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Cat. No. | Product Name | Target | Signaling Pathways |
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T1826 |
PI3K-IN-1
Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409 |
DNA-PK; PI3K | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI3K-IN-1 (Voxtalisib Analogue) 是 PI3K 抑制剂,PI3K-IN-1(25 μM) 能够阻断 PI3K/Akt 信号通路。 | |||
T12365 |
PARP/PI3K-IN-1
|
PARP; PI3K | Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PARP/PI3K-IN-1 是一种 新型双重聚(ADP-核糖)聚合酶(PARP)和磷酸肌醇 3-激酶(PI3K)双重抑制剂,具有抗癌、抗肿瘤和抗癌细胞增殖活性,可用于研究乳腺癌、胰腺癌和肺癌。 | |||
T12455 | PI3K/HDAC-IN-1 | PI3K | PI3K/Akt/mTOR signaling |
PI3K/HDAC-IN-1 is a potent PI3K and HDAC dual inhibitor(IC50s of 8.1 nM and 1.4 nM, respectively). | |||
T16422 |
P110δ-IN-1
PWT-143 |
PI3K | PI3K/Akt/mTOR signaling |
P110δ-IN-1 (PWT-143) 是一种有效的、选择性的P110δ抑制剂,其 IC50=8.4 nM。 | |||
T7015 |
Vps34-IN-1
VPS34-IN1 |
PI3K; Autophagy | Autophagy; PI3K/Akt/mTOR signaling |
Vps34-IN-1 (VPS34-IN1) 是一种有效且高度选择性的 Vps34 抑制剂,可调节自噬,IC50为4nM。 | |||
T74360 |
MEK/PI3K-IN-1
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MEK/PI3K-IN-1(compound 6r)是一种高效的MEK/PI3K抑制剂,IC50值为124 nM(MEK1)、130 nM(PI3Kα)及236 nM(PI3Kδ)。该化合物能够降低pAKT和pERK1/2的活性,并展现对肿瘤细胞的抗增殖作用。 | |||
T62103 | COX-2/PI3K-IN-1 | ||
COX-2/PI3K-IN-1 (compound 5d) 是一种 PI3K 的有效抑制剂 (IC50: 1.14 nM)。COX-2/PI3K-IN-1 是一种 COX-2 的选择性抑制剂 (Ki: 3.24 nM)。COX-2/PI3K-IN-1 显示出抗炎和抗癌效果。 | |||
T62997 | PI3K/AKT-IN-1 | ||
PI3K/AKT-IN-1 是一种有效的、双重的 PI3K/AKT 抑制剂,能够作用于 PI3Kγ (IC50: 6.99 μM)、PI3Kδ (IC50: 4.01 μM) 和 AKT (IC50: 3.36 μM)。PI3K/AKT-IN-1 通过抑制 PI3K/AKT 通路,诱导 caspase 3 依赖性凋亡,表现出抗癌作用。 | |||
T72713 |
PI3K/VEGFR2-IN-1
|
PI3K | PI3K/Akt/mTOR signaling |
PI3K/VEGFR2-IN-1是一种具有双重抑制效应的化合物,对PI3K和VEGFR2的IC50分别为2.21 μM和68 μM,能够诱导细胞凋亡(apoptosis),在癌症研究中应用。 | |||
T14214 |
AMG 511
|
PI3K | PI3K/Akt/mTOR signaling |
AMG 511 是一种高效的、口服有效的 I 类 pan-PI3K 抑制剂,对 PI3Kα, β, δ 和 γ 作用的 Ki 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。它它显著抑制了 PI3K 信号,减少 p-Akt (Ser473)。它在小鼠胶质母细胞瘤移植瘤模型中具有抗肿瘤作用。 | |||
T36083 |
DS-7423
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
DS-7423 是PI3K 和mTOR 的有效抑制剂,抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。 | |||
T83658 |
SQLE-IN-1
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Antifungal | Microbiology/Virology |
SQLE-IN-1 是一种角鲨烯环氧化酶 (SQLE) 抑制剂,具有抗肿瘤活性,可抑制肝癌细胞系 Huh7 的增殖和迁移能力,抑制细胞胆固醇的生成,增加抑癌基因PTEN的表达,抑制PI3K和AKT的蛋白表达。 | |||
T63790 |
Cbl-b-IN-3
|
E1/E2/E3 Enzyme | Ubiquitination |
Cbl-b-IN-3是一种有效的casitas b 系淋巴瘤原癌基因-b (Cbl-b)抑制剂(ic50 < 1 nM)。Cbl-b 是一种环型E3泛素蛋白连接酶,与T 淋巴细胞激活阈值的设定有关。Cbl-b 以不依赖于蛋白水解的方式负调控p85,通过其E3泛素连接酶活性,参与了p85向CD28和T 细胞抗原受体ζ的募集,抑制PI3K 抑制了Cblb-/- t 细胞活化的增强。 | |||
T16328 |
Nitroaspirin
2-乙酰氧基苯甲酸-3-硝酸甲基苯酯,NCX 4016 |
Apoptosis; COX | Apoptosis; Immunology/Inflammation; Neuroscience |
