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42

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T35827L PKCε Inhibitor Peptide acetate

PKCε Inhibitor Peptide acetate(182683-50-7 Free base)

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKCε Inhibitor Peptide acetate 是一种特异性 PKCε 抑制剂,含有其特定受体活化 C 激酶 (RACK) 的位点。 PKCε Inhibitor Peptide acetate 抑制 PKCε 的转运,但不抑制 αPKC,βPKC 和 δPKC 的转运。
T35827 Epsilon-V1-2

PKCε Inhibitor Peptide,Protein Kinase Cɛ Inhibitor Peptide,ɛV1-2

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membrane...
TP1051 Protein Kinase C Peptide Substrate

PRKCE,Peptide Epsilon,PKCε

Protein Kinase C Peptide Substrate targets specific cell spacers ina manner that is dependent on second messengers and specific adaptor proteins in response to extracellular signals that activate g protein-coupled receptors, tyrosine Kinase receptors, or
T80248 PKCε (85-92)

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKCε(85-92) 是一种具有生物活性的肽,其作为 e-PKC 特异性激活剂,能够促进野生型细胞中的 MARCKS 磷酸化作用,对基因敲除小鼠来源的细胞中的 MARCKS 磷酸化则无影响。
T80511 PKCε inhibitor peptide,myristoylated

Myr‐PKCɛ-

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
Myristoylated PKCε inhibitor peptide(Myr-PKCε-)是一种与肉豆蔻酸偶联、具有细胞渗透性的PKCε蛋白激酶Cε亚型特异性肽抑制剂,它能够降低人脐静脉内皮细胞(HUVECs)的一氧化氮(NO)释放。
T81450 PKCε Inhibitor Scramble Peptide

PKCε Inhibitor Scramble Peptide为一Scramble肽,其氨基酸序列与PKCε抑制肽相同。
T8376 PKCβ inhibitor 1

KUN79359

Apoptosis; PKC Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling
PKCβ inhibitor 1 (KUN79359) 是一种 ATP 竞争性和选择性PKCβ抑制剂,对人 PKCβ1 和 PKCβ2 的IC50分别为 21 和 5 nM。
TP1955L PKC β pseudosubstrate acetate

PKC β pseudosubstrate醋酸盐,Protein kinase C beta pseudosubstrate,PKC beta pseudosubstrate,PKC β pseudosubstrate acetate (172308-76-8 Free base)

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC β pseudosubstrate acetate (PKC β pseudosubstrate acetate (172308-76-8 Free base)) 是一种选择性的、细胞渗透的 PKC 抑制剂。
T12494 PKC-IN-1

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC-IN-1 是 ATP-竞争性可逆 PKC 抑制剂,对人 PKCβ 和 PKCα 的 Ki 值分别为 5.3 和 10.4 nM,对人 PKCα、PKCβI、PKCβII、PKCθ、PKCγ、PKC mu 和 PKCε 的IC50值分别为 2.3、8.1、7.6、25.6、57.5、314 和 808 nM。
TP1956L PKC ζ pseudosubstrate acetate

PKC ζ pseudosubstrate acetate (799764-07-1 free base)

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC ζ pseudosubstrate acetate 是蛋白激酶 C (PKC) ζ 的抑制剂;附着于细胞通透性触角足结构域载体肽。由 PKC ζ 假底物结构域的氨基酸 113-129 组成,通过二硫键连接到触角足结构域载体肽。 Antennapedia 肽在 4 或 37°C 时被完整细胞积极吸收,确保快速有效地吸收抑制肽。一旦进入细胞,二硫键在细胞质中被还原,导致抑制肽的释放。通过 PKC ζ 非依赖性途径诱导肥大细胞脱粒。
T5817 PKC-theta inhibitor hcl

PKC-theta inhibitor

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC-theta inhibitor hcl 是一种选择性 PKC-θ 抑制剂 (IC50:12 nM)。
T8764 PKC-iota inhibitor 1

