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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T62842	AKT-IN-8
	AKT-IN-8 是一种 AKT 的有效抑制剂，能够作用于 AKT1 (IC50: 4.46 nM)、AKT2 (IC50: 2.44 nM) 和 AKT3 (IC50: 9.47 nM)。
T76727	Teprotumumab R 1507,HZN 001	TSH Receptor; IGF-1R	GPCR/G Protein; Tyrosine Kinase/Adaptors
	Teprotumumab 是一种阻断 IGF-1 受体 (IGF-1R) 的人单克隆抗体。Teprotumumab 与 IGF-1R 的细胞外 α-亚基结构域配体结合。Teprotumumab 抑制纤维细胞中的 TSH 和 IGF-1 作用。Teprotumumab 可降低 TSH 依赖性 IL-6 和 IL-8 的表达和 Akt 的磷酸化。Teprotumumab 可用于甲状腺相关眼病的研究。
T61680	AKT-IN-5
	AKT-IN-5 (Example 8) is a chemical compound known as an Akt inhibitor, specifically targeting Akt1 and Akt2. Its potency is reflected in IC50 values of 450 nM and 400 nM for Akt1 and Akt2, respectively [1].
T61891	SHP2-IN-8
	SHP2-IN-8 是一种可逆、非竞争性、选择性、高效性的变构SHP2抑制剂（IC50= 23 nM，Ki= 22 nM），在细胞中也有效果。SHP2-IN-8 能引起显著的热位移（ΔTm = 7.01 ℃）。SHP2-IN-8 可抑制AKT 的磷酸化，诱导 Hela 细胞凋亡 (apoptosis)。
T81784	MK-2206 free base	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	MK-2206 free base是一种口服活性、高选择性的变构Akt抑制剂，IC50分别针对Akt1、Akt2、Akt3为8、12和65 nM 。多种乳腺癌细胞系、PIK3CA突变以及PTEN缺失细胞系对此化合物敏感，显示出抗癌活性。
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...
T36648	Tucatinib hemiethanolate
	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ...

化合物

Synonym: R 1507,HZN 001

Target: TSH Receptor, IGF-1R

PKI-179 hydrochloride

Cat.No: T36085

Synonym:

Target:

Tucatinib hemiethanolate

Cat.No: T36648

Synonym:

Target:

Cat. No.	Product Name	Target	Signaling Pathways
TN1346	Oxypalmatine 8-Oxypalmatine	Apoptosis	Apoptosis
	Oxypalmatine (8-Oxypalmatine) 是在 Phellodendron amurense 中分离出来的小檗碱型生物碱，通过抑制 PI3K/AKT 信号传导及其对乳腺癌类器官的功效来调节乳腺癌细胞的增殖和凋亡。
T3861	Isobavachalcone Corylifolinin,Isobacachalcone,补骨脂乙素	Apoptosis; Others; Reactive Oxygen Species; Akt; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; NF-κB; Others; PI3K/Akt/mTOR signaling
	Isobavachalcone (Corylifolinin) 是来源于补骨脂的一种Akt 信号通路抑制剂，可诱导人类癌细胞凋亡，以IC50值为 7.92 μM 抑制 OVCAR-8 癌细胞生长，具有抗癌和抗增殖活性。它还能诱导 OVCAR-8 细胞中活性氧的产生。
T40483	8-Aminoadenosine 8-NH2-Ado,8-氨基腺苷
	8-Aminoadenosine (8-NH2-Ado) is an RNA-directed nucleoside analogue that effectively diminishes cellular ATP levels and impedes mRNA synthesis. Furthermore, it effectively obstructs Akt/mTOR signaling, inducing autophagy and apoptosis in a p53-independent manner. Its significant antitumor activity further highlights its therapeutic potential.
TN1728	Hellebrigenin	PARP; Akt; CDK	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Hellebrigenin has anti-hepatoma activities, it induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells through inhibition of Akt. Hellebrigenin exhibites moderate to strong activity against human HL-60, SF-295, MDA-MB-435, and HCT-8 cancer cell strains without hemolysis of mouse erythrocytes.