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27

抑制剂 & 化合物

5

天然产物

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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。

化合物

Mito-LND
Cat.No: T9211
Synonym: Mito-Loidamine
Target: OXPHOS, Reactive Oxygen Species, Mitochondrial Metabolism, Autophagy
GSK-25
Cat.No: T4488
Synonym: GSK25
Target: ROCK, S6 Kinase, mTOR
DD1
Cat.No: T8978
Synonym: 3,3'-Diamino-4'-methoxyflavone,HUN85111
Target: Proteasome
S6K1-IN-DG2
Cat.No: T28652
Synonym: S6K1 Inhibitor DG2,S6K1-Inhibitor-DG2,S6K1 IN DG2,S6K1INDG2,S6K1InhibitorDG2
Target: mTOR
GSK299115A
Cat.No: T27471
Synonym: GSK 299115A,GSK-299115A
Target: GRK
M2698
Cat.No: T11928
Synonym: MSC2363318A
Target: Akt, mTOR
LY-2584702 tosylate salt
Cat.No: T1746
Synonym: LY2584702 tosylate
Target: S6 Kinase
AT7867
Cat.No: T6304
Synonym:
Target: Akt, PKA, S6 Kinase
GSK270822A
Cat.No: T27467
Synonym: GSK 270822A,GSK-270822A
Target: GRK
LY-2584702 free base
Cat.No: T6159
Synonym:
Target: S6 Kinase, mTOR
AT13148
Cat.No: T2482
Synonym:
Target: ROCK, SGK, Akt, PKA, S6 Kinase
SB-747651A Dihydrochloride
Cat.No: T9652
Synonym:
Target: ROCK
CCT128930 hydrochloride
Cat.No: T6303L
Synonym: CCT128930 hydrochloride(885499-61-6 Free base)
Target: Apoptosis, Akt, PKA, mTOR, Autophagy
AT-533
Cat.No: T67836
Synonym:
Target: HSP, HSV
AMPK activator 2 hydrochloride( 2410961-69-0 Free base)
Cat.No: T60675L
Synonym: AMPK activator 2 hydrochloride( 2410961-69-0 Free base)
Target: AMPK
LY-2584702 hydrochloride
Cat.No: T11900
Synonym:
Target: S6 Kinase
XL-418
Cat.No: T68477
Synonym:
Target:
SB-747651A
Cat.No: T28695
Synonym: SB 747651A
Target:
Akt/SKG Substrate Peptide TFA
Cat.No: T75719
Synonym:
Target:
AT7867 dihydrochloride
Cat.No: T21624
Synonym:
Target:
(32-Carbonyl)-RMC-5552
Cat.No: T39958
Synonym:
Target:
AMPK activator 2
Cat.No: T60675
Synonym:
Target: AMPK
AKT-IN-3
Cat.No: T10275
Synonym:
Target: Akt
22-(4′-py)-JA
Cat.No: T79560
Synonym: 22-(4′-Pyridinecarbonyl) jorunnamycin A
Target: Akt
Dactolisib
Cat.No: T2235
Synonym: 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
Target: ATM/ATR, PI3K, mTOR, Autophagy
CCT128930
Cat.No: T6303
Synonym:
Target: Akt, PKA, S6 Kinase, Autophagy
Hu7691 free base
Cat.No: T39733
Synonym:
Target: Akt
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...

天然产物

Acacetin
Cat.No: T3981
Synonym: 4'-Methoxyapigenin,金合欢素,5,7-Dihydroxy-4'-methoxyflavone,Linarigenin
Target: Apoptosis, IAP, COX, Autophagy
3'-Hydroxypterostilbene
Cat.No: T2S2382
Synonym: 3’-羟基紫檀茋,3'-羟基紫檀茋,3'-HPT
Target: Apoptosis, Autophagy
Chrysophanol
Cat.No: T2995
Synonym: 大黄酚,3-Methylchrysazin,Chrysophanic Acid,Turkey Rhubarb
Target: EGFR
Caffeic Acid Phenethyl Ester
Cat.No: T6429
Synonym: Phenylethyl Caffeate,咖啡酸苯乙酯,CAPE
Target: Apoptosis, NF-κB
L-Sepiapterin
Cat.No: T38250
Synonym:
Target:
TargetMol Loading
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