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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12124 |
mTOR inhibitor-2
|
mTOR | PI3K/Akt/mTOR signaling |
mTOR inhibitor-2 is an inhibitor of selective and oral mTOR (IC50 of 7 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。 | |||
T6100 |
Torin 2
|
Apoptosis; ATM/ATR; DNA-PK; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Torin 2 是一种特异性 mTOR 抑制剂,IC50值为0.25 nM,并改善了药代动力学特性。它抑制 ATM/ATR/DNA-PK 的 EC50 分别为 28 nM/35 nM/118 nM。 | |||
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。 | |||
T9310 |
mTOR inhibitor 13
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
mTOR inhibitor 13是一种选择性的mTOR 抑制剂,对mTOR 和PI3Kα的IC50分别为0.29nM 和119nM。 | |||
T8649 |
TMBIM6 antagonist-1
BAX-inhibitor-1,1-(2-氨基苯基)-3-(3-硝基苯基)-2-丙烯-1-酮,BIA |
mTOR | PI3K/Akt/mTOR signaling |
TMBIM6 antagonist-1 (BAX-inhibitor-1) 是有潜力的TMBIM6拮抗剂,能够抑制 TMBIM6 与 mTORC2 结合,抑制 mTORC2 活性,调节TMBIM6 释放 Ca2+。 | |||
T8055 |
TFEB activator 1
(1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1,,Curcumin analog compound C1,Curcumin analog C1,(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮,RPN77612 |
Others; Autophagy | Autophagy; Others |
TFEB activator 1 (Curcumin analog compound C1) 是转录因子 EB 的一种激活剂,有望预防或治疗阿尔茨海默病。 | |||
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。 | |||
T6820 |
D-α-Hydroxyglutaric acid disodium
D-alpha-Hydroxyglutaric acid disodium salt,(R)-2-羟基戊二酸二钠盐,Disodium (R)-2-Hydroxyglutarate |
ATPase; Others; Reactive Oxygen Species; Endogenous Metabolite; mTOR | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB; Others; PI3K/Akt/mTOR signaling |
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) 是神经代谢疾病 D-2-羟基戊二酸尿症中积累的主要代谢产物,可增加活性氧的产生。它是 α-酮戊二酸 (α-KG) 的弱竞争拮抗剂,可抑制多种α-KG 依赖性双加氧酶,Ki 为 10.87 mM。 | |||
T9309 |
mTOR inhibitor 11
|
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mTOR inhibitor 11 是一种有用的有机化合物,可用于生命科学领域的相关研究。其产品编号为 T9309,CAS号为 1195785-35-3。 | |||
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。 | |||
T16355 |
NSC781406
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
NSC781406是一种高效PI3K 和mTOR 抑制剂,其PI3Kα的IC50值为2 nM。 | |||
T9315 |
2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]-
|
Others | Others |
2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]- 是有效的mTOR 抑制剂,对于mTOR 和PI3Kα的IC50分别为0.176 μM 和 >30 μM。 | |||
T6045 |
Torin 1
|
DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Torin 1 是一种有效的 mTOR 抑制剂,IC50为 3 nM。它抑制 mTORC1/2复合物的 IC50值在 2 和 10 nM 之间,还诱导自噬。 | |||
T1838 |
Sapanisertib
沙帕色替,TAK-228,MLN0128,INK 128 |
PI3K; mTOR; Autophagy | Autophagy; PI3K/Akt/mTOR signaling |
Sapanisertib (INK 128) 是一种口服有效的 ATP 依赖性的mTOR1/2抑制剂,抑制 mTOR 激酶的IC50值为 1 nM,具有潜在抗肿瘤活性。 | |||
T3586 |
Compound 401
2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Compound 401 (2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one) 是一种可靶向 mTOR 的合成 DNA-PK 抑制剂,IC50为0.28 μM。 | |||
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。 | |||
T7014 |
Voxtalisib
XL765,SAR245409 |
DNA-PK; PI3K; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Voxtalisib (XL765) 是一种PI3K 抑制剂,抑制p110α,p110β,p110γ和p110δ。它抑制mTORC1和mTORC2,IC50s 分别为 160 和 910 nM。它也抑制 DNA-PK (其 IC50=150 nM) 和 mTOR (其 IC50=157 nM)。 | |||
T67705 |
mTOR inhibitor 9a
|
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mTOR inhibitor 9a 对人LNCap 细胞的生长具有抑制作用,ic50为80nm。mTOR inhibitor 9a 可能具有抗肿瘤活性。 | |||
T2414 |
Torkinib
PP 242 |
Apoptosis; Mitophagy; PI3K; mTOR; Autophagy | Apoptosis; Autophagy; PI3K/Akt/mTOR signaling |
Torkinib (PP 242) 是一种选择性,ATP 竞争型的mTOR 抑制剂,IC50为 8 nM。它也抑制mTORC1和mTORC2,IC50分别为 30 nM 和 58 nM。 | |||
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。 | |||
T6143 |
PI-103
