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抑制剂 & 化合物

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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

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

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

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

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

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

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

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

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

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...

化合物

mTOR inhibitor-2
Cat.No: T12124
Synonym:
Target: mTOR
PI3K/mTOR Inhibitor-2
Cat.No: T12459
Synonym:
Target: PI3K, mTOR
Torin 2
Cat.No: T6100
Synonym:
Target: Apoptosis, ATM/ATR, DNA-PK, mTOR, Autophagy
Bimiralisib
Cat.No: T2265
Synonym: 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2
Target: Others, PI3K, S6 Kinase, mTOR
mTOR inhibitor 13
Cat.No: T9310
Synonym:
Target: PI3K, mTOR
TMBIM6 antagonist-1
Cat.No: T8649
Synonym: BAX-inhibitor-1,1-(2-氨基苯基)-3-(3-硝基苯基)-2-丙烯-1-酮,BIA
Target: mTOR
TFEB activator 1
Cat.No: T8055
Synonym: (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
Target: Others, Autophagy
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
D-α-Hydroxyglutaric acid disodium
Cat.No: T6820
Synonym: D-alpha-Hydroxyglutaric acid disodium salt,(R)-2-羟基戊二酸二钠盐,Disodium (R)-2-Hydroxyglutarate
Target: ATPase, Others, Reactive Oxygen Species, Endogenous Metabolite, mTOR
mTOR inhibitor 11
Cat.No: T9309
Synonym:
Target:
PKI-402
Cat.No: T3656
Synonym:
Target: PI3K, mTOR
NSC781406
Cat.No: T16355
Synonym:
Target: PI3K, mTOR
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]​-
Cat.No: T9315
Synonym:
Target: Others
Torin 1
Cat.No: T6045
Synonym:
Target: DNA-PK, PI3K, mTOR, Autophagy
Sapanisertib
Cat.No: T1838
Synonym: 沙帕色替,TAK-228,MLN0128,INK 128
Target: PI3K, mTOR, Autophagy
Compound 401
Cat.No: T3586
Synonym: 2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one
Target: DNA-PK
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
Voxtalisib
Cat.No: T7014
Synonym: XL765,SAR245409
Target: DNA-PK, PI3K, mTOR
mTOR inhibitor 9a
Cat.No: T67705
Synonym:
Target:
Torkinib
Cat.No: T2414
Synonym: PP 242
Target: Apoptosis, Mitophagy, PI3K, mTOR, Autophagy
DS-7423
Cat.No: T36083
Synonym:
Target: PI3K, mTOR
PI-103
Cat.No: T6143
Synonym: PI103,PI 103
Target: Apoptosis, DNA-PK, PI3K, mTOR, Autophagy
PP121
Cat.No: T2415
Synonym:
Target: Apoptosis, VEGFR, Bcr-Abl, PDGFR, Src, mTOR, Hck
AT-533
Cat.No: T67836
Synonym:
Target: HSP, HSV
Samotolisib
Cat.No: T6883
Synonym: GTPL8918,LY3023414
Target: DNA-PK, PI3K, mTOR, Autophagy
BC-LI-0186
Cat.No: T9533
Synonym: 4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
Target: Others
Apitolisib
Cat.No: T1916
Synonym: RG 7422,GNE 390,GDC-0980
Target: Apoptosis, PI3K, mTOR
PQR530
Cat.No: T16567
Synonym: PQR-530
Target: PI3K, mTOR
BI-860585
Cat.No: T30441
Synonym: BI860585
Target:
DCBCI0901
Cat.No: T31223
Synonym: DCBCI-0901,DCBCI 0901
Target:
PI3K/mTOR Inhibitor-14
Cat.No: T81470
Synonym:
Target: PI3K
CC214-2
Cat.No: T61659
Synonym:
Target:
PKI-179
Cat.No: T36084
Synonym:
Target:
(32-Carbonyl)-RMC-5552
Cat.No: T39958
Synonym:
Target:
PI-103 Hydrochloride
Cat.No: T6143L
Synonym:
Target:
Apilimod HCl
Cat.No: T68485
Synonym:
Target:
PF-06843195
Cat.No: T36308
Synonym:
Target:
TBK1/IKKε-IN-4
Cat.No: T38263
Synonym: TBK1/IKKε-IN-4
Target:
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。

天然产物

Daphnetin
Cat.No: T2851
Synonym: 7,8-Dihydroxycoumarin,Daphnetol,瑞香素
Target: EGFR, PKA, PKC, Parasite, Autophagy
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