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11

抑制剂 & 化合物

15

天然产物

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Cat. No. Product Name Target Signaling Pathways
T72880 PI3K/AKT-IN-2

PI3K/AKT-IN-2 是一种 PI3KAKT 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。
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)。
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。
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。
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...
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].
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。
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...
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

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...

化合物

PI3K/AKT-IN-2
Cat.No: T72880
Synonym:
Target:
PI3K/Akt/mTOR-IN-2
Cat.No: T60564
Synonym:
Target: Apoptosis, Akt, PI3K, mTOR
AMG 511
Cat.No: T14214
Synonym:
Target: PI3K
Acetyl-Exenatide
Cat.No: T76648
Synonym:
Target:
Miransertib (ARQ 092) HCl
Cat.No: T22247
Synonym:
Target:
Thioridazine
Cat.No: T61476
Synonym:
Target:
Anticancer agent 164
Cat.No: T78608
Synonym:
Target: Apoptosis
MRK003
Cat.No: T68980
Synonym:
Target:
YS-49 monohydrate
Cat.No: T75238
Synonym:
Target:
TBK1/IKKε-IN-4
Cat.No: T38263
Synonym: TBK1/IKKε-IN-4
Target:
Aflatoxin B2-13C17
Cat.No: T35519
Synonym: Aflatoxin B2-13C17
Target:
Cat. No. Product Name Target Signaling Pathways
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。
TN1013 Cucurbitacin D

Apoptosis Apoptosis
Cucurbitacin D 是一种从 Ecballium elaterium (L.)分离出来的三萜类化合物,具有抗癌抗肿瘤活性,抑制转移性 PrC 中的葡萄糖摄取和乳酸产生,诱导独立于 ERK1/2 激活的炎症小体激活。 Cucurbitacin D 是巨噬细胞中的一种新的炎症小体激活剂,通过调节 JAK/STAT3、PI3K/Akt/mTOR 和 MAPK 信号通路抑制 HepG2 细胞增殖并诱导细胞凋亡, 可用于研究宫颈癌、白血病和前列腺癌。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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。
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

天然产物

Herbacetin
Cat.No: T5S1331
Synonym:
Target: c-Met/HGFR, Akt
Cucurbitacin D
Cat.No: TN1013
Synonym:
Target: Apoptosis
Ethyl gallate
Cat.No: T3729
Synonym: Nipagallin A,Phyllemblin,gallic acid ethyl ester,没食子酸乙酯
Target: MMP, NF-κB, Akt, Antibacterial
Linarin
Cat.No: T6S0653
Synonym: Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷
Target: TNF, AChE
Calycosin
Cat.No: T3923
Synonym: Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮
Target: Apoptosis, Tyrosinase
Beta-Sitosterol
Cat.No: T2966
Synonym: Cupreol,谷甾醇,Beta-Sitosterol,β-Sitosterol,Azuprostat,SKF 14463,beta-谷甾醇,22,23-Dihydrostigmasterol,Betaprost
Target: Apoptosis, Lipase, Endogenous Metabolite
Shogaol
Cat.No: T6S1699
Synonym: [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol
Target: Lipoxygenase, Autophagy
Geraniin
Cat.No: T6S2099
Synonym:
Target: Antioxidant, TNF
Oroxylin A
Cat.No: T6S1315
Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether
Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy
Nardosinone
Cat.No: T6S1740
Synonym: 苷松新酮,甘松新酮
Target: Others
Glaucocalyxin A
Cat.No: T4S0498
Synonym: 蓝萼甲素,Wangzaozin B,Leukamenin F
Target: Apoptosis, Akt, Caspase, PI3K
Periplocin
Cat.No: T5S1982
Synonym: Periplocoside,杠柳毒苷
Target: Apoptosis, Others
Aurantio-obtusin
Cat.No: T6S1559
Synonym:
Target: Others
Polygalasaponin F
Cat.No: T3826
Synonym: 异牡荆苷,瓜子金皂苷己
Target: NF-κB, TLR, Akt, PI3K
Dehydroglyasperin C
Cat.No: TN3806
Synonym:
Target: ERK, IκB/IKK, p38 MAPK, TNF, NF-κB, Akt, COX, PI3K, NADPH, DNA/RNA Synthesis, Nrf2, JNK, Autophagy
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