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40

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。
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。
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。
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)。
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...
T40101	(±)-1,2-Diolein 1,2-Dioleoyl-rac-glycerol,甘油1,2-二油酸酯	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) 是一种PKC 激活剂，可以增加肌小管 Ca2+内流。
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。
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。
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]
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。
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。
T71993	PKC-9
	PKC-9 is a PKC-zeta inhibitor 9.
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
T9863	PKCiota-IN-2 PKCiota-IN-49	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	PKCiota-IN-2 (PKCiota-IN-49) 是一种有效的 PKCiota (PKC-ι) 抑制剂，IC50 为 2.8 nM。PKCiota-IN-2 还抑制 PKC-α 和 PKC-ε，IC50 分别为 71 nM 和 350 nM。
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。
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。
T3689	Ruboxistaurin hydrochloride Ruboxistaurin,LY333531 HCl,LY 333531 hydrochloride,芦布妥林	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是蛋白激酶 C(PKC) 的同工酶选择性抑制剂，竞争性且可逆地抑制 PKCβI 和 PKCβII，IC50 值分别为 4.7 和 5.9 nM。
T72919	PKCiota-IN-1
	PKCiota-IN-1 是一种有效的 PKCiota (PKC-ι)抑制剂，IC50为 2.7 nM。PKCiota-IN-1 还抑制PKC-α和PKC-ε，IC50分别为 45 nM 和 450 nM。
T76388	Protein kinase C α peptide TFA
	Protein kinase C α peptide (TFA) 为PKC-α的脂质依赖性丝氨酸/苏氨酸蛋白激酶多肽片段，关键调节细胞生存、增殖、分化、迁移及粘附等过程。
T69914	Variegatic acid
	Variegatic acid is a natural inhibitor of β-hexosaminidase release and tumor necrosis factor (TNF)-α secretion from rat basophilic leukemia (RBL 2H3) cells, with IC50 values of 10.4 μM and 16.8 μM, respectively, also inhibiting PKC β1 activity with an IC50 value of 36.2 μM.
T69438	MT477
	MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.
T74691	Aprinocarsen sodium
	Aprinocarsen (ISIS 3521) sodium，是针对蛋白激酶C-α（PKC-α）的特异性反义寡核苷酸抑制剂，为一种20-mer寡核苷酸，通过调节细胞分化和增殖来发挥作用。其能有效抑制人类肿瘤细胞系在裸鼠体内的生长，展示了作为人类癌症化疗化合物的潜力。
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。
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
T35536	Tpl2 Kinase Inhibitor (hydrochloride)
	Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...

化合物

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 ζ pseudosubstrate acetate

Cat.No: TP1956L

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

Target: PKC

PKCβ inhibitor 1

Cat.No: T8376

Synonym: KUN79359

Target: Apoptosis, PKC

PKCε Inhibitor Peptide acetate

Cat.No: T35827L

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

Target: PKC

PKC-iota inhibitor 1

Cat.No: T8764

Target: PKC

PKC-theta inhibitor hcl

Cat.No: T5817

Synonym: PKC-theta inhibitor

Target: PKC

Cat.No: T35827

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

(±)-1,2-Diolein

Cat.No: T40101

Synonym: 1,2-Dioleoyl-rac-glycerol,甘油1,2-二油酸酯

Target: PKC

PKC fragment (530-558)

Cat.No: T35826

PKC β pseudosubstrate TFA

Cat.No: T75885

PKCδ Peptide Substrate

Cat.No: T76412

PKCζ/ι pseudosubstrate inhibitor

Cat.No: T80071

Cat.No: T61604

PKCδ Substrate TFA

Cat.No: T83754

Synonym: Protein Kinase Cδ Substrate

Cat.No: T12494

Target: PKC

Cat.No: T71993

PKCε (85-92)

