Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.6284 mL
13.1420 mL
26.2840 mL
5 mM
0.5257 mL
2.6284 mL
5.2568 mL
10 mM
0.2628 mL
1.3142 mL
2.6284 mL
50 mM
0.0526 mL
0.2628 mL
0.5257 mL
Description
MKC3946 is a potent and soluble inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells.
MKC-3946 triggers modest growth inhibition in MM cell lines, without toxicity in normal mononuclear cells. Importantly, it significantly enhances cytotoxicity induced by bortezomib or 17-AAG, even in the presence of bone marrow stromal cells or exogenous IL-6. Both bortezomib and 17-AAG induce ER stress, evidenced by induction of XBP1s, which is blocked by MKC-3946. Apoptosis induced by these agents is enhanced by MKC-3946, associated with increased CHOP. MKC-3946 treatment does not inhibit IRE1α kinase function or binding of activated IRE1α to TRAF2 and downstream JNK signaling.
In vivo
MKC-3946 inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition of MM cells.
