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GCN2-IN-6

CAS No. : 2183470-09-7

MCE 国际站：GCN2-IN-6

产品活性：GCN2-IN-6 (Compound 6d) 是一种有效的口服 GCN2 抑制剂，通过酶法 (IC₅₀ 为 1.8 nM) 和细胞分析 (IC₅₀ 为 9.3 nM) 证实。GCN2-IN-6 还是 eIF2α 激酶 PERK 抑制剂，IC₅₀ 为 0.26 nM (酶法测定) 和 230 nM (细胞测定)。

研究领域：Cell Cycle/DNA Damage

作用靶点：Eukaryotic Initiation Factor (eIF)

In Vitro: To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF. GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase.

In Vivo: GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral administration; for 8 hours; mice) treatment at 3 mg/kg suppresses both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Endoplasmic Reticulum Stress Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  eIF4A3-IN-18  |  CR-1-31-B  |  rel-Zotatifin  |  eIF4A3-IN-14  |  4E2RCat  |  (Z)-4EGI-1  |  eIF4A3-IN-8  |  Rocaglamide  |  eIF4A3-IN-1  |  CMLD012073  |  eIF4A3-IN-11  |  eIF4A3-IN-13  |  ML291  |  ATPγS tetralithium salt  |  eIF4A3-IN-15  |  2BAct  |  GCN2-IN-1  |  eIF4A3-IN-10  |  eIF4E-IN-3  |  eIF4A3-IN-5  |  eIF4A3-IN-9  |  eIF4E-IN-1  |  Rohinitib  |  EIF2α activator 2  |  CMLD012612  |  eIF4A3-IN-2  |  GCN2iB  |  eIF4A3-IN-17

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