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Search Results for " pi3k/akt-in-1 "

28

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
T83658	SQLE-IN-1	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。
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。
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。
T72227	PI3K/Akt/CREB activator 1
	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。
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。
T21964	KP372-1
	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。
T35491	3,5-dimethyl PIT-1
	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...
T61656	Antitumor agent-53
	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。
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...
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。
T72780	HSP90/mTOR-IN-1
	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。
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].
T71284	Glimepiride urethane
	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...
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。
T78836	IHMT-PI3K-455	PI3K	PI3K/Akt/mTOR signaling
	IHMT-PI3K-455（Compound 15u）为一种高效、选择性且具口服活性的PI3Kγ/δ双重抑制剂，其针对PI3Kγ与PI3Kδ的IC50值分别为7.1 nM和0.57 nM。该化合物能够抑制AKT磷酸化，并通过促进CD8+杀伤性T细胞的招募与激活，抑制肿瘤生长，适用于肿瘤学研究领域。
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。
T70352	PH11
	PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL...
T79658	PI3Kδ-IN-14	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。
T79449	Antileishmanial agent-19	Parasite	Microbiology/Virology
	Antileishmanial agent-19 (Compound F27)是一种有效的抗利什曼病试剂，其对L. donovani promastigotes的IC50值为3.39 μM。该化合物能够抑制L. donovani promastigotes中的脯氨酰-tRNA合成酶，并干预宿主PI3K/Akt/CREB轴，从而抑制IL-10的分泌。此外，Antileishmanial agent-19能诱导L. donovani promastigotes自噬介导的细胞凋亡(apoptosis)过程，并在感染的动物体内显著减少寄生虫负担。
T60365	SY-LB-35
	SY-LB-35 是骨形态发生蛋白 (BMP) 受体的有效激动剂。SY-LB-35 可以刺激 C2C12 成肌细胞系中细胞数量和细胞活力的显著增加，并引起细胞周期向 S 期和 G2/M 期转变。SY-LB-35 刺激典型的 Smad 和非典型的 PI3K/Akt、ERK、p38和 JNK 胞内信号通路。
T37476	Cyclo(L-Phe-L-Val)
	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-...
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...
T36309	AZ2 AZ2
	AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). AZ2 can be used for the research of inflammatory and immune diseases[1]. AZ2 (0.1~100 nM; 1 hour; SKOV-3 cells) excellent selectivity for PI3Kγ is further confirmed with a constitutively activated PI3K/Akt pathway[1]. [1]. Gangadhara G, et al. A class of highly selective inhibitors bind to an active state of PI3Kγ. Nat Chem Biol. 2019;15(4):348-357.
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-1

Cat.No: T62997

Cat.No: T1826

Synonym: Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409

Target: DNA-PK, PI3K

Cat.No: T83658

Target: Antifungal

Cat.No: T14214

Target: PI3K

Cat.No: T63957

PI3K/Akt/CREB activator 1

Cat.No: T72227

Cat.No: T79701

Target: Akt

Cat.No: T21964

3,5-dimethyl PIT-1

Cat.No: T35491

Antitumor agent-53

Cat.No: T61656

Acetyl-Exenatide

Cat.No: T76648

Miransertib (ARQ 092) HCl

Cat.No: T22247

Anticancer agent 164

Cat.No: T78608

Target: Apoptosis

HSP90/mTOR-IN-1

Cat.No: T72780

Cat.No: T61476

Glimepiride urethane

Cat.No: T71284

Cat.No: T82971

Cat.No: T78836

Target: PI3K

Cat.No: T71827

Cat.No: T70352

Cat.No: T79658

Target: PI3K

Antileishmanial agent-19

Cat.No: T79449

Target: Parasite

Cat.No: T60365

Cyclo(L-Phe-L-Val)

Cat.No: T37476

YS-49 monohydrate

Cat.No: T75238

TBK1/IKKε-IN-4

Cat.No: T38263

Synonym: TBK1/IKKε-IN-4

Cat.No: T36309

Synonym: AZ2

Aflatoxin B2-13C17

Cat.No: T35519

Synonym: Aflatoxin B2-13C17

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。
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。
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。
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。
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。
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。
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。
T79971	Asparanin A	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	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

Cat.No: T5S1331

Target: c-Met/HGFR, Akt

Cat.No: T6S0653

Synonym: Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷

Target: TNF, AChE

Cat.No: T6S1699

Synonym: [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol

Target: Lipoxygenase, Autophagy

Cat.No: T6S2099

Target: Antioxidant, TNF

Cat.No: T6S1740

Synonym: 苷松新酮,甘松新酮

Target: Others

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

Cat.No: T5S1982

Synonym: Periplocoside,杠柳毒苷

Target: Apoptosis, Others

Glaucocalyxin A

Cat.No: T4S0498

Synonym: 蓝萼甲素,Wangzaozin B,Leukamenin F

Target: Apoptosis, Akt, Caspase, PI3K

Aurantio-obtusin

Cat.No: T6S1559

Target: Others

6-O-Isobutyrylbritannilactone

Cat.No: T75554

Cat.No: T79971

Target: Apoptosis

Dehydroglyasperin C

Cat.No: TN3806

Target: ERK, IκB/IKK, p38 MAPK, TNF, NF-κB, Akt, COX, PI3K, NADPH, DNA/RNA Synthesis, Nrf2, JNK, Autophagy

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