化合物STF083010 T6681

Product Introduction
Bioactivity


英文名: STF-083010

描述: STF-083010 是一种 IRE1α 核酸内切酶的选择性抑制剂。

细胞实验: 3×10E3 (Panc0403, Panc1005, BxPc3, and MiaPaCa2) cell lines are seeded in 96-well plates overnight, and STF-083010(~50 μM) treatment for 48 hours started the next day.

激酶实验: Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography.

动物实验: NOD/SCID/IL2Rγ null mice were injected intraperitoneally of STF-083010(30 mg/kg) dissolved in 16% chremophor.

体外活性: WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 hours cultures. In MM.1R MM, MM.1S, and RPMI 8226 cell lines, STF-083010 displays cytostatic and cytotoxic activity in a dose and time-dependent manner. In Eμ-TCL1 CLL cells, STF-083010 displays about 70% growth inhibition after 3 days culture. In SU8686, Panc0403, and MiaPaCa2 cell lines, STF-083010 blocks IRE1α's endonuclease and inhibits XBP1 splicing activity without affecting its kinase activity.

体内活性: STF-083010（i.p.，30 mg/kg）在人类多发性骨髓瘤（MM）异种移植模型中显著抑制了肿瘤的生长。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 31.7 mg/mL (100 mM)


关键字: STF 083010 | Inositol requiring enzyme 1 | Inhibitor | inhibit | IRE1 | STF-083010

相关产品: B I09 | IRE1α kinase-IN-9 | IXA6 | MKC3946 | IRE1α kinase-IN-1 | IXA4 | 6-Bromo-2-hydroxy-3-methoxybenzaldehyde | 4μ8C | Toyocamycin | MKC9989

相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Endoplasmic Reticulum Stress Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Diabetic Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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