Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12465 | PI3Kγ inhibitor 2 | PI3K | PI3K/Akt/mTOR signaling |
PI3Kγ inhibitor 2 is an orally bioavailable inhibitor of PI3Kγ(Ki of 4 nM). | |||
T12459 |
PI3K/mTOR Inhibitor-2
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
PI3K/mTOR Inhibitor-2 是一种有效的 PI3K 和 mTOR 泛抑制剂,对 PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ 和 mTOR 的 IC50 分别为 3.4、34、16,1 和 4.7 nM。 PI3K/mTOR Inhibitor-2 具有抗肿瘤活性。 | |||
T3656 |
PKI-402
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
PKI-402 是一种有效的 PI3K 和 mTOR 抑制剂,对 PI3Kα, mTOR, PI3Kβ, PI3Kδ 和 PI3Kγ 抑制的IC50 分别为 2, 3, 7, 14 和 16 nM。 | |||
T1916 |
Apitolisib
RG 7422,GNE 390,GDC-0980 |
Apoptosis; PI3K; mTOR | Apoptosis; PI3K/Akt/mTOR signaling |
Apitolisib (RG 7422) 是一种口服有效的 PI3K 和 mTOR(TORC1/2) 激酶抑制剂,抑制 PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ的活性,IC50值为 5 nM/27 nM/7 nM/14 nM,抑制 mTOR,Ki 为 17 nM。它用于乳腺癌、前列腺癌、肾细胞癌和子宫内膜癌等实体癌的试验研究 。 | |||
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。 | |||
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。 | |||
T2265 |
Bimiralisib
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2 |
Others; PI3K; S6 Kinase; mTOR | MAPK; Others; PI3K/Akt/mTOR signaling |
Bimiralisib (PI3K-IN-2) 是一种有效的,可渗透脑的 mTOR/PI3K 抑制剂,是一种 mTORC1和 mTORC2抑制剂。它能够抑制 PI3Kα,PI3Kδ,PI3Kβ,PI3Kγ和 mTOR,IC50分别为 33 nM,451 nM,661 nM,708 nM 和 89 nM。 | |||
T6883 |
Samotolisib
GTPL8918,LY3023414 |
DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Samotolisib (LY3023414) 在低纳摩尔浓度下,有效抑制mTORC1/2。它选择性地有效抑制PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ、DNA-PK 和mTOR,IC50分别为 6.07 nM、77.6 nM、38 nM、23.8 nM、4.24 nM 和 165 nM。它可用于多种肿瘤和癌症的试验。 | |||
T36315 |
NVS-PI3-4
NVS-PI3-4 |
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NVS-PI3-4 is a highly selective inhibitor of the enzyme PI3Kγ. It is specifically designed for use in scientific investigations related to allergies, inflammatory conditions, and cancerous diseases[1][2]. | |||
T79111 | PI3Kγ inhibitor 7 | PI3K | PI3K/Akt/mTOR signaling |
PI3Kγ inhibitor7(compound 2)作为一种有效的PI3Kγ抑制剂,拥有口服活性,并对PI3Kα、PI3Kβ、PI3Kγ、PI3Kδ的抑制作用,其IC50值分别为4768 nM、878.1 nM、3.42 nM、355.2 nM。此外,PI3Kγ inhibitor7还展现出了抗肿瘤活性。 | |||
T63221 |
PI3Kδ/γ-IN-2
|
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PI3Kδ/γ-IN-2 是有效的、口服生物利用度高的 PI3Kδ (IC50: 1 nM) 和 PI3Kγ (IC50: 4.3 nM) 双重抑制剂,具有潜力用于抗 B 细胞恶性肿瘤的研究。 | |||
T62912 |
PI3K/HDAC-IN-2
|
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PI3K/HDAC-IN-2 是一种有效的 PI3K/HDAC 双重抑制剂,能够作用于 PI3Kα (IC50: 226 nM)、PI3Kβ (IC50: 279 nM)、PI3Kγ (IC50: 467 nM)、PI3Kδ (IC50: 29 nM)、HDAC1 (IC50: 1.3 nM)、HDAC2 (IC50: 3.4 nM)、HDC4 (IC50: 973 nM)、HDAC6 (IC50: 17 nM)、HDAC8 (IC50: 12 nM)。PI3K/HDAC-IN-2 具有 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性,并表现出显着的抗癌作用。 | |||
T35525 |
PI3-Kinase α Inhibitor 2
PI3-Kinase α Inhibitor 2 |
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Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It... | |||
T35488 |
(S)-PI3Kα-IN-4
(S)-PI3Kα-IN-4 |
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(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitor... |