27
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9211 |
Mito-LND
Mito-Loidamine |
OXPHOS; Reactive Oxygen Species; Mitochondrial Metabolism; Autophagy | Apoptosis; Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Mito-LND (Mito-Loidamine) 是一种有口服活性和靶向线粒体的氧化磷酸化抑制剂。它抑制线粒体生物能,刺激活性氧的形成,并诱导肺癌细胞自噬细胞死亡。 | |||
T4488 |
GSK-25
GSK25 |
ROCK; S6 Kinase; mTOR | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
GSK-25 是一种选择性的,具有口服活性的 ROCK1抑制剂。它对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性,RSK1的 IC50 为 398 nM,p70S6K 的 IC50 为 1000nM。它可抑制 P450,对 CYP2C9、CYP2D6和 CYP3A4的 IC50分别为2.5、5.2和2.5 μM。 | |||
T8978 |
DD1
3,3'-Diamino-4'-methoxyflavone,HUN85111 |
Proteasome | Proteases/Proteasome; Ubiquitination |
DD1 (HUN85111) 是一种蛋白酶体抑制剂,可诱导人髓系肿瘤选择性凋亡。 | |||
T28652 |
S6K1-IN-DG2
S6K1 Inhibitor DG2,S6K1-Inhibitor-DG2,S6K1 IN DG2,S6K1INDG2,S6K1InhibitorDG2 |
mTOR | PI3K/Akt/mTOR signaling |
S6K1-IN-DG2(S6K1InhibitorDG2) 是一种有效的 p70S6K 抑制剂 ,IC50 值小于 100 nM。 | |||
T27471 |
GSK299115A
GSK 299115A,GSK-299115A |
GRK | GPCR/G Protein |
GSK299115A (GSK-299115A) 是一种选择性的ROCK1抑制剂。GSK299115A 抑制ROCK1、RSK1和p70S6K 的IC50分别为8nM、620nM 和560nM。 | |||
T11928 |
M2698
MSC2363318A |
Akt; mTOR | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
M2698 (MSC2363318A) 是 p70S6K、Akt1 和 Akt3 的抑制剂,IC50 为 1 nM。 M2698 显示出抗癌活性。 | |||
T1746 |
LY-2584702 tosylate salt
LY2584702 tosylate |
S6 Kinase | MAPK; PI3K/Akt/mTOR signaling |
LY-2584702 tosylate salt 是一种选择性的 ATP 竞争性 p70S6K 抑制剂,IC50为 4 nM,对S6K1的IC50为 2 nM,用于研究癌症治疗的试验。 | |||
T6304 |
AT7867
|
Akt; PKA; S6 Kinase | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
AT7867 是 ATP 竞争性的Akt1/Akt2/Akt3和p70S6K/PKA 抑制剂,IC50分别为 32、17、47 和 85、20 nM。 | |||
T27467 |
GSK270822A
GSK 270822A,GSK-270822A |
GRK | GPCR/G Protein |
GSK270822A 是一种选择性的 ROCK1抑制剂。GSK270822A 抑制 ROCK1,RSK1,p70S6K 的 IC50 分别为9nM,1100nM,1550nM。 | |||
T6159 |
LY-2584702 free base
|
S6 Kinase; mTOR | MAPK; PI3K/Akt/mTOR signaling |
LY-2584702 free base 是一种选择性的 ATP 竞争性 p70S6K 抑制剂,IC50为 4 nM,对S6K1的IC50为 2 nM,用于研究癌症治疗的试验。 | |||
T2482 |
AT13148
|
ROCK; SGK; Akt; PKA; S6 Kinase | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
AT13148 是一种 ATP 竞争性 AGC 激酶口服抑制剂,能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性,IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。 | |||
T9652 |
SB-747651A Dihydrochloride
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SB-747651A dihydrochloride是一种与ATP竞争性相互作用的抑制剂,特别针对丝裂原和应激激活激酶1 (MSK1),IC50值为11 nM。此化合物还能抑制PRK2、RSK1、p70S6K和ROCK-II等酶的活性。因其对上述激酶的抑制作用,SB-747651A dihydrochloride在炎症研究中显示出潜力。 | |||
T6303L |
CCT128930 hydrochloride
CCT128930 hydrochloride(885499-61-6 Free base) |
Apoptosis; Akt; PKA; mTOR; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
CCT128930 hydrochloride (CCT128930 hydrochloride) 是一种选择性 AKT 抑制剂,具有抗肿瘤活性。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性。 | |||
T67836 |
AT-533
|
HSP; HSV | Cytoskeletal Signaling; Metabolism; Microbiology/Virology |
AT-533 是有效的 HSV 和 Hsp90 抑制剂。AT-533 可以阻断 HIF-1α/VEGF/VEGFR-2 信号通路,从而抑制血管生成和肿瘤生长。AT-533 也抑制下游通路的激活,包括 Erk1/2, FAK, Akt/mTOR/p70S6K。AT-533 抑制人脐静脉内皮细胞 (HUVEC) 的细胞迁移、侵袭和管形成。 | |||
T60675L |
AMPK activator 2 hydrochloride( 2410961-69-0 Free base)
AMPK activator 2 hydrochloride( 2410961-69-0 Free base) |
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
AMPK activator 2 hydrochloride 是一种含氟氯胍衍生物,可上调 AMPK 信号通路并下调 mTOR/4EBP1/p70S6K。AMPK activator 2 hydrochloride 抑制人类癌细胞系 (UMUC3、T24、A549) 的增殖和迁移。 | |||
T11900 |
LY-2584702 hydrochloride
|
S6 Kinase | MAPK; PI3K/Akt/mTOR signaling |
Ly-2584702 hydrochloride is a p70S6K selective ATP competitive inhibitor with IC50 of 4 nM.In the S6K1 enzyme assay, the IC50 of LY-2584702 was 2 nM. | |||
T68477 | XL-418 | ||
