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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10274 |
AKT-IN-2
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1). | |||
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)。 | |||
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。 | |||
T36310 |
AKT-IN-6
INCB-047775 |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT-IN-6 (INCB-047775)对ATK 有抑制作用。Akt 是对生长因子、细胞因子和其他细胞刺激的细胞信号传导的重要组成部分。Akt 的异常激活与2型糖尿病和癌症的发生密切相关。 | |||
T39988 |
6'-GNTI dihydrochloride
|
Opioid Receptor; Akt | Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Neuroscience; PI3K/Akt/mTOR signaling |
6'-GNTI dihydrochloride 是一种κ-阿片受体(KOR)激动剂,它偏向于激活 G 蛋白介导的信号传导,而不是β-阿司匹林2的募集。6'-GNTI dihydrochloride 只能激活纹状体神经元中的 Akt 通路。 | |||
T72968 |
ZINC00640089
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
ZINC00640089 是一种选择性的脂质运载蛋白-2 (LCN2) 抑制剂。ZINC00640089 对细胞增殖、细胞活力有抑制作用,可减少 SUM149 细胞的 AKT 磷酸化水平。ZINC00640089 可用于研究炎症性乳腺癌 (IBC) 。 | |||
T8656 |
CAY10404
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T |
Apoptosis; Akt; COX | Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; PI3K/Akt/mTOR signaling |
CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) 是一种有效且高度选择性的 COX-2 和 COX-1 抑制剂。 它还是 PKB/Akt 和 MAPK 信号通路的有效抑制剂,可诱导 NSC-LC 细胞凋亡,具有镇痛、抗炎和抗癌活性。 | |||
T50107 |
ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate
|
Others | Others |
ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate 是一种合成化合物,属于姜黄素家族。它通过抑制NF-κB 信号通路参与免疫反应和炎症的调节,通过激活Nrf2信号通路参与抗氧化反应的调节,通过抑制Akt 信号通路参与细胞存活和增殖的调节。 | |||
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。 | |||
T4444 |
A-674563 HCl (552325-73-2(free base))
|
ERK; Akt; PKA; CDK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
A-674563 HCl (552325-73-2(free base)) 是一种口服的、ATP 竞争性的、可逆的 Akt 抑制剂(Akt1 的 Ki:11 nM)。它对 PKA 和 Cdk2 具有抑制活性(IC50:16/46 nM),但对 Akt1 的选择性比 CMGC、CAMK 和 TK 家族中的其他激酶高 10 至 >1800 倍。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。 | |||
T72885 |
Akt1&PKA-IN-1
|
||
Akt1&PKA-IN-1 是一种有效的Akt/PKA 双重抑制剂,对 PKAa、Akt 和CDK2的IC50值分别为 0.03、0.11 μM 和 9.8 μM。Akt1&PKA-IN-1 对细胞周期蛋白依赖性激酶 2 (CDK2) 具有选择性。 | |||
T35489 |
1-O-Octadecyl-2-O-methyl-sn-glycerol
|
||
1-O-Octadecyl-2-O-methyl-sn-glycerol is a metabolite of a phosphotidylinositol ether lipid analog (PIA). PIAs are known to target the pleckstrin homology domain of the serine/threonine kinase Akt and to induce apoptosis in cancer cell lines with high levels of endogenous Akt activity. | |||
T35490 |
2-Amino-5-bromo-6-chloropyrazine
|
||
2-Amino-5-bromo-6-chloropyrazine is a heterocyclic building block.1,2It has been used in the synthesis of Akt inhibitors. 1.Kettle, J.G., Brown, S., Crafter, C., et al.Diverse heterocyclic scaffolds as allosteric inhibitors of AKTJ. Med. Chem.55(3)1261-1273(2012) 2.Goel, R., Luxami, V., and Paul, K.Recent advances in development of imidazo[1,2-a]pyrazines: Synthesis, reactivity and their biological applicationsOrg. Biomol. Chem.13(12)3525-3555(2015) | |||
T79722 |