Nitroaspirin (NCX 4016) 是一氧化氮供体和阿司匹林的硝基衍生物,与 Aspirin 结合可抑制环氧合酶=,可作为 COX-1 的直接和不可逆抑制剂。 它通过下调 EGFR/PI3K/STAT3 信号传导和调节 Bcl-2 家族蛋白,显着诱导顺铂耐药人卵巢癌细胞的细胞周期停滞和凋亡,具有抗血栓和抗血小板特性。 | |||
T22794 |
G36
G-36 |
Estrogen Receptor/ERR | Endocrinology/Hormones |
G36是一种细胞可渗透的G 蛋白偶联雌激素受体(GPER/GPR30)的非甾体拮抗剂。G36抑制17β-雌二醇或GPER 选择性激动剂G-1的激活(IC50分别为112和165 nM)。G36对ERα或ERβ均无可检测的结合活性。G36通过GPER 阻断由雌激素触发的PI3K 的激活或钙动员,并且它通过雌激素或G-1而不是通过EGF 抑制ERK 的激活。 | |||
T63957 | PI3K-IN-29 | ||
PI3K-IN-29 是一种有效的 PI3K 抑制剂。PI3K-IN-29 对 U87MG、HeLa 和 HL60 细胞具有较好的抑制作用,IC50值分别为 0.264、2.04 和 1.14 µM。PI3K-IN-29 通过抑制PI3K 催化的Akt 的磷酸化来抑制PI3K/Akt 通路。 | |||
T79701 |
PI3K-IN-48
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
PI3K-IN-48,PI3K抑制剂,对A549细胞系表现出1.55 ± 0.18 μM的IC50值。该化合物能够诱导G0/G1期细胞周期阻滞与细胞凋亡,并可下调p-PI3K与p-Akt的表达水平,适用于人类肺癌研究。 | |||
T36084 |
PKI-179
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PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ... | |||
T60769 | COX-2/PI3K-IN-2 | ||
COX-2/PI3K-IN-2 (compound 5f) 显示出抗癌和抗炎的特性。它是COX-2的选择性抑制剂(Ki = 3.02 nM),也是PI3K 的有效抑制剂 (IC50 = 2.78 nM)。 | |||
T79566 |
PI3K-IN-41
|
PI3K | PI3K/Akt/mTOR signaling |
PI3K-IN-41(compound 2)是一种具抗癌特性的光笼PI3K抑制剂(IC50=18.92 nM),适用于精确控制的癌症治疗。在紫外线照射下,PI3K-IN-41能有效抑制PI3K活性,并增强其抗癌效果。 | |||
T72227 |
PI3K/Akt/CREB activator 1
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PI3K/Akt/CREB activator 1 是一种口服有效的PI3K/Akt/CREB 的激活剂。PI3K/Akt/CREB activator 1 通过 PI3K/Akt/CREB 通路上调脑源性神经营养因子,促进神经元增殖,诱导 Neuro-2a 细胞分化成神经元样形态,加速海马原代神经元轴突-树突极化的建立。PI3K/Akt/CREB activator 1 可用于血管性痴呆 (VaD) 的研究。 | |||
T74361 | MEK/PI3K-IN-2 | ||
MEK/PI3K-IN-2 (compound 6s) 是一种有效的 MEK/PI3K 抑制剂,其 IC50值分别为 352 nM (MEK1), 107 nM (PI3Kα), 和 137 nM (PI3Kδ)。MEK/PI3K-IN-2 抑制 pAKT 和 pERK1/2 水平。MEK/PI3K-IN-2 对肿瘤细胞具有抗增殖活性。 | |||
T62545 |
HDAC-IN-43
|
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HDAC-IN-43 是一种强效的 HDAC 1/3/6 抑制剂,对 HDAC 1、HDAC 3 和 HDAC 6 的 IC50 值分别为 82 nM、45 nM 和 24 nM。HDAC-IN-43 是一种弱的 PI3K/mTOR 抑制剂,对 PI3K 和 mTOR 的 IC50 值分别为 3.6 μM 和 3.7 μM。HDAC-IN-43 具有广谱的抗增殖效果。 | |||
T35491 |
3,5-dimethyl PIT-1
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PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorab... | |||
T21964 |
KP372-1
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KP372-1是一种 Akt 的抑制剂,通过阻断 PI3K 通路信号,抑制细胞增殖,同时诱导癌细胞凋亡,可用于头颈部鳞状细胞癌的研究。 | |||
T78853 |
PI3K-IN-47
|
PI3K | PI3K/Akt/mTOR signaling |
PI3K-IN-47 (Compound 27) 是一款高度选择性的二价PI3K抑制剂,对PI3Kα具有极低的半抑制浓度(IC50: 0.44 nM), 同时对PI3Kβ、PI3Kγ、PI3Kδ也表现出良好的抑制活性(IC50分别为7.18 nM、13.92 nM、22.83 nM)。此化合物能够有效诱导细胞周期在G1期发生暂停,并且在体外抑制集落形成和细胞迁移。对于HGC-27异种移植的小鼠模型,PI3K-IN-47能够显著抑制肿瘤生长。 | |||
T61627 | iMDK quarterhydrate | ||
