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Search Results for " akt-in-6 "

14

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T36310	AKT-IN-6 INCB-047775	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	AKT-IN-6 (INCB-047775)对ATK 有抑制作用。Akt 是对生长因子、细胞因子和其他细胞刺激的细胞信号传导的重要组成部分。Akt 的异常激活与2型糖尿病和癌症的发生密切相关。
T39988	6'-GNTI dihydrochloride	Opioid Receptor; Akt	Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Neuroscience; PI3K/Akt/mTOR signaling
	6'-GNTI dihydrochloride 是一种κ-阿片受体（KOR）激动剂，它偏向于激活 G 蛋白介导的信号传导，而不是β-阿司匹林2的募集。6'-GNTI dihydrochloride 只能激活纹状体神经元中的 Akt 通路。
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。
T14214	AMG 511	PI3K	PI3K/Akt/mTOR signaling
	AMG 511 是一种高效的、口服有效的 I 类 pan-PI3K 抑制剂，对 PI3Kα, β, δ 和 γ 作用的 Ki 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。它它显著抑制了 PI3K 信号，减少 p-Akt (Ser473)。它在小鼠胶质母细胞瘤移植瘤模型中具有抗肿瘤作用。
T1830	BX795	IκB/IKK; Chk; CDK; c-Kit; PDK; Autophagy	Autophagy; Cell Cycle/Checkpoint; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	BX795 是一种选择性PDK1抑制剂，也是相对特异性的TBK1和IKKɛ 抑制剂。它抑制 S6K1，Akt，PKCδ 和 GSK3β 的磷酸化，可调节自噬。
T10804	CHMFL-PI3KD-317	PI3K; PI4K	PI3K/Akt/mTOR signaling
	CHMFL-PI3KD-317 是一种高效、选择性、可口服的 PI3Kδ 抑制剂，IC50 值为 6 nM，对其选择性是对其他 PIKK 家族的 10-1500 倍，例如 PI3Kα (IC50，62.6 nM)，PI3Kβ (IC50，284 nM)，PI3Kγ (IC50，202.7 nM)，PIK3C2A (IC50，>10000 nM)，PIK3C2B (IC50，882.3 nM)，VPS34 (IC50，1801.7 nM)，PI4KIIIA (IC50，574.1 nM) 和 PI4KIIIB (IC50，300.2 nM)。在 Raji 细胞中，CHMFL-PI3KD-317 抑制 PI3Kδ 介导的 Akt T308 磷酸化，EC50 值为 4.3 nM。CHMFL-PI3KD-317 对癌细胞具有抗增殖作用。
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)
T64219	PI3K/mTOR Inhibitor-6
	PI3K/mTOR Inhibitor-6 (Compound 19c) 是一种有效的 PI3K/mTOR 双重抑制剂，在人工胃液中的稳定性比 gedatolisib 更高。10 μM 的 PI3K/mTOR Inhibitor-6 能够明显抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-6 对癌症疾病表现出研究潜力。
T36246	SJF 8240
	c-MET degrader. Comprises MET inhibitor foretinib (GSK 1363089; Cat. No. 6056) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Degrades c-MET within 6 hours in vitro. Inhibits agonist-driven AKT phosphorylation and GTL16 cell proliferation (IC50 = 66.7 nM). Also degrades exon-14-deleted c-MET in Hs746T cells.
T36015	PDMP (hydrochloride)
	PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enanti...
T38263	TBK1/IKKε-IN-4 TBK1/IKKε-IN-4
	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...
T28157	Nephrin
	Nephrin is a cell surface signaling receptor protein that regulates podocyte function and plays a role in β-cell survival signaling; it is a protein necessary for the proper functioning of the renal filtration barrier. Nephrin belongs to a family of highl
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...
T35519	Aflatoxin B2-13C17 Aflatoxin B2-13C17
	Aflatoxin B2-13C17(AFB2-13C17) is intended for use as an internal standard for the quantification of AFB2by GC- or LC-MS. AFB2is a mycotoxin that has been found inA. terricola.1It induces hepatic autophagy and apoptosis in broiler chickens when administered at doses of 0.2, 0.4, and 0.8 mg/kg.2AFB2(0.5 and 1 mg/animal) also induces parenchymal cell hyperplasia in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Alimen...

化合物

Cat.No: T36310

Synonym: INCB-047775

Target: Akt

6'-GNTI dihydrochloride

Cat.No: T39988

Target: Opioid Receptor, Akt

Cat.No: T76727

Synonym: R 1507,HZN 001

Target: TSH Receptor, IGF-1R

Cat.No: T14214

Target: PI3K

Cat.No: T1830

Target: IκB/IKK, Chk, CDK, c-Kit, PDK, Autophagy

CHMFL-PI3KD-317

Cat.No: T10804

Target: PI3K, PI4K

2-Amino-5-bromo-6-chloropyrazine

Cat.No: T35490

PI3K/mTOR Inhibitor-6

Cat.No: T64219

Cat.No: T36246

PDMP (hydrochloride)

Cat.No: T36015

TBK1/IKKε-IN-4

Cat.No: T38263

Synonym: TBK1/IKKε-IN-4

Cat.No: T28157

Cat.No: T35897

Aflatoxin B2-13C17

Cat.No: T35519

Synonym: Aflatoxin B2-13C17

Cat. No.	Product Name	Target	Signaling Pathways
T6S1699	Shogaol [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol	Lipoxygenase; Autophagy	Autophagy; Metabolism
	6-Shogaol (6-Shogaol) 是从生姜中分离的一种天然产物，具有抗癌、抗炎和抗氧化的多种生物活性。
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。
T2940	6-Hydroxyflavone 6-羟基黄酮,6-HF	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	6-Hydroxyflavone (6-HF) 是天然存在的黄酮化合物，具有抗炎作用。它对牛血红蛋白糖基化具有抑制作用。它能激活 AKT、ERK 1/2、JNK 信号通路，有效促进成骨细胞分化。它能抑制 LPS 诱导的 NO 的产生。
TN5171	Tricetin	Apoptosis; Others; Nrf2	Apoptosis; Immunology/Inflammation; Others
	Tricetin 是一种从石榴中分离出的类黄酮。Tricetin 是 Keap1-Nrf2 蛋白相互作用（PPI）的强效竞争性抑制剂，通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路，保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1（PS-1）表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症，保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。
T2S2215	Crebanine	Apoptosis; Others; Akt	Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
	Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
T75554	6-O-Isobutyrylbritannilactone
	6-O-Isobutyrylbritannilactone 是一种天然的黑素生成抑制剂。6-O-Isobutyrylbritannilactone 是一种倍半萜，可从英菊花中分离得到。6-O-Isobutyrylbritannilactone 抑制 IBMX 诱导 B16F10 细胞产生黑色素。6-O-Isobutyrylbritannilactone 也调控 ERK、PI3K/AKT 和 CREB，在斑马鱼胚胎模型中显示出抗黑色素原活性。

天然产物

Cat.No: T6S1699

Synonym: [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol

Target: Lipoxygenase, Autophagy

Cat.No: T6S1315

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

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

6-Hydroxyflavone

Cat.No: T2940

Synonym: 6-羟基黄酮,6-HF

Target: GABA Receptor

Cat.No: TN5171

Target: Apoptosis, Others, Nrf2

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

6-O-Isobutyrylbritannilactone

Cat.No: T75554

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