生物活性 | |||
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描述 | CCF642 is a strong inhibitor of protein disulfide isomerases (PDI) with an IC50 of 2.9 μM. It induces acute endoplasmic reticulum (ER) stress in multiple myeloma cells, leading to apoptosis through calcium release. CCF642 is recognized for its extensive anti-multiple myeloma effects. When used at 3 μM for 0.5 to 6 hours, CCF642 enhances PERK dimerization through phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE cells, indicating the accumulation of misfolded proteins in the ER. As a compound that spares bone marrow, CCF642 shows a submicromolar IC50 across a range of multiple myeloma cell lines (MM1.S, MM1.R, KMS-12-PE, KMS-12-BM, NCI-H929, U266, RPMI 8226, JJN-3, HRMM.09-luc, 5TGM1-luc)[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.21mL 2.64mL 1.32mL |
26.42mL 5.28mL 2.64mL |
参考文献 |
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