| Identification | Back Directory | [Name]
CCF-642 | [CAS]
346640-08-2 | [Synonyms]
CCF-642
AC1LYELL
CCF 642;CCF-642
CCF642 >=98% (HPLC)
CCF 642;CCF-642;AC1LYELL
3-(4-Methoxyphenyl)-5-[(5-nitro-2-thienyl)methylene]-2-thioxo-4-thiazolidinone
4-Thiazolidinone, 3-(4-methoxyphenyl)-5-[(5-nitro-2-thienyl)methylene]-2-thioxo- | [Molecular Formula]
C15H10N2O4S3 | [MDL Number]
MFCD01836919 | [MOL File]
346640-08-2.mol | [Molecular Weight]
378.45 |
| Chemical Properties | Back Directory | [Boiling point ]
567.3±60.0 °C(Predicted) | [density ]
1.60±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO:14.4(Max Conc. mg/mL);38.05(Max Conc. mM) | [form ]
powder | [pka]
-0.70±0.20(Predicted) | [color ]
yellow to orange |
| Hazard Information | Back Directory | [Uses]
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. | [Biochem/physiol Actions]
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. | [in vivo]
CCF642 (10 mg/kg；腹腔注射；每周 3 次；持续 24 天) 显著延长携带 5TGM1-luc 小鼠的寿命并抑制 5TGM1-luc 生长，如成像所确定[1]。
| Animal Model: | C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc[1] | | Dosage: | 10 mg/kg | | Administration: | i.p.; three times a week; for 24 days | | Result: | Significantly prolonged life of 5TGM1-luc–bearing mice and suppressed 5TGM1-luc growth as determined by life imaging.
|
| [storage]
Store at -20°C |
|
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Twochem Co.Ltd.
|
| Telephone: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
Henan Alfachem Co.,Ltd.
|
| Telephone: |
0371-55051623 18137891487 |
| Website: |
www.chemicalbook.com/supplier/14555231/ |
|