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12

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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].
T4489	AKT-IN-1 AZD26,AZD-26,6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺,AZD 26	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	AKT-IN-1 (AZD-26) 是一种变构的 AKT 抑制剂，其 IC50=1.042 μM。
T3132	SC66	Apoptosis; Akt	Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	SC66 是一种Akt 抑制剂，可降低细胞活力。它以剂量和时间依赖性地抑制肝癌细胞的集落形成和诱导凋亡。
T8656	CAY10404 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T	Apoptosis; Akt; COX	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; PI3K/Akt/mTOR signaling
	CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) 是一种有效且高度选择性的 COX-2 和 COX-1 抑制剂。它还是 PKB/Akt 和 MAPK 信号通路的有效抑制剂，可诱导 NSC-LC 细胞凋亡，具有镇痛、抗炎和抗癌活性。
T10274	AKT-IN-2	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1).
T79722	2-Chlorophenoxazine	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	2-Chlorophenoxazine为Akt抑制剂，体外IC50为2-5 μM，能够诱导细胞凋亡(apoptosis)，适用于癌症病理研究。
T35490	2-Amino-5-bromo-6-chloropyrazine
	2-Amino-5-bromo-6-chloropyrazine is a heterocyclic building block.1,2It has been used in the synthesis of Akt inhibitors. 1.Kettle, J.G., Brown, S., Crafter, C., et al.Diverse heterocyclic scaffolds as allosteric inhibitors of AKTJ. Med. Chem.55(3)1261-1273(2012) 2.Goel, R., Luxami, V., and Paul, K.Recent advances in development of imidazo[1,2-a]pyrazines: Synthesis, reactivity and their biological applicationsOrg. Biomol. Chem.13(12)3525-3555(2015)
T64083	MMP-9-IN-5
	MMP-9-IN-5 是一种 MMP-9 抑制剂，其 IC50 值为 4.49 nM，能够与 MMP-9 形成氢键。MMP-9-IN-5 也抑制 AKT 活性，其 IC50 值为 1.34 nM。MMP-9-IN-5 表现出细胞毒性，可诱导细胞凋亡 (apoptosis)，能够用于研究癌症。
T35855	AAA
	AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...
T36197	CAY10747
	CAY10747 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) and a derivative of celastrol .1It decreases protein levels of the Hsp90-Cdc37 complex and the Hsp90-Cdc37 clients phosphorylated Akt and Cdk4 in A549 cells when used at a concentration of 5 μM. CAY10747 inhibits proliferation of A549, MCF-7, HOS, and HepG2 cells (IC50s = 0.41, 0.64, 0.9, and 0.94 μM, respectively) and induces apoptosis in A549 cells. 1.Li, N., Xu,...
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT...
T35874	CC260
	CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph...

化合物

Cat.No: T61680

Cat.No: T4489

Synonym: AZD26,AZD-26,6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺,AZD 26

Target: Akt

Cat.No: T3132

Target: Apoptosis, Akt

Cat.No: T8656

Synonym: 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T

Target: Apoptosis, Akt, COX

Cat.No: T10274

Target: Akt

2-Chlorophenoxazine

Cat.No: T79722

Target: Akt

2-Amino-5-bromo-6-chloropyrazine

Cat.No: T35490

Cat.No: T64083

Cat.No: T35855

Cat.No: T36197

Cat.No: T35897

Cat.No: T35874

Cat. No.	Product Name	Target	Signaling Pathways
T4S0498	Glaucocalyxin A 蓝萼甲素,Wangzaozin B,Leukamenin F	Apoptosis; Akt; Caspase; PI3K	Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K/Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。
T6S0659	Rhynchophylline 钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin	Calcium Channel; NF-κB	Membrane transporter/Ion channel; Metabolism; NF-κB
	Rhynchophylline (Mitrinermine) 是一种生物碱类化合物，从钩藤中分离得到，具有很高的生物活性，被广泛用于抗炎、神经保护等方面的研究。
T6S2099	Geraniin	Antioxidant; TNF	Apoptosis; oxidation-reduction
	Geraniin 是一种肿瘤坏死因子α释放抑制剂，其IC50值为 43 μM，具有抗肿瘤、抗炎和抗高血糖活性。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

天然产物

Glaucocalyxin A

Cat.No: T4S0498

Synonym: 蓝萼甲素,Wangzaozin B,Leukamenin F

Target: Apoptosis, Akt, Caspase, PI3K

Rhynchophylline

Cat.No: T6S0659

Synonym: 钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin

Target: Calcium Channel, NF-κB

Cat.No: T6S2099

Target: Antioxidant, TNF

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

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