2-Chlorophenoxazine
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
2-Chlorophenoxazine为Akt抑制剂,体外IC50为2-5 μM,能够诱导细胞凋亡(apoptosis),适用于癌症病理研究。 | |||
T29543 |
ACAF4
ACAF-4,ACAF 4 |
||
ACAF4 is a neurotrophic agent which significantly increases survival in PC12 neuronal cells and enhances the effect of nerve growth factor (NGF). ACAF4 induces neurite outgrowth, and modulates ERK1/2 and AKT signaling pathways. | |||
T62013 |
PI3Kδ-IN-10
|
||
PI3Kδ-IN-10 是高效的、具有口服活性的PI3Kδ抑制剂(IC50= 2 nM)。在肝细胞癌模型中,PI3Kδ-IN-10 强烈抑制下游AKT 通路,并诱导细胞凋亡(apoptosis)。 | |||
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... | |||
T72886 |
Akt1&PKA-IN-2
|
||
Akt1&PKA-IN-2 ((R)-29) 是一种具有周期蛋白依赖性激酶 2 (CDK2) 选择性的酰胺类 PKB/AKT 抑制剂。Akt1&PKA-IN-2 抑制 AKT1、PKAa 和 CDK2a,IC50值分别为 0.007 µM、0.01 µM 和 0.69 µM。 | |||
T70926 | BRN-103 | ||
BRN-103 was found to suppress the VEGF-induced phosphorylation of VEGF receptor 2 (VEGR2) and the activations of AKT and eNOS. Taken together, these results suggest that BRN-103 inhibits VEGF-mediated angiogenesis signaling in human endothelial cells. | |||
T78149 |
ZINC00784494
|
Others | Others |
ZINC00784494 是一种特异性脂质运载蛋白-2(LCN2)抑制剂,可阻抑细胞增殖和活力,同时减少SUM149细胞的AKT磷酸化水平,对炎症性乳腺癌(IBC)具有研究潜力。 | |||
T61522 | Nrf2/HO-1 activator 2 | ||
Nrf2/HO-1 activator 2 (compound 13m), a difluoro-substituted derivative, is a highly potent activator of Nrf2/HO-1. It exhibits substantial neuroprotective and antioxidant properties by activating the Nrf2/HO-1 pathway through phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. This compound finds utility in the investigation of Parkinson's disease (PD) [1]. | |||
T63967 |
Multi-kinase-IN-2
|
||
Multi-kinase-IN-2 是口服具有活力的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 能够显著抑制血管激酶的活性,如 VEGFR-1/2/3、PDGFRα/β、FGFR-1、LYN 和 c-KIT 激酶。Multi-kinase-IN-2 能够明显减弱 AKT 和 ERK 蛋白的磷酸化,并可诱导细胞凋亡 (apoptosis),具有抗癌作用。 | |||
T79458 |
YF704
|
||
YF704 (化合物 4w) 作为一种选择性SHP2变构抑制剂,具有0.25 μM的半抑制浓度(IC50)。该化合物在癌细胞中表现出抗增殖效果,并能诱导细胞凋亡。YF704 同时能够降低癌细胞内Erk1/2和Akt的磷酸化水平。 | |||
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。 | |||
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。 | |||
T69990 |
Ruboxistaurin mesylate monohydrate
|
||
Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt. | |||
T3689L |
Ruboxistaurin mesylate
LY-333531,LY333531,LY 333531,LY-333531 Mesylate |
||
Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/ | |||
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]. | |||
T81784 |
MK-2206 free base
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MK-2206 free base是一种口服活性、高选择性的变构Akt抑制剂,IC50分别针对Akt1、Akt2、Akt3为8、12和65 nM 。多种乳腺癌细胞系、PIK3CA突变以及PTEN缺失细胞系对此化合物敏感,显示出抗癌活性。 | |||
T76800 | Dalotuzumab | ||
Dalotuzumab (MK-0646) 是一种靶向IGF-1R 的重组人源化单克隆抗体 (IgG1 型)。Dalotuzumab 通过抑制IGF-1和IGF-2介导的肿瘤细胞增殖、IGF-1R 自体磷酸化和Akt 磷酸化而发挥作用。Dalotuzumab 还可诱导细胞凋亡和周期停滞。Dalotuzumab 与其他抗癌活性分子(如他汀类活性分子)共同使用,可增强 Dalotuzumab 的体外和体内抗肿瘤活性。 | |||
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。 | |||
T35855 |
AAA
|
||
AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension... | |||
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... | |||
T79487 | MAO A/HSP90-IN-2 | Monoamine Oxidase | Neuroscience |
MAO A/HSP90-IN-2(compound 4-C)是一种针对HSP90和MAO A的双重抑制剂,显示出分别对这两种酶有0.016 μM和4.58 μM的IC50值。该化合物能够上调HSP70,降低HER2和磷酸化AKT的表达,同时能减少GL26细胞中由IFN-γ诱导的PD-L1表达增加。此外,MAO A/HSP90-IN-2能够抑制对Temozolomide敏感或耐药的胶质母细胞瘤(GBM)、结肠癌、白血病和非小细胞肺癌细胞的生长,并可能有助于阻止肿瘤逃避免疫监控。 | |||
T74561 | JBJ-09-063 TFA | ||
JBJ-09-063 TFA 是一种突变选择性变构EGFR 抑制剂,对EGFRL858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的IC50分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 TFA 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 TFA 对EGFR 酪氨酸激酶抑制剂 (TKI) 敏感和耐药模型均有效。JBJ-09-063 TFA 可用于EGFR 突变型肺癌研究。 | |||
T72237 | JBJ-09-063 hydrochloride | ||
JBJ-09-063 hydrochloride 是一种突变选择性变构EGFR 抑制剂,对EGFRL858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的IC50分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 hydrochloride 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 hydrochloride 对EGFR 酪氨酸激酶抑制剂 (TKI) 敏感和耐药模型均有效。JBJ-09-063 hydrochloride 可用于EGFR 突变型肺癌研究。 | |||
T41240 |
Verrucarin A
|
||
Verrucarin A (Muconomycin A) 是一种 D 型大环真菌毒素。Verrucarin A 是一种蛋白质合成 (protein synthesis) 的抑制剂,来源于Myrothecium verrucaria,可抑制白血病细胞系生长,并激活巨噬细胞 caspases、凋亡和炎症信号。Verrucarin A 能有效提高 p38 MAPK 的磷酸化,降低 ERK/Akt 的磷酸化。Verrucarin A 通过 p21 和 p53 的诱导引起细胞周期调控的解除。 | |||
T63939 |
JBJ-09-063
|
||
JBJ-09-063 是一种突变选择性变构 EGFR 抑制剂,对 EGFRL858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的 IC50分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 对EGFR 酪氨酸激酶抑制剂 (TKI) 敏感与耐药模型均有效。JBJ-09-063 可用于EGFR 突变型肺癌研究。 | |||
T83877 |
2-(cyclohexylmethyl)-Plumbagin
|
||
2-(cyclohexylmethyl)-Plumbagin是naphthoquinone plumbagin的衍生物。在模拟胰腺癌肿瘤微环境的营养匮乏条件下,与营养丰富条件下的PANC-1细胞相比,对PANC-1人类胰腺癌细胞表现出选择性的细胞毒性,50%优选细胞毒性值(PC50s)分别为0.11和47.2 µM。1 µM浓度下,还可诱导PANC-1细胞发生凋亡。此外,2-(cyclohexylmethyl)-Plumbagin在营养匮乏条件下,而非营养丰富条件下,选择性降低PANC-1细胞中Akt和哺乳动物雷帕霉素靶蛋白(mTOR)的磷酸化。在以每周五次、每次50和250 µg/动物剂量给药的MiaPaCa-2胰腺癌小鼠异种移植模型中,能减少肿瘤体积和重量。 | |||
T79560 |
22-(4′-py)-JA
22-(4′-Pyridinecarbonyl) jorunnamycin A |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
22-(4′-py)-JA是久那霉素A的半合成衍生物,源自泰国蓝海绵(Xestospongia sp.)。该化合物显示出抗转移活性,能抑制AKT/mTOR/p70S6K信号通路,并阻断人脐静脉内皮细胞(HUVEC)中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶(MMP-2和MMP-9)、缺氧诱导因子1α(HIF-1α)和血管内皮生长因子(VEGF)来发挥作用。此外,22-(4′-py)-JA对非小细胞肺癌(NSCLC)显示出显著的抗癌效果。 | |||
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。 | |||
T35806 |
N-Stearoylsphingosine
C(18:0)/C(18:1),Cer(d18:1/18:0),C18 Ceramide (d18:1/18:0),C18 Ceramide |
Phosphatase | Metabolism |
N-Stearoylsphingosine (Cer(d18:1/18:0)) 是一种广泛存在真核生物体内的酰胺类化合物,通过干扰PP2A与PP2A抑制剂2的结合来增强蛋白质磷酸酶2A(PP2A)活性,导致Akt去磷酸化。N-Stearoylsphingosine 可用于研究前列腺癌。 | |||
T28157 |
Nephrin
|
||
Nephrin is a cell surface signaling receptor protein that regulates podocyte function and plays a role in β-cell survival signaling; it is a protein necessary for the proper functioning of the renal filtration barrier. Nephrin belongs to a family of highl | |||