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC-iota inhibitor 1 是一种蛋白激酶 C-iota(PKC-ι ℩)的抑制剂,IC50值为 0.34 μM。
T61604 PKC-IN-4

PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]
T75885 PKC β pseudosubstrate TFA

PKCβ pseudosubstrate TFA 是一种选择性的、细胞渗透的 PKC 抑制剂。
T76412 PKCδ Peptide Substrate

PKCδPeptide Substrate 是一种δ-typePKC 的特异性底物,其序列与含有 Thr-431 的小鼠 eEF-1α 序列 422-443 相对应。
T80071 PKCζ/ι pseudosubstrate inhibitor

PKCζ/ι偽基質抑制劑對PKC酶家族表現廣譜抑制作用,並可能促成記憶功能障礙。
T35826 PKC fragment (530-558)

PKC fragment (530-558) 是蛋白激酶C (PKC) 的肽片段,是一种有效的 PKC 激活剂。Protein Kinase C (530-558) 可显著抑制破骨细胞骨吸收。
T71993 PKC-9

PKC-9 is a PKC-zeta inhibitor 9.
T62945 Aurora A/PKC-IN-1

Aurora A/PKC-IN-1 (Compound 2e) 是一种有效的 Aurora A (AurA) 和 PKC (α, β1, β2, θ) 双重抑制剂,作用于 AurA (IC50: 6.9 nM) 和 PKCα (IC50: 16.9 nM)。Aurora A/PKC-IN-1 对乳腺癌细胞表现出抗增殖和抗转移作用。
T83754 PKCδ Substrate TFA

Protein Kinase Cδ Substrate

PKCδ substrate是一种用于PKCδ的肽基底,常用于无细胞及细胞内测定中监测PKCδ活性。
T80508 PKCη pseudosubstrate inhibitor,myristoylated

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
Myristoylated PKCη pseudosubstrate inhibitor 是一种具有细胞渗透性的化合物,它主要应用于研究PKCη的作用机制。
T5423 PKC-theta inhibitor

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC-theta inhibitor 是一种PKC-θ抑制剂,IC50值为 12 nM。
T80504 ɛPKC(85–92),Myristoylated

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC(85-92),Myristoylated 是一种结合肉豆蔻酸的细胞渗透性肽,作为 PKC 激活剂,可以增强HUVECs的NO释放。
T81449 PKC-ε translocation inhibitor peptide

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC-ε translocation inhibitor peptide,作为一种特定的PKC-ε易位抑制剂,能够特异性地调控FcγR介导的调理珠内化速率,而对FcαR运输不产生影响。
T80507 PKCθ pseudosubstrate peptide inhibitor,myristoylated

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
Myristoylated PKCθ pseudosubstrate peptide inhibitor 是一款合成肽,专门用于研究 PKCθ 的机制。
T80070 PKCβII Peptide Inhibitor I

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKCβII Peptide Inhibitor I 为一种特定的PKCβII抑制剂。在大鼠心脏缺血/再灌注损伤模型中,该化合物显著表现出心脏保护效应,并能有效预防血管内皮功能障碍。
T80509 PKC 20-28,myristoylated

Myristoylated protein kinase C inhibitor 20-28

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKC20-28,myristoylated(Myristoylated protein kinase C inhibitor 20-28)为具细胞渗透性之PKC抑制剂,可抑制AngII所诱导之IKca电流激活,用途涵盖癌症与心血管疾病研究。
T80505 PKCα (C2-4) inhibitor peptide

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
PKCα(C2-4) inhibitor peptide为专一性PKCα抑制剂,能够抑制α1A‐肾上腺素受体激动剂A-61603对IKr通道的影响。
T10980 DCPLA-ME

Methyl 8-[2-[(2-pentylcyclopropyl)methyl]cyclopropyl]octanoate,2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester,Methyl 8-(2-((2-pentylcyclopropyl)methyl)cyclopropyl)octanoate,DCPLA methyl ester