Cat.No: T80248

Target: PKC

Aurora A/PKC-IN-1

Cat.No: T62945

PKCε Inhibitor Scramble Peptide

Cat.No: T81450

ɛPKC(85–92),Myristoylated

Cat.No: T80504

Target: PKC

PKC-theta inhibitor

Cat.No: T5423

Target: PKC

PKCε inhibitor peptide,myristoylated

Cat.No: T80511

Synonym: Myr‐PKCɛ-

Target: PKC

PKCη pseudosubstrate inhibitor,myristoylated

Cat.No: T80508

Target: PKC

PKC 20-28,myristoylated

Cat.No: T80509

Synonym: Myristoylated protein kinase C inhibitor 20-28

Target: PKC

PKCθ pseudosubstrate peptide inhibitor,myristoylated

Cat.No: T80507

Target: PKC

PKCβII Peptide Inhibitor I

Cat.No: T80070

Target: PKC

PKC-ε translocation inhibitor peptide

Cat.No: T81449

Target: PKC

PKCα (C2-4) inhibitor peptide

Cat.No: T80505

Target: PKC

Cat.No: T9863

Synonym: PKCiota-IN-49

Target: PKC

Bisindolylmaleimide VIII acetate

Cat.No: T10549

Synonym: Ro 31-7549 acetate,Bis VIII acetate

Target: Apoptosis, PKC

Ro 31-8220 Mesylate

Cat.No: T6643

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

Target: PKC

Ruboxistaurin hydrochloride

Cat.No: T3689

Synonym: Ruboxistaurin,LY333531 HCl,LY 333531 hydrochloride,芦布妥林

Target: PKC

Cat.No: T72919

Protein kinase C α peptide TFA

Cat.No: T76388

Variegatic acid

Cat.No: T69914

Cat.No: T69438

Aprinocarsen sodium

Cat.No: T74691

Cat.No: T78833

Target: PKC

(-)-Indolactam V

Cat.No: T17299

Synonym: Indolactam V

Target: PKC

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Cat. No.	Product Name	Target	Signaling Pathways
T2A2481	Taurochenodeoxycholic Acid Chenodeoxycholyltaurine,TCDCA,Chenyltaurine,Taurochenodeoxycholate,12-Deoxycholyltaurine,牛磺鹅去氧胆酸	Apoptosis; TNF; Caspase; Endogenous Metabolite	Apoptosis; Metabolism; Proteases/Proteasome
	Taurochenodeoxycholic Acid (12-Deoxycholyltaurine) 是动物胆汁酸的主要生物活性物质之一，可诱导细胞凋亡，具有明显的抗炎和免疫调节作用。
TN2215	Taurochenodeoxycholic acid sodium 牛磺鹅去氧胆酸钠盐,Sodium taurochenodeoxycholate,牛磺鹅去氧胆酸钠	Apoptosis; Endogenous Metabolite	Apoptosis; Metabolism
	Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) 是动物胆汁酸的主要生物活性物质之一。它可诱导细胞凋亡，具有抗炎和免疫调节作用。
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。
TN1299	Desmethylglycitein 4',6,7-三羟基异黄酮,4',6,7-三羟异黄酮,6-羟基大豆苷元,6,7,4'-Trihydroxyisoflavone	PI3K; CDK; PKC	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Desmethylglycitein (6,7,4'-Trihydroxyisoflavone) 是大豆中苷元的代谢产物，具有抗氧化性和抗癌活性。它是蛋白激酶 C(PKC)α 的直接抑制剂，抑制正常人皮肤成纤维细胞中的太阳紫外线诱导的基质金属蛋白酶1。它在体内直接结合CDK1和CDK2，抑制 CDK1 和 CDK2 活性。
TN3655	Cimiside E	ERK; TNF; ROS; Akt; PI3K; PKC; PPAR	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Metabolism; PI3K/Akt/mTOR signaling
	Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/2, PI3K, and PKC are involved in this effect.Cimiside E may be an effective chemopreventive agen
TN5593	Euphohelioscopin A
	Euphohelioscopin A, an activator of protein kinase C (PKC), it inhibits proliferation and induces differentiation of the myeloid leukemia cell lines THP-1 and HL-60. Euphohelioscopin A has anti-inflammary activity, it exhibits moderate inhibitory activity

天然产物

Taurochenodeoxycholic Acid

Cat.No: T2A2481

Synonym: Chenodeoxycholyltaurine,TCDCA,Chenyltaurine,Taurochenodeoxycholate,12-Deoxycholyltaurine,牛磺鹅去氧胆酸

Target: Apoptosis, TNF, Caspase, Endogenous Metabolite

Taurochenodeoxycholic acid sodium

Cat.No: TN2215

Synonym: 牛磺鹅去氧胆酸钠盐,Sodium taurochenodeoxycholate,牛磺鹅去氧胆酸钠

Target: Apoptosis, Endogenous Metabolite

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

Desmethylglycitein

Cat.No: TN1299

Synonym: 4',6,7-三羟基异黄酮,4',6,7-三羟异黄酮,6-羟基大豆苷元,6,7,4'-Trihydroxyisoflavone

Target: PI3K, CDK, PKC

Cat.No: TN3655

Target: ERK, TNF, ROS, Akt, PI3K, PKC, PPAR

Euphohelioscopin A

Cat.No: TN5593

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