Cat. No. | Product Name | Target | Signaling Pathways |
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T62696 | PI3K-IN-30 | ||
PI3K-IN-30 (compound 6d) 是一种 PI3K 的有效抑制剂,能够作用于 PI3Kα (IC50: 5.1 nM)、PI3Kβ (IC50: 136 nM)、PI3Kγ (IC50: 30.7 nM) 和 PI3Kδ (IC50: 8.9 nM)。 | |||
T6070 |
(E/Z)-Rigosertib sodium
N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium |
PLK | Cell Cycle/Checkpoint |
ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂(IC50 为 9 nM,在无细胞试验中)。它对 Plk2 的选择性高出 30 倍,对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物,具有潜在的抗肿瘤活性。 | |||
T36085 |
PKI-179 hydrochloride
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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... | |||
T78568 |
PI3Kδ-IN-15
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PI3K | PI3K/Akt/mTOR signaling |
PI3Kδ-IN-15(compound 6b)为一选择性PI3Kδ抑制剂,p110δ的IC50为0.5 nM,其对PI3Kδ的抑制效力高于PI3Kγ、PI3Kβ及PI3Kα30倍。 | |||
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 ... | |||
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... |