上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
GCN2-IN-6 纯度: 98.47%
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)。
GCN2-IN-6 Chemical Structure
CAS No. : 2183470-09-7
| 规格 | 价格 | 是否有货 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO | ￥3850 | In-stock | |
| 5 mg | ￥3500 | In-stock | |
| 10 mg | ￥5500 | In-stock | |
| 50 mg | ￥16500 | In-stock | |
| 100 mg | ￥28000 | In-stock | |
| 200 mg | 询价 | ||
| 500 mg | 询价 |
* Please select Quantity before adding items.
GCN2-IN-6 相关产品
•相关化合物库:
- 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
| 生物活性 |
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 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] |
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| 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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 |
485.29 |
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| Formula |
C19H12Cl2F2N4O3S |
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| CAS 号 |
2183470-09-7 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 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
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
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| 参考文献 |
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