中文名：MKC-3946
英文名：MKC-3946
英文別名：1-?Naphthalenecarboxald?ehyde,2-?hydroxy-?6-?[5-?[(4-?methyl-?1-?piperazinyl)?carbonyl]?-?2-?thienyl]?-
純度：99%
貨號：M413961
包裝：25mg、2mg、5mg
Cas號：1093119-54-0
存儲(chǔ)溫度：-20°C儲(chǔ)存
產(chǎn)品介紹：
Information
MKC-3946 MKC3946 is a potent and soluble IRE1α endoribonuclease domain inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells.
Targets
IRE1α endoribonuclease
In vitro
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 associated with significant growth inhibition of MM cells.
Cell Research(from reference)
Cell lines：RPMI 8226 cells?
Concentrations：2.5, 5, 10 μM?
Incubation Time：3 hours?
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關(guān)鍵字： 1-?Naphthalenecarboxald?ehyde,2-?hydroxy-?6-?[5-?[(4-?methyl-?1-?piperazinyl)?carbonyl]?-?2-?thienyl]?-
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