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Search Results for " pkc-in-1 "

31

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
T14860	CaMKII-IN-1	CaMK; Autophagy	Autophagy; Neuroscience
	CaMKII-IN-1是高效的 CaMKII 选择性抑制剂，IC50为63nM，对 CaMKIV, MLCK, p38a, Akt1,和 PKC 这些靶点几乎无作用。
T35407	Ζ-Stat	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	ζ-Stat 是非典型的、特异性的PKC-ζ抑制剂，IC50为 5 μM。ζ-Stat 能够减少黑色素瘤细胞系的增殖并诱导细胞凋亡，在体外显示除抗肿瘤活性。
TP1924L1	ZIP acetate(863987-12-6 free base)	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	ZIP acetate(863987-12-6 free base) 是一种新型的细胞渗透性蛋白激酶 Mζ (PKMζ) 抑制剂，它是一种参与 LTP 维持的组成型活性非典型 PKC 同工酶。在体外选择性阻断 PKMζ 诱导的海马切片突触增强。逆转晚期 LTP (IC50 = 1 - 2.5 μM) 并在体内中央给药后导致 1 天前的空间记忆持续丧失。
T8969	API-1 NSC177223	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	API-1 (NSC-177223) 是Akt/PKB 抑制剂，可同 PH 结构域相结合并抑制 Akt 膜易位，有效降低 Akt 的磷酸化水平。它可选择性的抑制PKB，对 PKC 和 PKA 的激活无抑制作用。它可以和 TNF 相关的凋亡诱导配体协同作用从而诱导细胞凋亡。
T0825	Ebselen SPI-1005,PZ-51,依布硒,CCG-39161	Phosphatase; Virus Protease; Calcium Channel; COX; HIV Protease	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。
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。
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...
T76422	Protein Kinase C (661-671)
	Protein Kinase C (661-671) 是蛋白激酶 C (PKC) β1 亚种的片段肽。PKC 在细胞生长控制和肿瘤促进中发挥作用。
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。
T75887	[Ala113]MBP(104-118) TFA
	[Ala113]MBP(104-118) TFA 是 protein kinase C (PKC)的非竞争性的肽抑制剂，IC50值范围为 28-62 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]
T35829	CC-90005
	CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS...
T83684	Myelin Basic Protein Peptide (mouse, bovine) TFA Gln-Lys-Arg-Pro-Ser-Gln-Arg-Ser-Lys-Tyr-Leu,MBP Peptide
	Myelin基础蛋白(MBP)肽是PKC的肽底物，相比PKA、酪蛋白激酶1(CK1)、CK2、磷酸化酶激酶及钙/钙调蛋白依赖性蛋白激酶(CaMKII)，它对PKC有选择性。MBP肽已用于监测原发性人类肾动脉平滑肌细胞中的PKC活性。
T76486	Ac-MBP (4-14) Peptide
	Ac-MBP (4-14) Peptide 是一种乙酰化的 MBP (4-14) Peptide。MBP (4-14) Peptide 是一种选择性的 (蛋白激酶 C)PKC 底物。Ac-MBP (4-14) Peptide 可用于提取物中的PKC 检测，无需事先纯化便可消除干扰蛋白激酶或磷酸酶。
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。
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。
T76008	Protein Kinase C (19-31) (TFA)
	Protein Kinase C (19-31) TFA 是蛋白激酶 C (PKC)的抑制剂,是由 PKCa (残基 19-31) 伪底物调控域衍生而来，25 位丝氨酸取代野生型丙氨酸作为蛋白激酶 C 底物肽，用于检测蛋白激酶 C 的活性。Protein kinase C (PKC) TFA 通过磷酸化丝氨酸和苏氨酸氨基酸残基上的羟基来调控其它蛋白的功能。
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。
T83692	EGFR Peptide (human, mouse) (myristoylated) TFA Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide,N-myristoyl-RKRTLRRL
	EGFR peptide (myristoylated) 是一种合成的肽类PKC抑制剂，其IC50值为5µM，与EGFR内部区域的氨基酸序列相对应。当浓度为1µM时，可以逆转紫外线-2237M (UV-2237M-ADRR) 成纤维细胞瘤细胞对多柔比星的抗药性。
TP1924	ZIP
	Novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-phase LTP (IC50 = 1
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。
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。
T76185	N-Myristoyl-Lys-Arg-Thr-Leu-Arg
	N-Myristoyl-Lys-Arg-Thr-Leu-Arg 是一种蛋白激酶 C (PKC) 抑制剂，其 IC50值为 75 μM。N-Myristoyl-Lys-Arg-Thr-Leu-Arg 抑制人白血病细胞系 Jurkat 中 IL-2受体的诱导和 IL-2的产生。
T75937	Pep2m, myristoylated TFA
	Pep2m, myristoylated TFA (Myr-Pep2m TFA)为具备细胞渗透性的肽。该化合物通过破坏PKMζ与其下游靶点NSF/GluR2的相互作用而发挥作用，其中PKMζ为具有自主活性的PKC同工酶。
T76021	Myelin Basic Protein TFA
	Myelin Basic Protein (MHP4-14) TFA 是一种合成肽，包含髓鞘碱性蛋白的残基4-14，是一种非常有选择性的 PKC 底物 (Km=7 μM)。Myelin Basic Protein TFA 不被环腺苷酸依赖性蛋白激酶、酪蛋白激酶 I 和 II、Ca2+/钙调素依赖性蛋白激酶 II 或磷酸化酶激酶磷酸化，可常规用于测定粗组织提取物中低背景的蛋白激酶 C。
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。
T75989	Malantide TFA
	Malantide TFA 是一种合成的十二肽，由被磷酸化酶激酶β亚基上的PKA 磷酸化的位点衍生而来。Malantide TFA 是PKA 的高度特异性底物，Km 为 15 μM，并且在各种大鼠组织提取物中显示出 PKI 抑制 > 90％底物磷酸化。Malantide TFA 也是PKC 的有效底物，Km 为 16 μM。
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...
T36679	Rp-cAMPS sodium salt
	Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic t...