XL-418 is a selective, orally active small molecule, targeting protein kinase B (PKB or AKT) and ribosomal protein S6 Kinase (p70S6K), with potential antineoplastic activity. XL418 inhibits the activities of PKB and p70S6K, both acting downstream of phosphoinosotide-3 kinase (PI3K). These kinases are often upregulated in a variety of cancers. Inhibition of PKB by this agent will induce apoptosis, while inhibition of p70S6K will result in the inhibition of translation within tumor cells. | |||
T28695 |
SB-747651A
SB 747651A |
||
SB-747651A is a potent, ATP-competitive inhibitor of mitogen- and stress-activated kinase 1 (MSK1, IC50 = 11 nM). It targets the N-terminal kinase domain. SB-747651A inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells. | |||
T75719 |
Akt/SKG Substrate Peptide TFA
|
||
Akt/SKG Substrate Peptide TFA 是一种合成的 Akt/PKB 底物肽,不会被 p70S6K 或 MAPK1 磷酸化。 | |||
T21624 | AT7867 dihydrochloride | ||
AT7867 dihydrochloride 是一种有效的ATP 竞争性的Akt1/Akt2/Akt3和p70S6K/PKA 抑制剂,IC50值分别为 32 nM/17 nM/47 nM 和 85 nM/20 nM,具有癌症治疗的潜力。 | |||
T39958 | (32-Carbonyl)-RMC-5552 | ||
(32-Carbonyl)-RMC-5552 is a highly effective mTOR inhibitor, exhibiting inhibitory effects on both mTORC1 and mTORC2 substrate phosphorylation. Specifically, it significantly suppresses the phosphorylation of p-P70S6K-(T389), p-4E-BP1-(T37/36), and p-AKT1/2/3-(S473) with pIC50 values > 9, >9 and 8~9, respectively. | |||
T60675 |
AMPK activator 2
|
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
AMPK activator 2 是一种含氟氯胍衍生物,具有潜在的抗癌活性,可上调 AMPK 信号通路并下调 mTOR/4EBP1/p70S6K,对人类癌细胞系 (UMUC3、T24、A549) 的增殖和迁移有抑制作用。 | |||
T10275 |
AKT-IN-3
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1 | |||
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。 | |||
T2235 |
Dactolisib
2-甲基-2-[4-[3-甲基-2-氧代-8-(喹啉-3-基)-2,3-二氢咪唑并[4,5-c]喹啉-1-基]苯基]丙腈,BEZ235,NVP-BEZ235 |
ATM/ATR; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Dactolisib (BEZ235) 是一种可口服的 pan-class IPI3K 和 mTOR 抑制剂,抑制 mTORC1和 mTORC2,作用于 p110α/γ/δ/β和 mTOR,IC50分别为 4 nM/5 nM/7 nM/75 nM 和 20.7 nM。 | |||
T6303 |
CCT128930
|
Akt; PKA; S6 Kinase; Autophagy | Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
CCT128930 是一种 ATP 竞争性,选择性 AKT 抑制剂。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性,具有抗肿瘤活性。 | |||
T39733 |
Hu7691 free base
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Hu7691 free base 是一种具有口服活性、高效性和选择性的 Akt 抑制剂,对多种神经母细胞瘤细胞系的抗增殖和神经发生作用。Hu7691 free base 抑制 Akt1、Akt2 和 Akt3 ,诱导神经母细胞瘤细胞分化。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T2S2382 |
3'-Hydroxypterostilbene
3’-羟基紫檀茋,3'-羟基紫檀茋,3'-HPT |
Apoptosis; Autophagy | Apoptosis; Autophagy |
3'-Hydroxypterostilbene (3'-HPT) 是天然紫檀芪类似物,通过诱导细胞凋亡和自噬,有效抑制人结肠癌细胞的生长。它抑制 PI3K/Akt/mTOR/p70S6K 和 p38MAPK 途径并激活 ERK1/2,JNK1/2 MAPK 途径。 | |||
T2995 |
Chrysophanol
大黄酚,3-Methylchrysazin,Chrysophanic Acid,Turkey Rhubarb |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Chrysophanol (Turkey Rhubarb) 是掌叶大黄中的一种蒽醌类天然产物,可抑制EGF-诱导的EGFR 磷酸化,且抑制AKT 和mTOR/p70S6K 激活。 | |||
T6429 |
Caffeic Acid Phenethyl Ester
Phenylethyl Caffeate,咖啡酸苯乙酯,CAPE |
Apoptosis; NF-κB | Apoptosis; NF-κB |
Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) 是咖啡酸的苯乙醇酯,是蜂巢蜂胶的生物活性成分。它抑制核转录因子 NF-kappa B 的激活,具有抗肿瘤、细胞保护和免疫调节活性。它抑制 PDGF 诱导的血管平滑肌细胞增殖。 | |||
T38250 | L-Sepiapterin | ||
L-Sepiapterin, also known as Sepiapterin, is a precursor compound crucial for the production of tetrahydrobiopterin (BH4), which serves as a coenzyme for endothelial nitric oxide synthase (eNOS). This compound demonstrates its efficacy by improving endothelial dysfunction in small mesenteric arteries from db/db mice and promoting angiogenesis. Moreover, L-Sepiapterin exerts inhibitory effects on cellular proliferation and migration in ovarian cancer cells through the down-regulation of p70S6K-de... |