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
DCPLA-ME (2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester) 是 DCPLA 的甲酯形式。DCPLA-ME 是一种有效的 PKCε 激活剂。DCPLA-ME 可用于研究神经退行性疾病。
T4391 Syk Inhibitor II dihydrochloride

Syk Inhibitor II (hydrochloride)

Others; Tyrosine Kinases; Syk; PKC; BTK Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling; Others; Tyrosine Kinase/Adaptors
Syk Inhibitor II (hydrochloride) 是一种非受体酪氨酸激酶,磷酸化后,它与 FcRγ 链的基于免疫受体酪氨酸的激活基序结合,并介导与血小板功能和炎症相关的下游信号传导。 Syk inhibitor II 是一种可渗透细胞的嘧啶-甲酰胺化合物,以 ATP 竞争性方式选择性和可逆地阻断 Syk (IC50 = 41 nM)。它对 PKCε、PKCβII、ZAP-70、Btk 和 Itk 的效力要低得多(IC50s 分别为5.1、11、11.2、15.5 和 22.6 μM)。
T6280 Enzastaurin

LY317615,恩扎妥林

Apoptosis; PKC; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling
Enzastaurin (LY317615) 是一种PKCβ抑制剂,IC50值为 6 nM。它对 PKCβ 选择性是 PKCα,PKCγ 和 PKCε 的 6-20 倍。
T6278 Sotrastaurin

索曲妥林,AEB071

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
Sotrastaurin (AEB071) 是一种口服有效的泛 PKC 抑制剂,对 PKCθ、PKCβ、PKCα、PKCη、PKCδ 和 PKCε,Ki 分别为 0.22、0.64、0.95、1.8、2.1 和 3.2 nM。
T6643 Ro 31-8220 Mesylate

Ro 31-8220 methanesulfonate,Bisindolylmaleimide IX,Bisindolylmaleimide IX mesylate

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) 是PKC 抑制剂,对 PKCα、PKCβI、PKCβII、PKCγ、PKCε 和大鼠大脑 PKC 的IC50值为 5、24、14、27、24 和 23 nM。它还抑制 MAPKAP-K1b、MSK1、S6K1 和 GSK3β,IC50为3、8、15 和 38 nM。
T13637 DCP-LA

FR236924

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
DCP-LA (FR236924), linoleic acid derivatives, selective and direct activation of PKCε.
T6643L Ro 31-8220

Ro 31-8220 是一种有效的PKC 抑制剂,对 PKCα,PKCβI,PKCβII,PKCγ,PKCε 和大鼠大脑 PKC 的IC50值为 5,24,14,27,24 和 23 nM。Ro 31-8220还显著抑制 MAPKAP-K1b,MSK1,S6K1 和 GSK3β,IC50值分别为3,8,15,38 nM,对 MKK3,MKK4,MKK6 和 MKK7 无作用。
T82007 JH-131e-153

JH-131e-153, 作为一种二酰基甘油(DAG)内酯,具有激活 Munc13-1 的功能,靶向其 C1 结构域。JH-131e-153 对 Munc13-1 激活效率表现为 WT>I590≈R592A≈W588A。值得注意的是,Munc13-1 的 C1 结构域与蛋白激酶 C (PKC) 在序列和结构上具有同源性。对于 Munc13-1 和 PKC 的激活效率,JH-131e-153 的效果排序为 PKCα>Munc13-1>PKCε。该化合物通过调节 Munc13-1,对神经元过程产生影响,因此可用于神经退行性疾病的相关研究。
T78833 AJH-836

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
AJH-836为Munc13-1及PKCε/α激活剂(Kd:4.5 nM PKCα),促进Munc13-1由细胞质转位至质膜,并可应用于神经退行性疾病研究。
T10549 Bisindolylmaleimide VIII acetate

Ro 31-7549 acetate,Bis VIII acetate

Apoptosis; PKC Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) 是一种选择性蛋白激酶 C 抑制剂。它促进 Fas 介导的细胞凋亡,并抑制 T 细胞介导的自身免疫性疾病。
T14328 AS2521780

