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19
Cat. No. | Product Name | Target | Signaling Pathways |
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T63682 |
PI3K-IN-2
|
||
PI3K-IN-2 是口服具有活力的 PI3Kβ/δ 抑制剂,他们的 IC50 值分别为7.1 nM、8.6 nM,且选择性高于 PI3Kσ (IC50: 13 nM)、PI3Kγ (IC50: 190 nM) 高。 | |||
T2265 |
Bimiralisib
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2 |
Others; PI3K; S6 Kinase; mTOR | MAPK; Others; PI3K/Akt/mTOR signaling |
Bimiralisib (PI3K-IN-2) 是一种有效的,可渗透脑的 mTOR/PI3K 抑制剂,是一种 mTORC1和 mTORC2抑制剂。它能够抑制 PI3Kα,PI3Kδ,PI3Kβ,PI3Kγ和 mTOR,IC50分别为 33 nM,451 nM,661 nM,708 nM 和 89 nM。 | |||
T6330 |
Linperlisib
PI3Kδ-IN-2 |
PI3K | PI3K/Akt/mTOR signaling |
Linperlisib (PI3Kδ-IN-2) 是一种有效的,效选择性的,具有口服活性的 PI3Kδ的抑制剂,其 IC50=6.4 nM。 | |||
T60564 |
PI3K/Akt/mTOR-IN-2
|
Apoptosis; Akt; PI3K; mTOR | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
PI3K/Akt/mTOR-IN-2 是一种有效的 PI3K/AKT/mTOR 抑制剂。PI3K/Akt/mTOR-IN-2 具有抗癌作用,并对 MDA-MB-231 细胞具有选择性,IC50 为 2.29 μM。PI3K/Akt/mTOR-IN-2 具有抗癌活性,可诱导癌细胞周期阻滞和细胞凋亡 (apoptosis)。 | |||
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。 | |||
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)。 | |||
T72880 |
PI3K/AKT-IN-2
|
||
PI3K/AKT-IN-2 是一种 PI3K 和 AKT 抑制剂。PI3K/AKT-IN-2 阻断上皮-间质转化 (EMT),诱导细胞凋亡 (apoptosis)。PI3K/AKT-IN-2 抑制微管蛋白 (tubulin) 的聚合。 | |||
T62912 |
PI3K/HDAC-IN-2
|
||
PI3K/HDAC-IN-2 是一种有效的 PI3K/HDAC 双重抑制剂,能够作用于 PI3Kα (IC50: 226 nM)、PI3Kβ (IC50: 279 nM)、PI3Kγ (IC50: 467 nM)、PI3Kδ (IC50: 29 nM)、HDAC1 (IC50: 1.3 nM)、HDAC2 (IC50: 3.4 nM)、HDC4 (IC50: 973 nM)、HDAC6 (IC50: 17 nM)、HDAC8 (IC50: 12 nM)。PI3K/HDAC-IN-2 具有 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性,并表现出显着的抗癌作用。 | |||
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。 | |||
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。 | |||
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。 | |||
T1916 |
Apitolisib
RG 7422,GNE 390,GDC-0980 |
Apoptosis; PI3K; mTOR | Apoptosis; PI3K/Akt/mTOR signaling |
Apitolisib (RG 7422) 是一种口服有效的 PI3K 和 mTOR(TORC1/2) 激酶抑制剂,抑制 PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ的活性,IC50值为 5 nM/27 nM/7 nM/14 nM,抑制 mTOR,Ki 为 17 nM。它用于乳腺癌、前列腺癌、肾细胞癌和子宫内膜癌等实体癌的试验研究 。 | |||
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。 | |||
T6883 |
Samotolisib
GTPL8918,LY3023414 |
DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Samotolisib (LY3023414) 在低纳摩尔浓度下,有效抑制mTORC1/2。它选择性地有效抑制PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ、DNA-PK 和mTOR,IC50分别为 6.07 nM、77.6 nM、38 nM、23.8 nM、4.24 nM 和 165 nM。它可用于多种肿瘤和癌症的试验。 | |||
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。 | |||
T36084 |
PKI-179
|
||
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 ... | |||
T74360 |
MEK/PI3K-IN-1
|
||
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。 | |||
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。 | |||
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。 | |||
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]. | |||
T68485 | Apilimod HCl | ||
Apilimod dimesylate is a potent and selective PIKfyve inhibitor. It exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Apilimod dimesylate inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. It reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. It also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma ... | |||
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。 | |||
T22247 | Miransertib (ARQ 092) HCl | ||
