lyn in 1

Lyn-IN-1 (Bafetinib analog) 是一种高活性 Bcr-Abl 和 Lyn 双重抑制剂。

LYN-1604 2HCl 是一种有效的 UNC-51 样激酶 1 激活剂，EC50值为 18.94 nM。LYN-1604 可研究三阴性乳腺癌。

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

LYN-1604 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).

Multi-kinase-IN-2 是口服具有活力的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 能够显著抑制血管激酶的活性，如 VEGFR-1 2 3、PDGFRα β、FGFR-1、LYN 和 c-KIT 激酶。Multi-kinase-IN-2 能够明显减弱 AKT 和 ERK 蛋白的磷酸化，并可诱导细胞凋亡 (apoptosis)，具有抗癌作用。

Lyn peptide inhibitor TFA 是一种有效的，可以细胞渗透的抑制剂，抑制Lyn 偶联的IL-5受体相关信号通路，同时保持其他信号的完整。Lyn peptide inhibitor TFA 可以阻断 Lyn 的激活，抑制 Lyn 酪氨酸激酶与 IL-3 GM-CSF IL-5 受体的 βc 亚基结合。Lyn peptide inhibitor TFA 可用于哮喘、过敏等嗜酸性疾病的研究。

BTK-IN-34 (compound 9h) 作为选择性BTK抑制剂，主要通过抑制 pBTK (Tyr223) 来展现其在 RAMOS 细胞中的抗增殖活性，同时不干扰 Lyn 和 Syk (上游蛋白) 在 BCR 信号通路中的作用。