T79311 |
CNBCA
|
||
CNBCA是一种有效的SHP2酶抑制剂,具有选择性和竞争性,IC50值为0.87 μM。该化合物可结合SHP2全长蛋白并抑制其酶活性,进而阻止Akt和ERK1/2的磷酸化,以及抑制BT474和MDA-MB468乳腺癌细胞的生长。CNBCA主要用于乳腺癌的研究。 | |||
T36991 |
Monascuspiloin
|
||
Monascuspiloin is a fungal metabolite that has been found inM. pilosusM93-fermented rice.1It induces endoplasmic reticulum stress and autophagy in PC3 prostate cancer cells. Monascuspiloin (15-45 μM) decreases viability of PC3 cells and has an additive effect on the reduction in viability of PC3 cells induced by irradiation when used at a concentration of 25 μM. It induces intratumor apoptosis and autophagy and reduces tumor growth in a PC3 mouse xenograft model when administered at doses of 40 ... | |||
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... | |||
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... | |||
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 ... | |||
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... |
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。 | |||
T5S2178 |
Fargesin
辛夷脂素,(+/-)-Fargesin |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Fargesin ((+/-)-Fargesin) 是一种活性新木脂素,从木兰植物中分离得到,具有抗高血压和抗炎活性。 | |||
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。 | |||
T5S0055 |
Chelidonine
Helidonine,Khelidonin,白屈菜碱,Stylophorin |
Apoptosis; Others; Influenza Virus | Apoptosis; Microbiology/Virology; Others |
Chelidonine (Stylophorin) 是白屈菜中的一种异喹啉生物碱,有抗肿瘤和抗病毒作用。它可导致细胞周期 G2/M 停滞,诱导 caspase 依赖和非依赖性的细胞凋亡。 | |||
TN6694 |
5,6-Benzoflavone
β-Naphthoflavone,beta-NF |
Antioxidant | oxidation-reduction |
5,6-Benzoflavone (β-Naphthoflavone) 是芳烃受体的外源配体,可破坏人肝癌 HepG2 细胞中的锌稳态。5,6-Benzoflavone (β-Naphthoflavone) 具有抗炎和抗氧化活性,抑制通过 AKT/Nrf-2/HO-1-NF-kappaB 信号转导轴,抑制 LPS 诱导的炎症,抑制TNF-α诱导的ICAM-1和VCAM-1表达,可用于研究神经退行性疾病。 | |||
T4S1419 |
(±)-Praeruptorin A
Praeruptorin A,(±)-白花前胡甲素,白花前胡甲素,(-)-Praeruptorin A |
p38 MAPK; Calcium Channel; Akt | Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling |
(±)-Praeruptorin A 是来自白花前胡的干燥根中的一种主要成分,用于研究伴有厚痰和呼吸困难的咳嗽,非天生性咳嗽和上呼吸道感染。它是顺式-内酯 (CKL) 的二酯化产物,可作为 Ca2+-反流阻滞剂,用于高血压的研究。 | |||
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。 | |||
T6S0659 |
Rhynchophylline
钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin |
Calcium Channel; NF-κB | Membrane transporter/Ion channel; Metabolism; NF-κB |
Rhynchophylline (Mitrinermine) 是一种生物碱类化合物,从钩藤中分离得到,具有很高的生物活性,被广泛用于抗炎、神经保护等方面的研究。 | |||
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。 | |||
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。 | |||
T4S21320 |
ISOGINKGETIN
异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮 |
MMP; Others | Others; Proteases/Proteasome |
ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂,也是一种Pre-mRNA Splicing 抑制剂。 | |||
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。 | |||
T6S0525 |
Farrerol
|
ERK; p38 MAPK; Akt | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
Farrerol 是一种杜鹃花的生物活性成分,具有抗氧化、抗肿瘤、抗炎、神经保护和肝保护等多种功能。 | |||
T5S1097 |
Neferine
