PI3K/Akt/mTOR Signaling(PI3K/Akt/mTOR 信号传导)

Cat.No. 产品名称 Information

GC46531 2-Amino-5-bromo-6-chloropyrazine

2-氨基-5-溴-6-氯吡嗪

A heterocyclic building block

GC61382 Xanthoangelol

黄色当归醇

Xanthoangelol, a chalcone found in the roots of Angelica keiskei, is a nonselective monoamine oxidase (MAO) inhibitor and a potent dopamine β-hydroxylase (DBH) inhibitor. It has anti-inflammatory, antibiotic and pro-apoptotic activities.

GC61336 TMBIM6 antagonist-1

1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮

TMBIM6antagonist-1是一个有潜力的TMBIM6拮抗剂，抑制TMBIM6与mTORC2结合，降低mTORC2活性，调节TMBIM6释放Ca2+。

GC61227 Quercetin D5

槲皮素 d5

QuercetinD5是Quercetin的一种氘代化合物。Quercetin是一种天然黄酮类化合物，可激活或抑制许多蛋白质的活性。Quercetin可激活SIRT1，也可抑制PI3K，抑制PI3Kγ，PI3Kδ，PI3Kβ的IC50分别为2.4μM,3.0μM,5.4μM。

GC61045 Metformin D6 hydrochloride

二甲双胍盐酸,1,1-Dimethylbiguanide-d6 hydrochloride

An internal standard for the quantification of metformin

GC61029 Marein

马里甙

A glucoside chalcone with diverse biological activities

GC60970 KY19382

A3051

KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively.

GC60782 Disitertide TFA

P144 TFA

Disitertide(P144)TFA是转化生长因子TGFβ1的多肽抑制剂，特异性的阻断其与受体间的相互作用。Disitertide(P144)TFA也是PI3K的抑制剂和凋亡(apoptosis)诱导剂。

GC60339 SKI V

2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮

SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.

GC60262 N-Feruloyloctopamine

N-阿魏酰章鱼胺

N-Feruloyloctopamine，从 Garlic 皮中分离出来的，是一种抗氧化剂成分。N-Feruloyloctopamine 显着降低 Akt 和 p38 MAPK 磷酸化水平。

GC60258 MT 63-78 MT 63-78 是一种有效的直接 AMPK 激活剂，EC50 为 25 μM。M 63-78 还诱导细胞有丝分裂阻滞和细胞凋亡 (apoptosis)。MT 63-78 通过抑制脂肪生成和 mTORC1 途径来阻止前列腺癌的生长。MT 63-78 具有抗肿瘤作用。

GC60245 Metformin

二甲双胍; 1,1-Dimethylbiguanide

二甲双胍（1,1-二甲基双胍）主要介导 AMPK 的激活，AMPK 是一种参与调节细胞能量代谢的丝氨酸/苏氨酸蛋白激酶，可导致癌细胞中 mTOR 信号传导和蛋白质合成的减少。

GC39715 M2698

MSC2363318A

A dual inhibitor of p70S6K and Akt1

GC39377 EB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.

GC50332 TC KHNS 11 强效选择性 PI 3-激酶 δ；抑制剂；口服生物利用度

GC50276 LTURM 36 PI 3-kinase δ inhibitor

GC50072 ETP 45658 ETP 45658 是一种有效的 PI3K 抑制剂，对 PI3Kα、PI3Kδ、PI3Kβ 和 PI3Kγ 的 IC50 分别为 22.0 nM、39.8 nM、129.0 nM 和 717.3 nM。 ETP 45658 还可以抑制 DNA-PK (IC50\u003d70.6 nM) 和 mTOR (IC50\u003d152.0 nM)。 ETP 45658 可用于癌症研究。

GC50009 LY 294002 hydrochloride Prototypical PI 3-kinase inhibitor; also inhibits other kinases

GC39292 Rheb inhibitor NR1 Rheb inhibitor NR1 是一种 Rheb 抑制剂，在 Rheb-IVK分析中，IC50 为 2.1 μM。Rheb inhibitor NR1 是一种选择性的 mTORC1 抑制剂。Rheb inhibitor NR1 抑制 S6K1 在 T389 位点磷酸化，并增加 AKT 在 S473 位点磷酸化。

GC39266 Hematein

氧化苏木精

Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.

GC46123 Comprehensive Kinase Screening Library For screening of a variety of kinase inhibitors

GC39181 BRD0705 BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).

GC39155 PI-273 PI-273, the first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM, can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.

