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22

抑制剂 & 化合物

16

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3467	Miransertib ARQ-092,AKT inhibitor 2	Akt; Parasite	Cytoskeletal Signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling
	Miransertib (ARQ-092) 是一种具有口服活性的，选择性和变构性Akt 抑制剂。它有效抑制利什曼原虫，还是 AKT1-E17K 突变蛋白抑制剂，可研究PI3K/AKT 驱动的肿瘤和 Proteus 综合征。
T2423	P7C3-A20	Others	Others
	P7C3-A20 是促神经原性和神经保护活性的 P7C3 衍生物。它具有抗抑郁活性，能够透过血脑屏障，并可用于研究脑损伤。
T13416	ZX-29	ALK	Angiogenesis; Tyrosine Kinase/Adaptors
	ZX-29 是一种选择性ALK 抑制剂，对ALK、ALK L1196M 和ALK G1202R 的IC50分别为 2.1 nM、1.3 nM 和 3.9 nM。它还可诱导保护性自噬并具有抗肿瘤作用。它通过诱导内质网应激来诱导细胞凋亡，并克服了由ALK 突变引起的细胞抗性。
T12412L	PDK4-IN-1 hydrochloride	Apoptosis; PDK	Apoptosis; PI3K/Akt/mTOR signaling
	PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，对丙酮酸脱氢酶激酶 4有抑制作用，IC50为 84 nM，具有口服活性。它抑制细胞转化和细胞增殖并诱导细胞凋亡。它具有抗过敏，抗糖尿病和抗癌作用。
T6203	Saxagliptin BMS-477118,沙克列汀,Onglyza,沙格列汀	Proteasome; DPP-4	Proteases/Proteasome; Ubiquitination
	Saxagliptin (BMS-477118) 是一种选择性，可逆性，竞争性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin 能够用于 2 型糖尿病的研究。
T35528	TD52	Apoptosis; Phosphatase; Akt	Apoptosis; Cytoskeletal Signaling; Metabolism; PI3K/Akt/mTOR signaling
	TD52 是 PP2A (CIP2A) 癌性抑制剂的口服活性抑制剂。 TD52 是厄洛替尼衍生物，通过干扰 Elk1 与 CIP2A 启动子的结合间接降低了 CIP2A。
T0178	Saxagliptin hydrate 沙格列汀单水化合物,Onglyza hydrate,BMS-477118 hydrate	Proteasome; DPP-4	Proteases/Proteasome; Ubiquitination
	Saxagliptin hydrate (Onglyza hydrate) 是一种选择性，竞争性，可逆性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin hydrate 能够用于 2 型糖尿病的研究。
T6730	WAY-600 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶,WAY600	VEGFR; PI3K; Src; mTOR	Angiogenesis; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	WAY-600 是一种有效的，选择性的，ATP 竞争型的mTOR 抑制剂，抑制重组 mTOR 酶，其 IC50=9 nM。它能够阻断 mTOR 复合物 1/2 (mTORC1/2) 组装和激活。
T6731	WYE-354 4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯	Apoptosis; PI3K; mTOR; Autophagy	Apoptosis; Autophagy; PI3K/Akt/mTOR signaling
	WYE-354 是一种 ATP 竞争性的mTOR 抑制剂，IC50为 5 nM。它抑制PI3Kα和PI3Kγ，IC50分别为 1.89 μM 和 7.37 μM，也抑制mTORC1和mTORC2。它在体外能诱导自噬激活。
T6732	WYE-687 N-[4-[4-(4-吗啉基)-1-[1-(3-吡啶甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶-6-基]苯基]氨基甲酸甲酯	p38 MAPK; PI3K; Src; mTOR	Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	WYE-687 是 ATP 竞争性的 mTOR 抑制剂，其 IC50=7 nM。它能够抑制PI3Kα和PI3Kγ，IC50分别为 81 nM 和 3.11 μM。它能够抑制mTORC1和mTORC2活化。
T35528L	TD52 dihydrochloride TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl	Others	Others
	TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti...
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。
T6997	SU6656	FAK; Akt; Src	Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	SU6656 是Src 家族激酶抑制剂，抑制 Src，Yes，Lyn，Fyn 的IC50分别为 280，20，130，170 nM。它还能抑制p-AKT。它可抑制FAK Y576/577、 Y925、Y861位点的磷酸化。
T63259	PP2A Cancerous-IN-1
	PP2A Cancerous-IN-1 是强效的 CIP2A(Cancerous inhibitor of PP2A) 和 p-Akt 抑制剂，表现出强大的抗增殖作用。
T68464	PABA/NO
	PABA/NO is a novel glutathione-S-transferase-p-activated nitric oxide donor, inhibiting proliferation and inducing apoptosis by targeting PI3K/AKT/mTOR and MEK/ERK pathways in hepatocellular carcinoma cells.
T73310	AXL-IN-14	TAM Receptor	Tyrosine Kinase/Adaptors
	AXL-IN-14为有效的口服活性AXL抑制剂，具IC50值0.8 nM。该化合物能抑制Gas6/AXL介导的细胞迁移与侵袭，并降低p-AXL与p-AKT蛋白表达，表现出抗肿瘤活性。
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。
T74833	EGFR T790M/L858R-IN-2
	EGFRT790M/L858R-IN-2是一种有效选择性的EGFRT790M/L858R抑制剂，其对EGFRT790M/L858R和EGFRWT的IC50值分别为3.5nM和1290nM。该化合物能够降低p-EGFR、P-AKT、P-ERK1/2的表达，诱导细胞凋亡及细胞周期在G1期的停滞，显示出抗癌活性。
T73039	CYP1B1-IN-3
	CYP1B1-IN-3为选择性CYP1B1抑制剂，其IC50值分别针对CYP1B1、CYP1A1、CYP1A2为6.6, 347.3, >10000 nM。该化合物能够抑制细胞迁移与侵袭，并作用于P-gp、AKT/ERK、FAK/SRC及EMT信号通路。
T35531	FD223
	FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML[1].
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT...
T36648	Tucatinib hemiethanolate
	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ...