化合物

Cat.No: T12494

Target: PKC

Aurora A/PKC-IN-1

Cat.No: T62945

Cat.No: T14860

Target: CaMK, Autophagy

Cat.No: T35407

Target: PKC

ZIP acetate(863987-12-6 free base)

Cat.No: TP1924L1

Target: PKC

Cat.No: T8969

Synonym: NSC177223

Target: Akt

Cat.No: T0825

Synonym: SPI-1005,PZ-51,依布硒,CCG-39161

Target: Phosphatase, Virus Protease, Calcium Channel, COX, HIV Protease

Cat.No: T72919

Cat.No: T35827

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

Protein Kinase C (661-671)

Cat.No: T76422

ɛPKC(85–92),Myristoylated

Cat.No: T80504

Target: PKC

[Ala113]MBP(104-118) TFA

Cat.No: T75887

Cat.No: T61604

Cat.No: T35829

Myelin Basic Protein Peptide (mouse, bovine) TFA

Cat.No: T83684

Synonym: Gln-Lys-Arg-Pro-Ser-Gln-Arg-Ser-Lys-Tyr-Leu,MBP Peptide

Ac-MBP (4-14) Peptide

Cat.No: T76486

PKC 20-28,myristoylated

Cat.No: T80509

Synonym: Myristoylated protein kinase C inhibitor 20-28

Target: PKC

Cat.No: T82007

Protein Kinase C (19-31) (TFA)

Cat.No: T76008

Cat.No: T78833

Target: PKC

EGFR Peptide (human, mouse) (myristoylated) TFA

Cat.No: T83692

Synonym: Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide,N-myristoyl-RKRTLRRL

Cat.No: TP1924

Protein kinase C α peptide TFA

Cat.No: T76388

Aprinocarsen sodium

Cat.No: T74691

N-Myristoyl-Lys-Arg-Thr-Leu-Arg

Cat.No: T76185

Pep2m, myristoylated TFA

Cat.No: T75937

Myelin Basic Protein TFA

Cat.No: T76021

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

Synonym: Tat-A-kinase Anchor Protein 79 (326-336)

Cat.No: T75989

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Rp-cAMPS sodium salt

Cat.No: T36679

Cat. No.	Product Name	Target	Signaling Pathways
T3927	Phellopterin	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Phellopterin 是一种分离自P. trifoliata 中的天然产物。它能够调节 Akt 和 PKC 通路，抑制 TNF-alpha 诱导的 VCAM-1 表达，进而减少单核细胞与内皮细胞的粘附。
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。
T6S1740	Nardosinone 苷松新酮,甘松新酮	Others	Others
	Nardosinone 是一个 dbcAMP 和 staurosporine 的神经生成作用增强剂，分离自Nardostachys chinensis 中。Nardosinone 可能成为一种有用的药理学工具，不仅可用于研究神经生长因子 (NGF) 的作用机理，而且可用于研究神经毒性物质的作用机理。
T35895	Ingenol 3,20-dibenzoate
	Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms. It effectively induces the translocation of nPKC-delta, -epsilon, and -theta as well as PKC-mu from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].
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
T38262	Sphingosine (d14:1)
	Sphingosine (d14:1) is a bioactive sphingolipid that has been found in B. mori (silkworm), P. clarkii (crayfish), and A. aurita (jellyfish) extracts. It increases the germination rate of N. rileyi, an entomopathogenic fungus, with an EC50 value of 10.2 nM. Sphingosine (d14:1) inhibits protein kinase C (PKC) in vitro (IC50 = 7.3 mol%) as well as superoxide generation induced by phorbol 12-myristate 13-acetate in neutrophils and reduces growth of CHO cells (IC50s = 19 and 8 μM, respectively).
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

Cat.No: T3927

Target: GABA Receptor

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: T6S1740

Synonym: 苷松新酮,甘松新酮

Target: Others

Ingenol 3,20-dibenzoate

Cat.No: T35895

Cat.No: TN3655

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

Sphingosine (d14:1)

Cat.No: T38262

Euphohelioscopin A

Cat.No: TN5593

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