iMDK quarterhydrate, a potent PI3K inhibitor, is effective in inhibiting the growth factor MDK (also known as midkine or MK) while demonstrating suppression of non-small cell lung cancer (NSCLC). In combination with a MEK inhibitor, iMDK quarterhydrate demonstrates cooperative inhibition of NSCLC without causing harm to normal cells and mice [1]. | |||
T61587 | ATR-IN-15 | ||
ATR-IN-15 (compound 1) is a highly potent and orally active inhibitor of ATR kinase with an IC50 of 8 nM. Additionally, ATR-IN-15 demonstrates inhibitory activity against several targets, including human colon tumor cells LoVo, DNA-PK, and PI3K, with IC50 values of 47, 663, and 5131 nM, respectively [1]. | |||
T35534 |
7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine
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7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine is a building block.1It has been used in the synthesis of PI3K inhibitors. 1.Scott, W.J., Hentemann, M.F., Rowley, R.B., et al.Discovery and SAR of novel 2,3-dihydroimidazo[1,2-c]quinazoline PI3K inhibitors: Identification of copanlisib (BAY 80-6946)ChemMedChem.11(14)1517-1530(2016) | |||
T81499 | PH14 | PI3K | PI3K/Akt/mTOR signaling |
PH14,作为一种PI3K/HDAC双重抑制剂,对PI3Kα和HDAC3表现出强效抑制能力,其IC50值分别为20.3 nM 和24.5 nM 。该化合物不仅具备抗增殖特性,还能有效诱导Jeko-1细胞走向凋亡,是研究癌症(例如淋巴瘤)的有力工具。 | |||
T61656 |
Antitumor agent-53
|
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Antitumor agent-53 is a potent compound that effectively inhibits tumor growth. It achieves this by inducing cell cycle arrest at the G2/M phase and promoting apoptosis in HGC-27 cells through the inhibition of the PI3K/AKT pathway. Furthermore, Antitumor agent-53 holds promise for further research in the treatment of gastrointestinal tumors [1]. | |||
T76648 |
Acetyl-Exenatide
|
||
Acetyl-Exenatide为Exenatide的乙酰化衍生物,具有类似胰岛素的功能,适用于2型糖尿病研究。它能促进Th17细胞分化,同时抑制Treg细胞分化,并下调PI3K/Akt/FoxO1的磷酸化水平。 | |||
T62724 | AQX-435 | ||
AQX-435 是一种有效的 SHIP1 (SH2 domain-containing inositol-5′-phosphatase 1) 激活剂。AQX-435 能够降低 B 细胞受体 (BCR) 下游 PI3K 活性,诱导恶性 B 细胞凋亡,对淋巴瘤生长表现出抑制作用。 | |||
T75723 |
740 Y-P TFA
|
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740 Y-P TFA (740YPDGFR;PDGFR740Y-P) 是一个有效的,具有细胞渗透性的PI3K 激活剂。740 Y-P TFA 很容易结合含有 p85 的 N- 和 C- 末端 SH2 结构域的 GST 融合蛋白,但不能单独结合 GST。 | |||
T36308 |
PF-06843195
|
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PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1]. PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells w... | |||
T78608 | Anticancer agent 164 | Apoptosis | Apoptosis |
CML-IN-1(compound 7)是一种高效抗癌药物,针对人类慢性粒细胞白血病(CML)细胞系K562,能有效诱导凋亡(apoptosis)。该化合物主要通过显著抑制PI3K/Akt信号通路的蛋白磷酸化来发挥作用,同时CML-IN-1(compound 4)也能通过抑制结直肠癌的MEK/ERK信号通路来阻止细胞增殖。 | |||
T74782 | CXJ-2 | PI3K | PI3K/Akt/mTOR signaling |
CXJ-2,一种环状肽,对EDP(弹性蛋白衍生肽)具中等亲和力。该化合物有效抑制PI3K/ERK通路,减少肝星状细胞的增殖与迁移,展现出显著的抗纤维化能力。 | |||
T36314 |
Wortmannin-Rapamycin Conjugate
