Cat. No. | Product Name | Target | Signaling Pathways |
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T63653 | AKT-IN-11 | ||
AKT-IN-11 是有效的抗人肝癌 Bel-7402 细胞株抗菌剂之一 (IC50: 1.15 μM)。 | |||
T4444 |
A-674563 HCl (552325-73-2(free base))
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ERK; Akt; PKA; CDK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
A-674563 HCl (552325-73-2(free base)) 是一种口服的、ATP 竞争性的、可逆的 Akt 抑制剂(Akt1 的 Ki:11 nM)。它对 PKA 和 Cdk2 具有抑制活性(IC50:16/46 nM),但对 Akt1 的选择性比 CMGC、CAMK 和 TK 家族中的其他激酶高 10 至 >1800 倍。 | |||
T62408 |
PI3Kδ-IN-11
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PI3Kδ-IN-11 是一种高效的、选择性的 PI3Kδ 抑制剂 (IC50: 27.5 nM),能够剂量依赖性地阻断 PI3K/Akt 通路的活性。PI3Kδ-IN-11 能够用于 B 细胞或 T 细胞相关的恶性肿瘤研究。 | |||
T63528 | HSP90-IN-11 | ||
HSP90-IN-11 是 HSP90 的有效抑制剂,诱导亚 G1 期群体的显着积累。 HSP90-IN-11 具有与 AUY-922 (Luminespib) 相当的有效 HSP90α 抑制作用。在 CRC 和 NSCLC 细胞中,HSP90-IN-11 具有显着的抗增殖活性,在两位数 nM 范围内。HSP90-IN-11 能够快速降解 NSCLC 细胞中客户蛋白 EGFR 和 Akt 。 | |||
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... | |||
T35527 |
PI3Kα-IN-4
PI3Kα-IN-4 |
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PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t... |