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| 品牌 | absin | CAS | 186611-52-9 |
|---|---|---|---|
| 分子式 | C18H17NO4 | 纯度 | ≥98% |
| 分子量 | 311.33 | 货号 | abs47028046 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a novel inhibitor of CK1 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
IC261 186611-52-9
| 产品描述 | |
| 描述 | IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM. |
| 纯度 | ≥98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | SU-5607；IC 261 |
| 外观 | yellow solid |
| 可溶性/溶解性 | DMSO : ≥ 33 mg/mL (106.00 mM) |
| 生物活性 | |
| 靶点 | Casein Kinase |
| In vitro(体外研究) | IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC261 is less active on PKA, p34cdc2, and p55fyn (IC50s > 100 μM). IC261 induces mitotic arrest, spindle defects and centrosome amplification in AC1-M88 cells. IC261 (1 μM) increases G2/M cells after 12 h, and causes cell death at 24 h in AC1-M88 cells. IC261 (1 μM) also induces apoptosis in the extravillous trophoblast hybrid cells. IC261 (1.25 μM) suppresses the proliferation of several pancreatic tumour cell lines, including ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1 and PancTu-2 cells. IC261 (1.25 μM) specifically enhances CD95-mediated apoptosis of pancreatic tumour cells. |
| In vivo(体内研究) | IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/∊, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice. |
| 研究领域 | |
| 研究领域 | Stem CellsSignaling Pathways Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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