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CC-99677 (Gamcemetinib) 是一种一种用于自身免疫性疾病的选择性靶向共价MAPKAPK2(MK2)抑制剂,通过亲核芳族取代(SNAr)机制将生化效力转化为LPS活化的单核细胞THP-27细胞中热休克蛋白27(HSP1)磷酸化的有效抑制所显示的细胞效力。CC-99677 在大鼠实验中展现出在生化(IC 50 =156.3 nM)和细胞检测(EC 50 =89 nM)中均有
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CC-99677 (Gamcemetinib) 是一种一种用于自身免疫性疾病的选择性靶向共价MAPKAPK2(MK2)抑制剂,通过亲核芳族取代(SNAr)机制将生化效力转化为LPS活化的单核细胞THP-27细胞中热休克蛋白27(HSP1)磷酸化的有效抑制所显示的细胞效力。CC-99677 在大鼠实验中展现出在生化(IC 50 =156.3 nM)和细胞检测(EC 50 =89 nM)中均有
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,230 | 现货 | |
5 mg | ¥ 2,650 | 现货 | |
10 mg | ¥ 4,560 | 现货 | |
25 mg | ¥ 6,900 | 现货 | |
50 mg | ¥ 9,490 | 现货 | |
100 mg | ¥ 12,800 | 现货 | |
200 mg | ¥ 17,200 | 现货 |
产品描述 | CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM). |
体外活性 | CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50 =156.3 nM) and cell based assays ( EC50 =89 nM).[1] |
别名 | Gamcemetinib, CC99677, CC 99677 |
分子量 | 469.94 |
分子式 | C22H20ClN5O3S |
CAS No. | 1887069-10-4 |
Smiles | CCOCc1cnc(Cl)nc1Oc1ccc2c3c4NC[C@@H](C)NC(=O)c4sc3ccc2n1 |
密度 | no data available |
存储 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 14.10 mg/mL (30 mM), Sonication is recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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