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).
T36228 Bisindolylmaleimide XI hydrochloride

Bisindolylmaleimide XI hydrochloride 是一种具有口服活性的 PKC 抑制剂,对 PKCα、PKCβI、PKCβII、PKCγ 具有抑制作用(IC50s 分别为 9 nM、28 nM、31 nM、37 nM 和 108 nM)。
T38462 PF-04577806

PF-04577806 is a potent, selective, and ATP competitive inhibitor of the protein kinase C (PKC). It exhibits significant inhibitory activity against various isoforms of PKC, including PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, with IC50 values of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. Furthermore, PF-04577806 has the ability to reverse retinal vascular leakage in diabetic rats.
T17299 (-)-Indolactam V

Indolactam V

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
(-)-Indolactam V is a PKC activator (Kis: 3.36 nM, 1.03 μM for η-CRD2 , γ-CRD2). (-)-Indolactam V also has the Kds are 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1

化合物

PKCε Inhibitor Peptide acetate
Cat.No: T35827L
Synonym: PKCε Inhibitor Peptide acetate(182683-50-7 Free base)
Target: PKC
Epsilon-V1-2
Cat.No: T35827
Synonym: PKCε Inhibitor Peptide,Protein Kinase Cɛ Inhibitor Peptide,ɛV1-2
Target:
Protein Kinase C Peptide Substrate
Cat.No: TP1051
Synonym: PRKCE,Peptide Epsilon,PKCε
Target:
PKCε (85-92)
Cat.No: T80248
Synonym:
Target: PKC
PKCε inhibitor peptide,myristoylated
Cat.No: T80511
Synonym: Myr‐PKCɛ-
Target: PKC
PKCε Inhibitor Scramble Peptide
Cat.No: T81450
Synonym:
Target:
PKCβ inhibitor 1
Cat.No: T8376
Synonym: KUN79359
Target: Apoptosis, PKC
PKC β pseudosubstrate acetate
Cat.No: TP1955L
Synonym: PKC β pseudosubstrate醋酸盐,Protein kinase C beta pseudosubstrate,PKC beta pseudosubstrate,PKC β pseudosubstrate acetate (172308-76-8 Free base)
Target: PKC
PKC-IN-1
Cat.No: T12494
Synonym:
Target: PKC
PKC ζ pseudosubstrate acetate
Cat.No: TP1956L
Synonym: PKC ζ pseudosubstrate acetate (799764-07-1 free base)
Target: PKC
PKC-theta inhibitor hcl
Cat.No: T5817
Synonym: PKC-theta inhibitor
Target: PKC
PKC-iota inhibitor 1
Cat.No: T8764
Synonym:
Target: PKC
PKC-IN-4
Cat.No: T61604
Synonym:
Target:
PKC β pseudosubstrate TFA
Cat.No: T75885
Synonym:
Target:
PKCδ Peptide Substrate
Cat.No: T76412
Synonym:
Target:
PKCζ/ι pseudosubstrate inhibitor
Cat.No: T80071
Synonym:
Target:
PKC fragment (530-558)
Cat.No: T35826
Synonym:
Target:
PKC-9
Cat.No: T71993
Synonym:
Target:
Aurora A/PKC-IN-1
Cat.No: T62945
Synonym:
Target:
PKCδ Substrate TFA
Cat.No: T83754
Synonym: Protein Kinase Cδ Substrate
Target:
PKCη pseudosubstrate inhibitor,myristoylated
Cat.No: T80508
Synonym:
Target: PKC
PKC-theta inhibitor
Cat.No: T5423
Synonym:
Target: PKC
ɛPKC(85–92),Myristoylated
Cat.No: T80504
Synonym:
Target: PKC
PKC-ε translocation inhibitor peptide
Cat.No: T81449
Synonym:
Target: PKC
PKCθ pseudosubstrate peptide inhibitor,myristoylated
Cat.No: T80507
Synonym:
Target: PKC
PKCβII Peptide Inhibitor I
Cat.No: T80070
Synonym:
Target: PKC
PKC 20-28,myristoylated
Cat.No: T80509
Synonym: Myristoylated protein kinase C inhibitor 20-28
Target: PKC
PKCα (C2-4) inhibitor peptide
Cat.No: T80505
Synonym:
Target: PKC
DCPLA-ME
Cat.No: T10980
Synonym: Methyl 8-[2-[(2-pentylcyclopropyl)methyl]cyclopropyl]octanoate,2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester,Methyl 8-(2-((2-pentylcyclopropyl)methyl)cyclopropyl)octanoate,DCPLA methyl ester
Target: PKC
Syk Inhibitor II dihydrochloride
Cat.No: T4391
Synonym: Syk Inhibitor II (hydrochloride)
Target: Others, Tyrosine Kinases, Syk, PKC, BTK
Enzastaurin
Cat.No: T6280
Synonym: LY317615,恩扎妥林
Target: Apoptosis, PKC, Autophagy
Sotrastaurin
Cat.No: T6278
Synonym: 索曲妥林,AEB071
Target: PKC
Ro 31-8220 Mesylate
Cat.No: T6643
Synonym: Ro 31-8220 methanesulfonate,Bisindolylmaleimide IX,Bisindolylmaleimide IX mesylate
Target: PKC
DCP-LA
Cat.No: T13637
Synonym: FR236924
Target: PKC
Ro 31-8220
Cat.No: T6643L
Synonym:
Target:
JH-131e-153
Cat.No: T82007
Synonym:
Target:
AJH-836
Cat.No: T78833
Synonym:
Target: PKC
Bisindolylmaleimide VIII acetate
Cat.No: T10549
Synonym: Ro 31-7549 acetate,Bis VIII acetate
Target: Apoptosis, PKC
AS2521780
Cat.No: T14328
Synonym:
Target: PKC
Bisindolylmaleimide XI hydrochloride
Cat.No: T36228
Synonym:
Target:
PF-04577806
Cat.No: T38462
Synonym:
Target:
(-)-Indolactam V
Cat.No: T17299
Synonym: Indolactam V
Target: PKC
Cat. No. Product Name Target Signaling Pathways
T16791 Rottlerin