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Phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1. Wortmannin-rapamycin conjugate consists of analogs of 17-hydroxy wortmannin and rapamycin conjugated via a prodrug linker. Hydrolysis of the prodrug linker in vivo releases the inhibitors. The wortmannin-rapamycin conjugate inhibits the growth of HT-29 colon tumors and A498 renal tumors in... | |||
T78568 |
PI3Kδ-IN-15
|
PI3K | PI3K/Akt/mTOR signaling |
PI3Kδ-IN-15(compound 6b)为一选择性PI3Kδ抑制剂,p110δ的IC50为0.5 nM,其对PI3Kδ的抑制效力高于PI3Kγ、PI3Kβ及PI3Kα30倍。 | |||
T79482 |
Anticancer agent 137
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PI3K | PI3K/Akt/mTOR signaling |
Anticanceragent 137 (8q) 是一种高效的 PI3k 抑制剂,展现出广谱的抗肿瘤活性。它能够诱导 G2/M 阶段的细胞周期阻滞与细胞凋亡(apoptosis),并促进 PARP、caspase 3 和 caspase 7 的裂解。该化合物主要用于癌症相关的生物医学研究。 | |||
T38263 |
TBK1/IKKε-IN-4
TBK1/IKKε-IN-4 |
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TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK... | |||
T72780 |
HSP90/mTOR-IN-1
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HSP90/mTOR-IN-1 是一种有效的Hsp90和mTOR 抑制剂,IC50分别为 69 nM 和 29 nM。HSP90/mTOR-IN-1 通过过度激活PI3K/AKT/mTOR 通路抑制 SW780 细胞增殖。HSP90/mTOR-IN-1 通过对HSP90和mTOR 的选择性抑制来诱导细胞凋亡 (apoptosis) 和细胞自噬 (autophagy)。HSP90/mTOR-IN-1 在异种移植小鼠体内也表现出良好的抗肿瘤活性。HSP90/mTOR-IN-1 可用于膀胱癌的研究。 | |||
T82971 | ARI-1 | ||
ARI-1是一种针对受体酪氨酸激酶样孤儿受体ROR1的抑制剂,对于ROR1异常表达所致的非小细胞肺癌(NSCLC)及EGFR-TKI诱导的耐药性治疗具有显著效果。该化合物能够特异性结合至ROR1的胞外卷曲结构域,并以ROR1依赖性方式抑制PI3K/AKT/mTOR信号通路,进而有效地阻断NSCLC细胞的增殖和迁移。此外,ARI-1还展现了显著的体内抗肿瘤活性。 | |||
T81468 | PI3Kδ-IN-17 | PI3K | PI3K/Akt/mTOR signaling |
PI3Kδ-IN-17 (Compound S5) 是一种PI3Kδ抑制剂,其IC50值为2.82 nM。该化合物在SU-DHL-6细胞中对增殖活性具有显著抑制效果,IC50为0.035 μM。 | |||
T61476 | Thioridazine | ||
Thioridazine is a chemical compound characterized by its potent anti-psychotic and anti-anxiety activities. As an antagonist of the dopamine receptor D2 family proteins, it exhibits a strong inhibitory effect on the PI3K-Akt-mTOR signaling pathways, resulting in anti-angiogenic effects. It also demonstrates significant antiproliferative and apoptosis induction effects in a diverse range of cancer cells, specifically targeting cancer stem cells (CSCs) [1] [2] [3] [4]. | |||
T36421 | Immuno-Oncology Screening Library | ||
The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list ... | |||
T37476 |
Cyclo(L-Phe-L-Val)
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Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1 that can autoinduce production of antibacterial substances active against S. aureus when co-cultured at a low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro when used at concentrations of 16 and 32 μM. It increases phosphorylation of the PI3K substrate Akt, and neurite outgrowth induced by cyclo(L-Phe-L-Val) can be blocked by the PI3K inhibitor LY294002 . Cyclo(L-... | |||