(R)-1,2-Dimethoxyaporphine,(-)-Neferine,甲基莲心碱 |
Apoptosis; NF-κB; Autophagy | Apoptosis; Autophagy; NF-κB |
Neferine ((-)-Neferine) 是一种双苄基异喹啉类生物碱,可强效抑制NF-κB 激活,具有抗肿瘤活性。 | |||
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。 | |||
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。 | |||
T3S0209 |
Vincristine
|
ERK; p38 MAPK; NF-κB; Akt; JNK; mTOR | Cytoskeletal Signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling |
Vincristine 与微管蛋白结合并抑制微管的形成,从而抑制癌细胞的有丝分裂。 Vincristine 可用作微管去稳定剂,用于研究治疗血液系统癌症,如白血病和淋巴瘤以及儿童肉瘤的相关研究。 | |||
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。 | |||
T3895 |
Polyphyllin I
重楼皂苷I,重楼皂甙 |
Apoptosis; Akt; JNK; PDK; mTOR; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
Polyphyllin I 是从七叶一枝花中提取的生物活性成分,具有很强的抗肿瘤活性。它是 JNK 信号通路的激活剂,也是 PDK1/Akt/mTOR 信号传导的抑制剂。它诱导自噬,G2/M 期阻滞和细胞凋亡。 | |||
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。 | |||
T2940 |
6-Hydroxyflavone
6-羟基黄酮,6-HF |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
6-Hydroxyflavone (6-HF) 是天然存在的黄酮化合物,具有抗炎作用。它对牛血红蛋白糖基化具有抑制作用。它能激活 AKT、ERK 1/2、JNK 信号通路,有效促进成骨细胞分化。它能抑制 LPS 诱导的 NO 的产生。 | |||
T2S2215 |
Crebanine
|
Apoptosis; Others; Akt | Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling |
Crebanine 是来自于韦诺萨千金藤的一种生物碱,通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性,还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。 | |||
TN6419 | Chamaejasmine | ||
Chamaejasmine could be a candidate drug for osteosarcoma and breast cancer chemoprevention, induces apoptosis in MG63 and HEp-2 cells by Akt inactivation and dephosphorylation of BAD. It inhibits Bcl-2 expression and induces Bax expression to desintegrate | |||
TN5100 | Taspine | ERK; EGFR; BCL; VEGFR; MAPK; Akt | Angiogenesis; Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-dependent manner, it has shown meaningful angiogenesis activity. Taspine exhibi | |||
T4S0083 |
Protostemonine
|
Others | Others |
Protostemonine 是一种主要从 Stemona sesslifolia 根中分离得到的生物碱,对哮喘及革兰氏阴性菌所致急性肺损伤有抗炎作用。 | |||
TN4168 | Grifolin | Others | Others |
Grifolin has anti-cancer effects, it induces apoptosis and promotes cell cycle arrest in the A2780 human ovarian cancer cell line via inactivation of the ERK1/2 and Akt pathways; it enhances the differentiation and proliferation of oligodendrocyte precurs | |||
TN4046 | Excisanin A | MMP; FAK; PARP; GSK-3; NF-κB; Wnt/beta-catenin; Akt; Caspase; PI3K; Prostaglandin Receptor; JNK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors |
ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the ... | |||
TN5050 |
Sprengerinin C
|
NADPH-oxidase; VEGFR; p38 MAPK; ROS; Akt; PI3K; mTOR; p53 | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Sprengerinin C exerts anti-tumorigenic effects in hepatocellular carcinoma via inhibition of proliferation and angiogenesis and induction of apoptosis, it can strongly suppress tumor angiogenesis in human umbilical vein endothelial cells, it blocks vascul | |||
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 |