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10

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2706 Palomid 529

P529,SG 00529

Apoptosis; mTOR Apoptosis; PI3K/Akt/mTOR signaling
Palomid 529 (SG 00529) 是一种mTORC1和mTORC2复合体抑制剂,已用于研究治疗年龄相关性黄斑变性的试验。
T0773 Febuxostat

非布索坦,TMX 67,非布司他,TEI 6720

ROS; Xanthine Oxidase Immunology/Inflammation; Metabolism
Febuxostat (TEI 6720) 是一种选择性黄嘌呤氧化酶(XO)抑制剂,Ki=0.6 nM。
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。
T28285 P-2281

P 2281,P2281

mTOR PI3K/Akt/mTOR signaling
P-2281 是一种 mTOR 抑制剂,具有抗癌和抗炎功效。P-2281 通过抑制 T 细胞功能来抑制葡聚糖硫酸钠 (DSS) 诱导的结肠炎,并且在人类结肠炎的小鼠模型中有效。
T36083 DS-7423

PI3K; mTOR PI3K/Akt/mTOR signaling
DS-7423 是PI3K 和mTOR 的有效抑制剂,抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。
T39776 RMC-4529

RMC-4529 is a chemical compound that demonstrates potent inhibition, with an IC50 value of 1.0 nM, against p-4E-BP1-(T37/46) in mTOR kinase cellular assays.
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.
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.

化合物

Palomid 529
Cat.No: T2706
Synonym: P529,SG 00529
Target: Apoptosis, mTOR
Febuxostat
Cat.No: T0773
Synonym: 非布索坦,TMX 67,非布司他,TEI 6720
Target: ROS, Xanthine Oxidase
WAY-600
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
WYE-354
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
WYE-687
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
P-2281
Cat.No: T28285
Synonym: P 2281,P2281
Target: mTOR
DS-7423
Cat.No: T36083
Synonym:
Target: PI3K, mTOR
RMC-4529
Cat.No: T39776
Synonym:
Target:
PABA/NO
Cat.No: T68464
Synonym:
Target:
(32-Carbonyl)-RMC-5552
Cat.No: T39958
Synonym:
Target:
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。

天然产物

Phellamurin
Cat.No: TN4761
Synonym:
Target: P-gp
Acacetin
Cat.No: T3981
Synonym: 4'-Methoxyapigenin,金合欢素,5,7-Dihydroxy-4'-methoxyflavone,Linarigenin
Target: Apoptosis, IAP, COX, Autophagy
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