A PDI inhibitor; inhibits the reducing capacity of PDI at 1 µM; inhibits proliferation in ten multiple myeloma cell lines (IC50s = 50 =

CCF-642 – 5 mg

Brand:
Cayman
CAS:
346640-08-2
Storage:
-20
UN-No:
Non-Hazardous - /

CCF-642 is an inhibitor of protein disulfide isomerase (PDI).{48409} It inhibits the reducing capacity of PDI when used at a concentration of 1 µM. It inhibits proliferation in ten multiple myeloma cell lines with IC50 values of less than 1 µM. It is cytotoxic to primary cells isolated from patients with refractory myeloma who developed secondary plasma cell leukemia (IC50 = <1 µM) but not to normal bone marrow mononuclear (NLBM) cells up to a concentration of 6.75 µM. CCF-642 (3 µM) also induces acute endoplasmic reticulum (ER) stress, increasing ERK phosphorylation and dimerization of IRE1-α, indicating an increase in the amount of misfolded ER proteins. It increases calcium accumulation and cleaved caspase-3 in MM1.S cells and induces apoptosis. CCF-642 increases survival in a 5TGM1 mouse syngeneic model of myeloma when administered at a dose of 10 mg/kg three times per week.  

 

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SKU: 27054 - 5 mg Category:

Description

A PDI inhibitor; inhibits the reducing capacity of PDI at 1 µM; inhibits proliferation in ten multiple myeloma cell lines (IC50s = 50 = <1 µM) but not to NLBM cells up to 6.75 µM; induces acute ER stress and increases the amount of misfolded ER proteins; increases survival in a 5TGM1 mouse syngeneic model of myeloma at 10 mg/kg three times per week

Formal name: 3-(4-methoxyphenyl)-5-[(5-nitro-2-thienyl)methylene]-2-thioxo-4-thiazolidinone

Synonyms: 

Molecular weight: 378.4

CAS: 346640-08-2

Purity: ≥98% (mixture of isomers)

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis

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