akt-in-6

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。

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。

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。

CHPG是一种选择性的mGluR5激动剂，能减少LDH释放与神经元凋亡，激活ERK和Akt通路并保护创伤性脑损伤，还能够提高人OPCs细胞的分化数量和减轻LPS诱导的炎症。

Rhodiolin(红景天灵)是一种来自于Rhodiola rosea（红景天）的天然产物，能够阻断葡萄糖6-磷酸异构酶（GPI）的糖酵解，抑制人乳头状甲状腺癌（PTC）中PI3K/AKT/mTOR信号通路磷酸化，诱导PTC细胞凋亡。

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。

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。

UNC10013 是一种 SETDB1 的变构调节剂，通过与 3TD 结构域的 Cys385 结合，形成共价键并展现负向变构调节活性，kinact/KI 为 1.0 × 10^6 M^-1*s^-1。UNC10013 能够有效地干扰 SETDB1 介导的 Akt 甲基化，对癌症和神经退行性疾病的研究有潜在应用价值。

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。

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。

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)

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. Aliment.31(4-6)607-615(1977) 2.Chen, B., Li, D., Li, M., et al.Induction of mitochondria-mediated apoptosis and PI3K/Akt/mTOR-mediated autophagy by aflatoxin B2 in hepatocytes of broilersOncotarget7(51)84989-84998(2016) 3.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971)

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 enantiomer is also responsible for inhibition of β-1,4-galactosyltransferase 6 and prevention of lactosylceramide synthesis, which is a promotor of neuroinflammation in mice during chronic experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis. PDMP enhances curcumin-induced inhibition of proliferation, JNK activation, and Akt inhibition, as well as induction of apoptosis in WM-115 melanoma cells in vitro.

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.

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/IKKε-IN-4 (Compound II; 0-2 μM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity[1].TBK1/IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC50 =62 nM), and the IFNβ target genes IP10 (IC50 =78 nM) and Mx1 (IC50=20 nM). TBK1/IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 μM[1]. [1]. Ou YH, et al. TBK1 directly engages Akt/PKB survival signaling to support oncogenic transformation. Mol Cell. 2011 Feb 18;41(4):458-70.

AKT-IN-1 (AZD-26) 是一种变构的 AKT 抑制剂，其 IC50=1.042 μM。

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。

Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

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。

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。

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。

Anticanceragent 109 (compound 6-15) 是 Gas6-Axl 轴的抑制剂，具有抑癌活性。Anticanceragent 109 抑制 Gas6 和 Axl 的表达，抑制 p-PI3K 和 p-AKT 的表达，导致肿瘤细胞周期 G1 期阻滞并促进细胞凋亡 (apoptosis)，在裸鼠荷瘤模型中显著抑制肿瘤生长。

Antidiabetic agent 6 (Compound 19)作为一种抗糖尿病化合物,通过激活PI3K/AKT依赖性信号通路来促进GLUT4的易位.此外,该化合物还能有效降低链脲佐菌素诱导的糖尿病大鼠的血糖水平.

6-Epi-ophiobolin G (MHO7) 是一种源自海洋真菌的代谢物，作为Akt抑制剂，其具备透过血脑屏障和口服活性的能力。6-Epi-ophiobolin G (MHO7) 能抑制胶质母细胞瘤 (GBM) 细胞增殖并促进其凋亡，可用于胶质母细胞瘤的研究。