CCF642

CCF642

Application

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.

Packaging

5, 25 mg in glass bottle

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575430 CCF642 yellow to orange 100 SIGMA-ALDRICH 2-8°C
£536.25 (exc VAT) per 25MG
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3575431 CCF642 yellow to orange 100 SIGMA-ALDRICH 2-8°C
£131.76 (exc VAT) per 5MG
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