T71827 |
AG-205
|
||
(rac)-AG-205 是一种对孕激素受体膜组分1 (Pgrmc1) 的有效抑制剂,并能诱导参与甾醇合成的基因表达,这些基因涉及 INSIG1 蛋白与 PGRMC1 形成复合物的过程。(rac)-AG-205 能够抑制 NF-kB 信号及 BDNF/PI3K/AKT 通路的活化,从而防止神经元对缺氧缺血状况的抵抗。 | |||
T79658 |
PI3Kδ-IN-14
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PI3K | PI3K/Akt/mTOR signaling |
PI3Kδ-IN-14(化合物(S)-29)是一种高选择性PI3Kδ抑制剂,具有出色的靶点亲和力(IC50为0.8 nM,Kd为84.8 nM)。该化合物特异性结合至PI3Kδ激酶的ATP结合位点,并通过抑制PI3K/AKT信号通路发挥抗炎作用。此外,PI3Kδ-IN-14在改善急性肺损伤(ALI)方面显示出潜在效果。 | |||
T71284 |
Glimepiride urethane
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Glimepiride urethane is a third generation sulfonylurea compound, which increases the release of insulin from pancreatic beta cells. In addition, glimepiride increases the activity of intracellular insulin receptors. Glimepiride increases osteoblast proliferation and differentiation, which is thought to be related to its ability to activate the PI3K and Akt pathway. Furthermore, Glimepiride enhances intrinsic peroxisome proliferator-activated receptor γ activity. Glimepiride also increases prote... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T5S1331 |
Herbacetin
|
c-Met/HGFR; Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Herbacetin 是一种亚麻籽中的天然类黄酮,具有多种药理活性,如抗氧化、抗炎、抗癌作用。 它是鸟氨酸脱羧酶Ornithine decarboxylase (ODC)变构抑制剂,能够直接与 ODC 上的 Asp44,Asp243 和 Glu384 结合。其中鸟氨酸脱羧酶是多胺生物合成中的限速酶。 | |||
T3410 |
Momordin Ic
地肤子皂苷Ic,地肤子皂苷 Ic,Momordin 1c |
Apoptosis; MAPK; PI3K | Apoptosis; MAPK; PI3K/Akt/mTOR signaling |
Momordin Ic (Momordin 1c) 是山茱萸的主要皂苷成分,通过氧化应激调控线粒体功能障碍诱导细胞凋亡,具有抗癌活性。 | |||
T3S0013 |
Ethyl trans-caffeate
咖啡酸乙酯,Ethyl caffeate,Caffeic Acid Ethyl Ester |
Others | Others |
Ethyl trans-caffeate (Caffeic Acid Ethyl Ester) 具有抗炎作用。 它是一种有前途的天然化合物,未来在慢性肝病中的应用。它是一种有效的化学预防化合物,可防止因太阳紫外线照射引起的皮肤癌变。它是与人胰腺α-淀粉酶复合的代表性抑制剂的高分辨率结构。 它强烈抑制 JB6 Cl41细胞的肿瘤转化,无毒性。 PI3K、ERK1/2 和 p38 激酶活性在体外通过与 HOEC 直接结合而受到抑制。 | |||
T6S0653 |
Linarin
Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷 |
TNF; AChE | Apoptosis; Neuroscience |
Linarin (Acacetin-7-O-rutinoside) 是一种选择性的乙酰胆碱酯酶 (AChE) 抑制剂,从薄荷花提取物中分离得到。 | |||
T6S2099 |
Geraniin
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Antioxidant; TNF | Apoptosis; oxidation-reduction |
Geraniin 是一种肿瘤坏死因子α释放抑制剂,其IC50值为 43 μM,具有抗肿瘤、抗炎和抗高血糖活性。 | |||
T6S1699 |
Shogaol
[6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol |
Lipoxygenase; Autophagy | Autophagy; Metabolism |
6-Shogaol (6-Shogaol) 是从生姜中分离的一种天然产物,具有抗癌、抗炎和抗氧化的多种生物活性。 | |||
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。 | |||
T6S1315 |
Oroxylin A
千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether |
Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy | Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology |
Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮,具有较强的抗癌作用。 | |||
