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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T63470 PI3K/mTOR Inhibitor-8

PI3K/mTOR Inhibitor-8PI3K (PI3Kα IC50: 0.46 nM) 和 mTOR (mTOR IC50: 12 nM) 双重抑制剂。PI3K/mTOR Inhibitor-8 能够将 HCT-116 细胞的细胞周期阻滞在G1/S 期,并诱导其凋亡 (apoptosis)。
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 IPI3KmTOR 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。
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 PI3KmTOR 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。
T62580 PI3K-IN-37

PI3K-IN-37 (Example 84.1) 是一种 PI3K α (IC50: 6 nM) /β (IC50: 8 nM) /δ (IC50: 4 nM) 抑制剂。PI3K-IN-37 对 mTOR 具有抑制作用,其 IC50 值为4 nM。
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 ...
T36085 PKI-179 hydrochloride

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC5...
T6143L PI-103 Hydrochloride

PI-103 Hydrochloride 是一种有效的PI3KmTOR 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)。

化合物

PI3K/mTOR Inhibitor-8
Cat.No: T63470
Synonym:
Target:
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
PI-103
Cat.No: T6143
Synonym: PI103,PI 103
Target: Apoptosis, DNA-PK, PI3K, mTOR, Autophagy
PI3K-IN-37
Cat.No: T62580
Synonym:
Target:
PKI-179
Cat.No: T36084
Synonym:
Target:
PKI-179 hydrochloride
Cat.No: T36085
Synonym:
Target:
PI-103 Hydrochloride
Cat.No: T6143L
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1891 Lupiwighteone

Apoptosis; BCL; PARP; Caspase Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Proteases/Proteasome
Lupiwighteone 是一种广泛存在于野生植物中的异黄酮。它通过抑制 PI3K/Akt/mTOR 通路,诱导人乳腺癌细胞 caspase 依赖性和非依赖性凋亡,具有抗氧化、抗菌和抗癌作用。

天然产物

Lupiwighteone
Cat.No: TN1891
Synonym:
Target: Apoptosis, BCL, PARP, Caspase
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