mek in 1

MEK-IN-1 is a MEK inhibitor.

MEK-IN-4 是一种 MEK 抑制剂，可用于研究炎症性疾病和癌症。

MEK RAF-IN-1 (Compound 16b) 作为一种针对MEK和RAF的抑制剂，其针对MEK1、BRAF和BRAFV600E的IC50值分别仅为28、3和3 nM。该化合物表现出明显的抗肿瘤效果，能够有效抑制体外MIA PaCa-2 (G12C KRAS)、HCT116 (G13D KRAS) 以及 C26 (G12D KRAS) 细胞的增殖，并在异种移植的结直肠癌小鼠模型中显著抑制肿瘤生长。

MEK PI3K-IN-1（compound 6r）是一种高效的MEK PI3K抑制剂，IC50值为124 nM（MEK1）、130 nM（PI3Kα）及236 nM（PI3Kδ）。该化合物能够降低pAKT和pERK1 2的活性，并展现对肿瘤细胞的抗增殖作用。

MEK1 2-IN-3 (Compound M15) 是一种MEK1抑制剂，IC50为10.29 nM。它能够抑制肿瘤细胞的增殖和迁移，并诱导细胞凋亡 (apoptosis)，同时表现出良好的肝微粒体稳定性。MEK1 2-IN-3 适用于实体瘤领域的研究。

MEK4 inhibitor-1 is a newly developed compound specifically designed to inhibit the activity of MEK4, a key enzyme involved in pancreatic adenocarcinoma, with an IC 50 value of 61 nM.

MEK1 2-IN-2 是有效的、ATP 竞争性的 MEK1 2 抑制剂，对野生型 MEK1 2 和一组 MEK1 2 突变细胞表现出同等的抑制效果。

Antiproliferative against-3 具有良好的抗癌细胞增殖活性，对 Hela、A549 和 MCF-7 的细胞的 IC50值分别为 0.21 µM、0.39 µM 和 0.33 µM。Antiproliferative against-3 (comp 33) 剂量依赖性的诱导 A549 细胞的凋亡，并将细胞阻滞在 G1 期。

MEK1Derived Peptide Inhibitor 1，一种肽抑制剂，以IC50值30 μM抑制MEK1激活ERK2。适用于细胞渗透性研究。

Myristoyl-MEK1 Derived Peptide Inhibitor 1 是MEK1Derived Peptide Inhibitor 1 的豆蔻酰化形式。Myristoyl-MEK1 Derived Peptide Inhibitor 1 抑制ERK 的激活，IC50为 10 μM。

PROTACMEK1Degrader-1是一种针对MEK1的PROTAC，显示出pIC50值为7.0。该化合物由MEK1抑制剂与von Hippel-Lindau配体构成，能够抑制ERK1 2的磷酸化，并对A375细胞展现出抗增殖活性。

STE-MEK1(13)（Ste-MPKKKPTPIQLNP-NH2）为一细胞渗透性ERK1 2抑制剂，IC50值为13-30μM，可抑制ERK1 2磷酸化。

MEK1 C-Raf-IN-1 (Compound 14d) 为一种MEK1与C-Raf的抑制剂，其IC50值分别达到97 nM及23 nM。此化合物展现出了抗肿瘤效果。

TAT-MEK1是ERK2的抑制剂，由TAT和MEK1(N-terminal)组成。TAT(YGRKKRRQRRR)源自人免疫缺陷(HIV-1)转录反式激活因子(TAT)，是一种穿透细胞的肽。TAT-MEK1体外对ERK2的IC50为29 μM。

Lidocaine (Alphacaine) 是一种酰胺衍生物，抑制涉及复杂电压和依赖性的钠通道，可用于研究室性心律失常。它通过调节 miR-145 表达和进一步抑制 MEK ERK 和 NF-κB 信号通路来减少胃癌细胞的生长，迁移和侵袭。

TAC(TERT activator compound) 作为 TERT 的激活剂，能通过 MEK ERK AP-1 级联途径增强 TERT 的转录活性。该化合物不仅促进端粒的合成，还可减少衰老标志物、炎症及衰老现象，同时维持脑部健康。这些作用突显了 TERT 在抗衰老及相关疾病治疗中的应用潜力。

PD 184161 是一种口服有效的，时间和浓度依赖的 MEK 抑制剂，IC50为10-100 nM。它诱导抑郁样行为，抑制细胞增殖并诱导细胞凋亡。

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Raf-MEK signaling, which results in an increased rate of SMN translation.

iMDK quarterhydrate, a potent PI3K inhibitor, is effective in inhibiting the growth factor MDK (also known as midkine or MK) while demonstrating suppression of non-small cell lung cancer (NSCLC). In combination with a MEK inhibitor, iMDK quarterhydrate demonstrates cooperative inhibition of NSCLC without causing harm to normal cells and mice [1].

Nardosinone 是一个 dbcAMP 和 staurosporine 的神经生成作用增强剂，分离自Nardostachys chinensis 中。Nardosinone 可能成为一种有用的药理学工具，不仅可用于研究神经生长因子 (NGF) 的作用机理，而且可用于研究神经毒性物质的作用机理。

MEK PI3K-IN-2 (compound 6s) 是一种有效的 MEK PI3K 抑制剂，其 IC50值分别为 352 nM (MEK1), 107 nM (PI3Kα), 和 137 nM (PI3Kδ)。MEK PI3K-IN-2 抑制 pAKT 和 pERK1 2 水平。MEK PI3K-IN-2 对肿瘤细胞具有抗增殖活性。

Trametiglue 是 Trametinib 的衍生物，通过独特的界面结合相互作用，以前所未有的效力和选择性靶向 KSR-MEK 和 RAF-MEK。

CML-IN-1（compound 7）是一种高效抗癌药物，针对人类慢性粒细胞白血病（CML）细胞系K562，能有效诱导凋亡（apoptosis）。该化合物主要通过显著抑制PI3K Akt信号通路的蛋白磷酸化来发挥作用，同时CML-IN-1（compound 4）也能通过抑制结直肠癌的MEK ERK信号通路来阻止细胞增殖。