GC39152 9-ING-41

Elraglusib

A GSK3β inhibitor

GC38892 BIP-135 BIP-135 是一个高效、选择性的，ATP 竞争性的 GSK-3 抑制剂，对 GSK-3α 和 GSK-3β 作用的IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。

GC38815 Methyl cinnamate

肉桂酸甲酯; Methyl 3-phenylpropenoate

Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes.

GC38787 GNF4877 GNF4877是 DYRK1A 和 GSK3β 的有效抑制剂，IC50 值分别为 6 nM 和 16 nM，可导致 NFATc 核输出受阻并增加 β 细胞增殖 (对小鼠 β (R7T1) 细胞的 EC50 值为 0.66 μM)。

GC38694 Erucic acid

芥酸

A 22-carbon monounsaturated fatty acid

GC38679 Urolithin B

尿石素B

A metabolite of ellagic acid

GC38609 Rotundic acid

铁冬青酸

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.

GC38606 Glaucocalyxin A

蓝萼甲素

Glaucocalyxin A is a biologically active ent-kauranoid diterpenoid isolated from Rabdosia japonica var. glaucocalyx with antitumor and anti-inflammatory activity. Glaucocalyxin A induces G2/M cell cycle arrest and apoptosis through the PI3K/Akt pathway in human bladder cancer cells.

GC38567 Nepodin

羊蹄素,Musizin

A naphthol with diverse biological activities

GC38482 Desmethylglycitein

4',6,7-三羟基异黄酮; 4',6,7-Trihydroxyisoflavone

An active metabolite of daidzein

GC38473 WYE-687 dihydrochloride

WYE-687二盐酸盐

An mTOR inhibitor

GC38422 Euphorbiasteroid

千金子甾醇

A tricyclic diterpene

GC38419 Cyclovirobuxine D

黄杨碱

An alkaloid with diverse biological activities

GC38401 rac-AZD 6482

2-[[1-[7-甲基-2-(吗啉-4-基)-4-氧代-4H-吡啶并[1,2-A]嘧啶-9-基]乙基]氨基]苯甲酸,(Rac)-KIN-193

rac-AZD 6482 (rac-KIN-193) 是 AZD 6482 的低活性外消旋体，AZD 6482 是一种有效的选择性 p110β 抑制剂，IC50 为 0.69 nM。

GC38392 Euscaphic acid

野鸦椿酸

A triterpene with diverse biological activities

GC38330 EHT 5372 EHT 5372 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，其 IC50 值分别为 0.22，0.28 nM。

GC38236 Esculetin

秦皮乙素

A coumarin with diverse actions

GC38209 Kahweol

咖啡豆醇

A natural diterpene with anti-inflammatory and antiangiogenic properties

GC38170 Phellodendrine

黄柏碱

An alkaloid with diverse biological activities

GC38168 Heterophyllin B

太子参环肽B

Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla, which provides a novel strategy for the treatment of esophageal cancer.

GC38101 Demethyleneberberine

去亚甲基小檗碱

去亚甲基小檗碱(DMB)作为药用植物黄柏的天然活性成分，具有良好的生物活性。

GC38088 Hederacolchiside A1

革叶常春藤皂苷 A1

Hederacolchiside A1 是从白头翁中分离的，通过调节 PI3K/Akt/mTOR 信号通路诱导凋亡，从而抑制肿瘤细胞的增殖。Hederacolchiside A1 具有抗血吸虫病活性，影响体内和体外的寄生虫生存力。

GC38033 KDU731 KDU731，具有口服活性的 C. parvum PI4K 抑制剂，阻断体内外隐孢子虫感染，IC50 值为 25 nM。KDU731 是治疗隐孢子虫引起的腹泻的有望候选药物，具有广泛的安全性。

GC37970 ZLN024

2-[[2-(2-溴-4-甲基苯氧基)乙基]硫基]嘧啶

An allosteric activator of AMPK

GC37955 YS-49 monohydrate An inhibitor of platelet aggregation

GC37954 YS-49

1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐

An inhibitor of platelet aggregation

GC37924 VP3.15 dihydrobromide VP3.15 dihydrobromide 是高效、口服生物可利用的，CNS 可渗透的 PDE7-GSK3 双重抑制剂，对PDE7 和GSK3 作用的 IC50 值分别为 1.59 μM 和 0.88 μM。VP3.15 dihydrobromide 具有神经保护和神经修复活性，是多发性硬化症 (MS) 潜在的抗炎和促髓鞘再生联合治疗药物。