T5S1982 |
Periplocin
Periplocoside,杠柳毒苷 |
Apoptosis; Others | Apoptosis; Others |
Periplocin (Periplocoside) 是从黑龙骨中分离出的一种强心类固醇。它可促进肿瘤细胞凋亡并抑制肿瘤生长。它通过激活 Na/K-ATPase 介导的 Src/ERK 和 PI3K/Akt 途径,具有促进伤口愈合的潜力。 | |||
T6S1559 |
Aurantio-obtusin
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Others | Others |
Aurantio-obtusin 是从决明子中分离出的蒽醌类化合物,具有抗炎、抗凝血、抗氧化、抗高血压的活性。它能抑制 IgE 介导的肥大细胞和过敏模型中的过敏反应,具有研究过敏相关疾病的潜力。在大鼠中,它通过内皮细胞 PI3K/AKT/ eNOS 依赖信号通路放松全身动脉,是潜在的新型血管扩张剂。 | |||
T2836 |
Isorhamnetin
3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin |
MEK; PI3K; Endogenous Metabolite | MAPK; Metabolism; PI3K/Akt/mTOR signaling |
Isorhamnetin (3-methylquercetin) 是从中草药沙棘中提取的一种类黄酮,可通过抑制MEK1和PI3K 来抑制皮肤癌。 | |||
T4S0498 |
Glaucocalyxin A
蓝萼甲素,Wangzaozin B,Leukamenin F |
Apoptosis; Akt; Caspase; PI3K | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜,具有抗肿瘤作用。它通过调节PI3K/Akt 信号通路抑制 GLI1 的核易位,诱导骨肉瘤凋亡。 | |||
T3S2344 |
β,β-Dimethylacrylshikonin
β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin |
ERK; HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; MAPK; Metabolism |
β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物,从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达,促进血管生成,具有抗肿瘤活性。 | |||
T73812 |
Phosphatidylinositol 4,5-bisphosphate
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Phosphatidylinositol 4,5-bisphosphate(L-alpha-Phosphatidylinositol-4,5-bisphosphate)为细胞膜磷脂成分,主要作为磷脂酶C(PLC)与磷酸肌醇3-激酶(PI3K)的底物,充当重要信使。 | |||
T37751 |
Streptazolin
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Streptazolin is a fungal metabolite originally isolated from S. viridochromogenes. It increases NF-κB activity when used at concentrations ranging from 60 to 130 μg/ml, at least in part, via PI3K signaling. Streptazolin enhances TNF-α secretion induced by LPS and enhances IL-8 secretion when used alone or in combination with LPS in THP-1 Blue cells. | |||
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。 | |||
TN3655 |
Cimiside E
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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 | |||
T79971 |
Asparanin A
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Apoptosis | Apoptosis |
Asparanin A 是一种具有抗癌活性的凋亡 (apoptosis) 诱导剂。它能够通过线粒体和 PI3K/AKT 信号通路使细胞周期在 G0/G1 期停滞,并有效抑制癌细胞生长。此外,Asparanin A 在小鼠Ishikawa子宫内膜癌异种移植模型中显示出显著的体内抑制肿瘤生长效力。 | |||
TN3806 |
Dehydroglyasperin C
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ERK; IκB/IKK; p38 MAPK; TNF; NF-κB; Akt; COX; PI3K; NADPH; DNA/RNA Synthesis; Nrf2; JNK; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Metabolism; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling |
Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neuroprotective activities, it has protective effects against chronic diseases |