Miransertib hydrochloride (ARQ-092 hydrochloride) is a powerful, orally bioavailable, selective, and allosteric inhibitor of Akt. It exhibits an inhibitory concentration (IC50) of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. In addition to its Akt inhibitory activity, Miransertib hydrochloride also demonstrates significant potency as an inhibitor of the AKT1-E17K mutant protein. This compound shows promise in research related to PI3K/AKT-driven tumors and Proteus syndrom... | |||
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 ... | |||
T68980 | MRK003 | ||
MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cel... | |||
T8996 |
AQX-016A
|
||
AQX-016A 是一种口服有效的 SHIP1激动剂。AQX-016A 是 Pelorol 的结构类似物,在相同摩尔浓度下,其效力是海洋天然产物 Pelorol 的 3 倍。AQX-016A 可以在体外激活重组 SHIP1酶并刺激 SHIP1活性。AQX-016A 还可抑制 PI3K 通路和 TNFa 的产生,可用于各种炎症疾病的研究。 | |||
T36308 |
PF-06843195
|
||
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... | |||
T75238 | YS-49 monohydrate | ||
YS-49 (单水合物) 作为PI3K/Akt(RhoA的下游靶点)的激活剂,有效降低3-甲基胆碱处理的细胞中RhoA/PTEN的活性。此外,YS-49通过促进血红素加氧酶(HO-1)的表达,抑制血管紧张素II(Ang II)诱导的血管平滑肌细胞(VSMC)增殖。作为一种异喹啉化合物生物碱,YS-49因激活心脏β-adrenoceptors而显示出显著的正性肌力效应。 | |||
T38263 |
TBK1/IKKε-IN-4
TBK1/IKKε-IN-4 |
||
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... | |||
T35519 |
Aflatoxin B2-13C17
Aflatoxin B2-13C17 |
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Aflatoxin B2-13C17(AFB2-13C17) is intended for use as an internal standard for the quantification of AFB2by GC- or LC-MS. AFB2is a mycotoxin that has been found inA. terricola.1It induces hepatic autophagy and apoptosis in broiler chickens when administered at doses of 0.2, 0.4, and 0.8 mg/kg.2AFB2(0.5 and 1 mg/animal) also induces parenchymal cell hyperplasia in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Alimen... |
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。 | |||
T3923 |
Calycosin
Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮 |
Apoptosis; Tyrosinase | Apoptosis; Proteases/Proteasome |
Calycosin (Cyclosin) 是一抗氧化和抗炎症活性天然产物。 | |||
T6S2099 |
Geraniin
|
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。 | |||
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。 | |||
T2966 |
Beta-Sitosterol
Cupreol,谷甾醇,Beta-Sitosterol,β-Sitosterol,Azuprostat,SKF 14463,beta-谷甾醇,22,23-Dihydrostigmasterol,Betaprost |
Apoptosis; Lipase; Endogenous Metabolite | Apoptosis; Metabolism |
Beta-Sitosterol (SKF 14463) 是一种植物甾醇,干扰细胞周期、细胞凋亡、增殖、存活、侵袭、血管生成和炎症等多种细胞信号通路。 | |||
T3729 |
Ethyl gallate
Nipagallin A,Phyllemblin,gallic acid ethyl ester,没食子酸乙酯 |
MMP; NF-κB; Akt; Antibacterial | Cytoskeletal Signaling; Microbiology/Virology; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Ethyl gallate (gallic acid ethyl ester) 是一种非类黄酮酚过氧化氢清除剂。 | |||
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。 | |||
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
|
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。 | |||
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。 | |||
T3826 |
Polygalasaponin F
异牡荆苷,瓜子金皂苷己 |
NF-κB; TLR; Akt; PI3K | Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling |
Polygalasaponin F 是从瓜子金中提取的齐墩果烷型三萜皂苷,可通过调节TLR4-PI3K/AKT-NF-kB 信号通路减少神经炎症细胞因子的分泌,能降低炎性细胞因子肿瘤坏死因子 α 的释放。 | |||
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。 | |||
T73812 |
Phosphatidylinositol 4,5-bisphosphate
|
||
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。 | |||
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 | |||
TN3806 |
Dehydroglyasperin C
|
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 |