化合物

Cat.No: T3467

Synonym: ARQ-092,AKT inhibitor 2

Target: Akt, Parasite

Cat.No: T2423

Target: Others

Cat.No: T13416

Target: ALK

PDK4-IN-1 hydrochloride

Cat.No: T12412L

Target: Apoptosis, PDK

Cat.No: T6203

Synonym: BMS-477118,沙克列汀,Onglyza,沙格列汀

Target: Proteasome, DPP-4

Cat.No: T35528

Target: Apoptosis, Phosphatase, Akt

Saxagliptin hydrate

Cat.No: T0178

Synonym: 沙格列汀单水化合物,Onglyza hydrate,BMS-477118 hydrate

Target: Proteasome, DPP-4

Cat.No: T6730

Synonym: 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶,WAY600

Target: VEGFR, PI3K, Src, mTOR

Cat.No: T6731

Synonym: 4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯

Target: Apoptosis, PI3K, mTOR, Autophagy

Cat.No: T6732

Synonym: N-[4-[4-(4-吗啉基)-1-[1-(3-吡啶甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶-6-基]苯基]氨基甲酸甲酯

Target: p38 MAPK, PI3K, Src, mTOR

TD52 dihydrochloride

Cat.No: T35528L

Synonym: TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl

Target: Others

Cat.No: T14214

Target: PI3K

Cat.No: T6997

Target: FAK, Akt, Src

PP2A Cancerous-IN-1

Cat.No: T63259

Cat.No: T68464

Cat.No: T73310

Target: TAM Receptor

Cat.No: T79701

Target: Akt

EGFR T790M/L858R-IN-2

Cat.No: T74833

Cat.No: T73039

Cat.No: T35531

Cat.No: T35897

Tucatinib hemiethanolate

Cat.No: T36648

Cat. No.	Product Name	Target	Signaling Pathways
TN4761	Phellamurin	P-gp	Membrane transporter/Ion channel; Neuroscience
	Phellamurin 是一种来自黄檗叶的黄酮糖苷，可诱导细胞凋亡，具有抗肿瘤活性。它抑制肠道 P-糖蛋白，还抑制凤蝶的产卵。
T3981	Acacetin 4'-Methoxyapigenin,金合欢素,5,7-Dihydroxy-4'-methoxyflavone,Linarigenin	Apoptosis; IAP; COX; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Neuroscience
	Acacetin (5,7-Dihydroxy-4'-methoxyflavone) 是一种来自狗舌草的口服有效类黄酮。它停在 PI3Kγ 的 ATP 结合口袋中，可导致癌细胞周期停滞，并诱导细胞凋亡和自噬。它有抗癌和抗炎活性，有潜力研究疼痛相关疾病。
TL0006	Cichoric Acid 菊苣酸,Dicaffeoyltartaric acid,Chicoric Acid	Reactive Oxygen Species; HIV Protease	Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome
	Cichoric Acid (Dicaffeoyltartaric acid) 是一种天然化合物，具有抗氧化作用。
T2S0500	Ilexsaponin A 毛冬青皂苷A,毛冬青皂苷甲,Ilexsaponin A1	Others	Others
	Ilexsaponin A (Ilexsaponin A1)1 是分离自冬凌草的根中，利用抗凋亡途径减轻缺血再灌注引起的心肌损伤。它能够减少心肌梗塞的大小，减少 LDH，AST 和 CK-MB 的血清水平，促进细胞活力并抑制缺氧/复氧心肌细胞的凋亡。
T2799	(20S)-Protopanaxadiol 20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇	Apoptosis; Reactive Oxygen Species; P-gp	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB
	(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) 是人参皂甙的代谢产物，是一种凋亡诱导剂，抑制Akt 活性并诱导多种肿瘤细胞凋亡。
T4085	Paris saponin VII 重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII	Apoptosis; BCL; Others; PARP; p38 MAPK; Akt; Caspase; P-gp; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Membrane transporter/Ion channel; Neuroscience; Others; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Paris saponin VII (Dioscini) 是从延龄草的根和根茎中分离的一种甾体皂苷。它减弱线粒体膜电位，增加凋亡相关蛋白的表达，并降低Bcl-2、caspase-9、caspase-3、PARP-1和p-Akt 的蛋白表达水平。它在 K562/ADR 细胞中诱导强烈的自噬，可研究白血病。
T3752	4-Hydroxybenzyl alcohol 4-Methylolphenol,P-Methylolphenol,对羟基苯甲醇	Apoptosis; Endogenous Metabolite	Apoptosis; Metabolism
