CAS NO: | 2183470-09-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | GCN2-IN-6 (Compound 6d) is a potent, and orally availableGCN2inhibitor confirmed by in-house enzymatic (IC50of 1.8 nM) and cellular assays (IC50of 9.3 nM). GCN2-IN-6 is also a eIF2α kinasePERKinhibitor with anIC50of 0.26 nM (in enzymatic assay) and 230 nM (in cells)[1]. | ||||||||||||||||
IC50& Target | IC50: 1.8 nM (GCN2, in-house enzymatic) and 9.3 nM (GCN2, cellular assays); 0.26 nM (PERK, in-house enzymatic) and 230 nM (PERK, cellular assays)[1] | ||||||||||||||||
体外研究 (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[1]. | ||||||||||||||||
体内研究 (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[1].
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分子量 | 485.29 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H12Cl2F2N4O3S | ||||||||||||||||
CAS 号 | 2183470-09-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(515.16 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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