Mallotoxin,NSC 56346,粗糠柴苦素,NSC 94525

CaMK; Apoptosis; Others; HIV Protease; PKA; PKC; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Neuroscience; Others; Proteases/Proteasome; Tyrosine Kinase/Adaptors
Rottlerin (NSC-56346) 是一种从Mallotus Philippinensis 中得到的天然产物, 是 PKC 的特异性抑制剂,抑制HIV-1整合和狂犬病病毒感染。它通过活化 caspase 3 诱导细胞凋亡.
TN1047 Ingenol mebutate

Ingenol 3-Angelate,巨大戟醇甲基丁烯酸酯,PEP005

gp120/CD4; HIV Protease; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Ingenol mebutate (Ingenol 3-Angelate) 是 PKC 的有效激动剂,包括 PKC-α、PKC-β、PKC-γ、PKC-δ 和 PKC-ε,Kis 为 0.3、0.105、0.162、0.376 和 0.171 nM。 Ingenol mebutate 具有抗炎和抗肿瘤活性。
T6680 Staurosporine

Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素

Apoptosis; PKA; Antibacterial; Antibiotic; Src; PKC; Antifungal Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。

天然产物

Rottlerin
Cat.No: T16791
Synonym: Mallotoxin,NSC 56346,粗糠柴苦素,NSC 94525
Target: CaMK, Apoptosis, Others, HIV Protease, PKA, PKC, Autophagy
Ingenol mebutate
Cat.No: TN1047
Synonym: Ingenol 3-Angelate,巨大戟醇甲基丁烯酸酯,PEP005
Target: gp120/CD4, HIV Protease, PKC
Staurosporine
Cat.No: T6680
Synonym: Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素
Target: Apoptosis, PKA, Antibacterial, Antibiotic, Src, PKC, Antifungal
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