathway [1].
T65994 (6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation...
T75944 Spadin TFA

Spadin TFA 是一种从血液中释放的前肽衍生的天然肽,是一种有效的 TREK-1 通道阻滞剂,其 IC50值为 10 nM。Spadin TFA 增强小鼠中缝背核 5-HT 神经传递,诱导海马 CREB 激活和神经发生。Spadin TFA 可用于抗抑郁研究。
T21795 CRT5

CRT5 是一种吡嗪苯甲酰胺,对经 VEGF 处理的内皮细胞中的所有三种 PKD 亚型 (对 PKD1、PKD2 和 PKD3 的 IC50s 分别为 1、2 和 1.5 nM) 都是一种有效的选择性抑制剂,并且 CRT5 减少 VEGF 诱导的内皮细胞迁移、增殖和微管生成。

化合物

666-15
Cat.No: T5318
Synonym: CREB inhibitor
Target: Epigenetic Reader Domain
653-47 hydrochloride
Cat.No: T8890
Synonym:
Target: Epigenetic Reader Domain
Naphthol AS-E
Cat.No: T7856
Synonym: 色酚 AS-E,nAS-E
Target: Epigenetic Reader Domain, Histone Acetyltransferase
PF-CBP1
Cat.No: T3973
Synonym:
Target: Epigenetic Reader Domain
XX-650-23
Cat.No: T24212
Synonym: XX65023,XX 650 23
Target: Apoptosis, Epigenetic Reader Domain
EML 425
Cat.No: T15216
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase
MS7972
Cat.No: T8774
Synonym:
Target: Epigenetic Reader Domain
KG-501
Cat.No: T7297
Synonym: Naphthol AS-E phosphate,色酚AS-E磷酸盐
Target: Epigenetic Reader Domain
PF-CBP1 hydrochloride
Cat.No: T3217
Synonym: PF-CBP1 HCl
Target: Epigenetic Reader Domain, Histone Acetyltransferase
Crebinostat
Cat.No: T27083
Synonym:
Target: Epigenetic Reader Domain, Histone Acetyltransferase, HDAC
CREB-IN-1 TFA
Cat.No: T64247
Synonym:
Target:
NASTRp
Cat.No: T21131
Synonym: Naphthol AS-TR phosphate
Target:
STF-038533
Cat.No: T28867
Synonym:
Target:
NSC-45576
Cat.No: T70736
Synonym:
Target:
MS2126
Cat.No: T24501
Synonym: NSC 71584,NSC71584,MS 2126,MS-2126,NSC-71584
Target:
PDE7 inhibitor S14
Cat.No: T24606
Synonym: PDE7 inhibitor-S14,S14
Target:
DC-CPin7
Cat.No: T61314
Synonym:
Target:
DS01080522
Cat.No: T63041
Synonym:
Target:
DC-CPin711
Cat.No: T61719
Synonym:
Target:
Prolylserine
Cat.No: T76597
Synonym:
Target:
CAY10669
Cat.No: T35818
Synonym:
Target:
Hcyb1
Cat.No: T61617
Synonym:
Target:
(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
Cat.No: T65994
Synonym:
Target:
Spadin TFA
Cat.No: T75944
Synonym:
Target:
CRT5
Cat.No: T21795
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1516 Curcumin

Diferuloylmethane,Natural Yellow 3,姜黄素,Indian Saffron,Turmeric yellow

Mitophagy; Epigenetic Reader Domain; Ferroptosis; Influenza Virus; Nrf2; Histone Acetyltransferase; HDAC; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology
Curcumin (Natural Yellow 3) 属于酚类天然产物,是一种组蛋白乙酰化转移酶 p300/CREB 的抑制剂 (IC50=25 μM),具有特异性。Curcumin 具有抗肿瘤、抗炎和抗氧化等多种药理活性。
T75554 6-O-Isobutyrylbritannilactone

6-O-Isobutyrylbritannilactone 是一种天然的黑素生成抑制剂。6-O-Isobutyrylbritannilactone 是一种倍半萜,可从英菊花中分离得到。6-O-Isobutyrylbritannilactone 抑制 IBMX 诱导 B16F10 细胞产生黑色素。6-O-Isobutyrylbritannilactone 也调控 ERK、PI3K/AKT 和 CREB,在斑马鱼胚胎模型中显示出抗黑色素原活性。

天然产物

Curcumin
Cat.No: T1516
Synonym: Diferuloylmethane,Natural Yellow 3,姜黄素,Indian Saffron,Turmeric yellow
Target: Mitophagy, Epigenetic Reader Domain, Ferroptosis, Influenza Virus, Nrf2, Histone Acetyltransferase, HDAC, Autophagy
6-O-Isobutyrylbritannilactone
Cat.No: T75554
Synonym:
Target:
TargetMol Loading
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