k 4

Antibiotic K 4 is an inhibitor of angiotensin I converting enzyme produced by Actinomadura spiculosospora.

Vitamin K4 (Menadiol Diacetate) 是一种维生素药物，用于治疗因缺乏 VK4 引起的凝血障碍。

K4 peptide 是一种抗菌肽，对革兰氏阳性细菌和革兰氏阴性细菌均显示出显著活性，能够有效作用于包括金黄色葡萄球菌和弧菌属海洋细菌在内的多种人类致病菌。

MAP4K4-IN-3 (Compound 17) 是 MAP4K4选择性抑制剂，在激酶实验中 IC50为 14.9 nM，在细胞实验中 IC50为 470 nM。具有抗糖尿病作用。

MAP4K4-IN-6 (Compound 15f) 是一种有效的MAP4K4抑制剂，其IC50值为80 nM。它能有效降低c-Jun的磷酸化水平，并具备神经保护功能，能增强运动神经元的活性。因此，MAP4K4-IN-6常被用于肌萎缩侧索硬化症（ALS）的相关研究中。

TNIK&MAP4K4-IN-1（化合物A-39）作为TNIK和MAP4K4 HGK的双效抑制剂，在LX-2人肝星状细胞中，其IC50为1.29 nM和<10 nM。该化合物适用于癌症和纤维化治疗。

TAK1 MAP4K2 inhibitor 1(compound 5)是一种 TAK1 和 MAP4K2 的双重激酶抑制剂，IC50 值分别为 41.1 nM 和 18.2 nM。

Menaquinone-4 (Vitamin K2) 是维生素 K 的一种，用作止血剂，有潜力用于骨质疏松的研究。

K-Ras G12C-IN-4 是一种 KRAS G12C 共价抑制剂。

K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras-IN-4（化合物CP163）属于K-Ras抑制剂类。

M4K2308 是一种高度选择性的ALK2醚连接抑制剂，具有 2 nM 的IC50值。相比之下，该化合物对 ALK5 的选择性较低，其 IC50 为 224 nM。此外，M4K2308 显示出对于研究弥漫性内在性脑桥神经胶质瘤 (DIPG) 具有重要潜力。

M4K2281是一种针对ALK2的高效选择性抑制剂，其半抑制浓度（IC50）为2纳摩尔。在生化及细胞分析中，M4K2281及M4K2308均展现出针对ALK2的高效作用。此外，M4K2281的大脑至血浆比率介于中等至高。

(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors. ACS Med Chem Lett. 2020 Jun 10;11(7):1463-1469.

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit tumor growth by 73.0% in mice[1].PI3Kα-IN-4 (15-40 mg kg; p.o. once daily for 30 d) dose dependently suppresses tumor growth by 62.5% (15 mg kg), 86.0% (30 mg kg) and 90.7% (40 mg kg), respectively in mice[1].PI3Kα-IN-4 (15-40 mg kg; p.o. once daily; 1-4 h) inhibits the phosphorylation of Akt in a dose- and time-dependent manner in vivo[1].PI3Kα-IN-4 shows high Cmax (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) following oral administration (mouse 10, rat 3 mg kg)[1].PI3Kα-IN-4 shows t1 2 (mouse 0.99, rat 1.22 h) and low plasma clearance (mouse 4.16, rat 5.28 mL min kg) following intravenous injection (mouse 1, rat 1 mg kg)[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors. ACS Med Chem Lett. 2020 Jun 10; 11(7): 1463-1469.

PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC 50 s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.

CHMFL-PI4K-127 (compound 15g) 是具有口服活性、高选择性的PfPI4K(恶性疟原虫 PI4K 激酶)抑制剂（IC50= 0.9 nM）。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性（EC50= 25.1 nM）。CHMFL-PI4K-127 具有抗疟疾作用。

PI3Kγ inhibitor 4 是一种选择性的、有效的、口服具有活力的 PI3Kγ 抑制剂 (IC50: 40 nM)。PI3Kγ inhibitor 4 对 PI3Kγ 的选择性是 α 亚型的~7 倍、是 β 亚型的 43 倍、是 δ 亚型的 18 倍。PI3Kγ inhibitor 4 能够用于研究气道炎症。

PI3K mTOR Inhibitor-4 是一种口服具有活力的泛 I 类 PI3K mTOR 抑制剂。PI3K mTOR Inhibitor-4 具有酶抑制作用，能够作用于 PI3Kα (IC50: 0.63 nM)、PI3Kγ (IC50: 22 nM)、PI3Kδ (IC50: 9.2 nM) 和 mTOR (IC50: 13.85 nM)。PI3K mTOR Inhibitor-4 能够用于研究癌症。

CDK8-IN-4k is a potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition.

M4K2234 (compound 26b) 是 ALK2的抑制剂。M4K2234 抑制 ALK2和 ALK5的 IC50值分别为 5 和 2144 nM。M4K2234 可用作 ALK1和 ALK2蛋白激酶的化学探针。M4K2234 可用于癌症的研究。

PI5P4Kα-IN-1（化合物13）是一种针对PI5P4Kα和PI5P4Kβ具有选择性抑制作用的化合物（IC50分别为2 μM和9.4 μM）。它适用于癌症、代谢和免疫紊乱相关研究。

PI5P4K-β-IN-2 (compound d5)为一种PI5P4K-β抑制剂，IC50值为0.35 μM，展现出抗癌活性。

PI5P4K-β-IN-1（compound vs1）是一款针对PI5P4K-β具有高效抑制活性的化合物，其IC50值为0.80 μM。