SML1827

CCF642

≥98% (HPLC)

• 別名: 3-(4-Methoxyphenyl)-5-((5-nitrothiophen-2-yl)methylene)-2-thioxothiazolidin-4-one
• 実験式（ヒル表記法）: C₁₅H₁₀N₂O₄S₃
• CAS番号: 346640-08-2
• 分子量: 378.45
• MDL番号: MFCD01899742
• UNSPSCコード: 12352200
• PubChem Substance ID: 329826084
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 保管条件: protect from light
• 色: yellow to orange
• 溶解性: DMSO: 5 mg/mL, clear (warmed)
• 保管温度: 2-8°C
• SMILES記法: S=C1SC(C(N1C(C=C2)=CC=C2OC)=O)=CC(S3)=CC=C3[N+]([O-])=O
• InChI: 1S/C15H10N2O4S3/c1-21-10-4-2-9(3-5-10)16-14(18)12(24-15(16)22)8-11-6-7-13(23-11)17(19)20/h2-8H,1H3

詳細

アプリケーション

CCF642 has been used as a protein disulfide isomerase (PDI) inhibitor to study its ability to reduce the expression of endoplasmic reticulum (ER) stress markers and neuroinflammation in the hippocampus of experimental autoimmune encephalomyelitis (EAE) mice.

生物化学的／生理学的作用

CCF642 is a cell-permeable protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action that most likely involves PDI active-site CGHCK motifs instead of cysteine known to be targeted by PACMA 31. CCF642 displays anti-multiple myeloma (MM) activity both in cultures in vitro (IC₅₀ <1 μM against murine 5TGM1 and nine human MM lines) and in mice in vivo (10 mg/kg, 3X i.p. per wk) without apparent adverse effects to the animals or being cytotoxic to normal bone marrow (NLBM) cells even at concentrations as high as 6.75 μM. Consistent with PDI′s role in ER protein folding process, CCF642 treatment causes acute ER stress accompanied by apoptosis-inducing calcium release in MM cells.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3