PI103,PI 103 |
Apoptosis; DNA-PK; PI3K; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI-103 是一种 PI3K 和 mTOR 抑制剂,抑制 p110α、p110β、p110δ、p110γ、mTORC1和 mTORC2,IC50分别为 8 nM、88 nM、48 nM、150 nM、20 nM 和 83 nM。它可诱导自噬,还抑制 DNA-PK,IC50为 2 nM。 | |||
T2415 |
PP121
|
Apoptosis; VEGFR; Bcr-Abl; PDGFR; Src; mTOR; Hck | Angiogenesis; Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
PP121是一种多靶点激酶抑制剂,抑制 PDGFR、Hck、mTOR、VEGFR2、Src、Abl、DNK-PK 的 IC50值分别为2、8、10、12、14、18、60 nM。 | |||
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。 | |||
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。 | |||
T9533 |
BC-LI-0186
4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide |
Others | Others |
BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) 是选择性抑制亮氨酸 tRNA 合成酶与 Ras 相关的 GTP 结合蛋白 D 相互作用(IC50=46.11 nM)。BC-LI-0186能有效抑制肿瘤相关 MTOR 突变体的特性和雷帕霉素耐药癌细胞的生长,能够用于肺癌的相关研究。 | |||
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 。 | |||
T16567 |
PQR530
PQR-530 |
PI3K; mTOR | PI3K/Akt/mTOR signaling |
PQR530 是一具有口服活性,种 ATP 竞争性的,可透过血脑屏障的 PI3K/mTORC1/2双重抑制剂,对于 PI3Kα 和 mTOR (分别为 0.84 和 0.33 nM) 的Kd 为亚摩尔。它具有抗肿瘤作用。 | |||
T30441 |
BI-860585
BI860585 |
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BI-860585 is an inhibitor of Raptor-Mammalian Target of Rapamycin (mTOR) Complex 1 (mTOR Complex 1; mTORC1) and rictor-mTOR Complex 2 (mTOR Complex 2; mTORC2), with potential Anti-tumor activity. | |||
T31223 |
DCBCI0901
DCBCI-0901,DCBCI 0901 |
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DCBCI0901 is an inhibitor of phosphatidylinositide 3-kinase (PI3K), raptor-mTOR (mTOR complex 1 or mTORC1) and rictor-mTOR (mTOR complex 2 or mTORC2) with potential antineoplastic activity. | |||
T81470 |
PI3K/mTOR Inhibitor-14
|
PI3K | PI3K/Akt/mTOR signaling |
PI3K/mTOR Inhibitor-14(化合物 Y-2)是一种针对PI3K和mTOR的双重抑制剂,其IC50值分别为171.4 nM 和10.1 nM ,具备抗肿瘤活性。 | |||
T61659 |
CC214-2
|
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CC214-2 is a potent dual inhibitor of mTORC1 and mTORC2, known for its ability to impede autophagy by modulating mammalian target of rapamycin (mTOR) signaling. With this capacity, CC214-2 shows promise in shortening the duration of tuberculosis (TB) [1]. | |||
T36084 |
PKI-179
|
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PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ... | |||
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. | |||
T6143L |
PI-103 Hydrochloride
|
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PI-103 Hydrochloride 是一种有效的PI3K 和mTOR 双重抑制剂,抑制p110α,p110β,p110δ,p110γ,mTORC1和mTORC2,IC50分别为 8 nM,88 nM,48 nM,150 nM,20 nM 和 83 nM。PI-103 Hydrochloride 也可抑制DNA-PK,IC50为 2 nM。PI-103 Hydrochloride 诱导细胞自噬 (autophagy)。 | |||
T68485 | Apilimod HCl | ||
Apilimod dimesylate is a potent and selective PIKfyve inhibitor. It exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Apilimod dimesylate inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. It reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. It also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma ... | |||
T36308 |
PF-06843195
|
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PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1]. PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells w... | |||
T38263 |
TBK1/IKKε-IN-4
TBK1/IKKε-IN-4 |
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TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2851 |
Daphnetin
7,8-Dihydroxycoumarin,Daphnetol,瑞香素 |
EGFR; PKA; PKC; Parasite; Autophagy | Angiogenesis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
Daphnetin (7,8-Dihydroxycoumarin) 是从 Genus Daphne 中分离得到的香豆素衍生物,有抗氧化、抗炎、抗疟疾和解热作用,可用于凝血功能障碍、类风湿性关节炎等疾病的相关研究。 |