	4-Hydroxybenzyl alcohol (P-Methylolphenol) 是广泛分布于各种植物中的一种酚类天然产物，具有抗炎、抗氧化和抗伤害感受活性。它抑制肿瘤血管生成和生长，有神经保护作用。
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。
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。
T3780	Oroxin B Hypocretin-2,木蝴蝶苷B	Apoptosis; PTEN; Antioxidant; PI3K; Autophagy	Apoptosis; Autophagy; oxidation-reduction; PI3K/Akt/mTOR signaling
	Oroxin B (Hypocretin-2) 是从传统中草药木蝴蝶中分离出来的黄酮类天然产物，在恶性淋巴瘤细胞中诱导肿瘤抑制性 ER 应激。它通过上调 PTEN，下调 COX-2，VEGF，PI3K 和 p-AKT，对肝癌细胞具有明显的抑制作用，诱导细胞早期凋亡。
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。
T2698	Asperosaponin VI Akebia saponin D,Asperosaponin Ⅵ,川续断皂苷 VI	Apoptosis; Others; Caspase	Apoptosis; Others; Proteases/Proteasome
	Asperosaponin VI (Akebia saponin D) 是一种来自续断壁的皂苷组分。它通过增加 Bcl-2/Bax 比值，降低活性 caspase-3 表达，以及增强 p-Akt 和 p-CREB，从而抑制缺氧诱导的心肌细胞凋亡。它通过 BMP-2/p38 和 ERK1/2 信号途径诱导成骨细胞分化。
T2163	Dihydrocapsaicin CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide	Others; TRP/TRPV Channel	Membrane transporter/Ion channel; Others
	Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。
T27807	13-Methyltetradecanoic acid LeDSF3
	LeDSF3 is a regulator of the biosynthesis of the antifungal polycyclic tetramate macrolactam HSAF in Lysobacter enzymogenes and anti-tumor agent. LeDSF3 down-regulates p-AKT and activates caspase-3.
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: TN4761

Target: P-gp

Cat.No: T3981

Synonym: 4'-Methoxyapigenin,金合欢素,5,7-Dihydroxy-4'-methoxyflavone,Linarigenin

Target: Apoptosis, IAP, COX, Autophagy

Cat.No: TL0006

Synonym: 菊苣酸,Dicaffeoyltartaric acid,Chicoric Acid

Target: Reactive Oxygen Species, HIV Protease

Cat.No: T2S0500

Synonym: 毛冬青皂苷A,毛冬青皂苷甲,Ilexsaponin A1

Target: Others

(20S)-Protopanaxadiol

Cat.No: T2799

Synonym: 20-Epiprotopanaxadiol,20(S)-APPD,20 (S)-原人参二醇,原人参二醇

Target: Apoptosis, Reactive Oxygen Species, P-gp

Paris saponin VII

Cat.No: T4085

Synonym: 重楼皂苷 VII,Chonglou Saponin VII,Polyphyllin-VII,Dioscinin,Paris saponin-VII

Target: Apoptosis, BCL, Others, PARP, p38 MAPK, Akt, Caspase, P-gp, Autophagy

4-Hydroxybenzyl alcohol

Cat.No: T3752

Synonym: 4-Methylolphenol,P-Methylolphenol,对羟基苯甲醇

Target: Apoptosis, Endogenous Metabolite

Cat.No: T3927

Target: GABA Receptor

Cat.No: T3729

Synonym: Nipagallin A,Phyllemblin,gallic acid ethyl ester,没食子酸乙酯

Target: MMP, NF-κB, Akt, Antibacterial

Cat.No: T6S0653

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

Target: TNF, AChE

Cat.No: T3780

Synonym: Hypocretin-2,木蝴蝶苷B

Target: Apoptosis, PTEN, Antioxidant, PI3K, Autophagy

Glaucocalyxin A

Cat.No: T4S0498

Synonym: 蓝萼甲素,Wangzaozin B,Leukamenin F

Target: Apoptosis, Akt, Caspase, PI3K

Asperosaponin VI

Cat.No: T2698

Synonym: Akebia saponin D,Asperosaponin Ⅵ,川续断皂苷 VI

Target: Apoptosis, Others, Caspase

Dihydrocapsaicin

Cat.No: T2163

Synonym: CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide

Target: Others, TRP/TRPV Channel

13-Methyltetradecanoic acid

Cat.No: T27807

Synonym: LeDSF3

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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