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MKC9989 Catalog No.GC32910

Size Price Stock Qty
10mM*1mLinDMSO
$225.00
In stock
1mg
$101.00
In stock
5mg
$304.00
In stock
10mg
$459.00
In stock
50mg
$1,379.00
In stock
100mg
$1,930.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Cell experiment:

Human RPMI 8226 plasmacytoma cells are grown in monolayer culture using medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37°C and 5% CO2. MKC9989 is prepared as 10 mM stocks in DMSO, stored at -20°C, and diluted in medium. Thapsigargin (Tg) is resuspended in DMSO and diluted in medium. Cells are grown to 50% confluency, treated with 1 μM Tg and/or 10 μM MKC9989 at the indicated time points. After incubation of cells for the indicated periods, cells are harvested[1].

References:

[1]. Sanches M, et al. Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors. Nat Commun. 2014 Aug 28;5:4202.

Chemical Properties

Cas No. 1338934-20-5 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES O=CC1=C(O2)C(C(C)=C(CCOCCOC)C2=O)=CC(OC)=C1O
Formula C17H20O7 M.Wt 336.34
Solubility DMSO : ≥ 50 mg/mL (148.66 mM);H2O : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.

At 10 μM concentration, MKC9989 completely inhibits both basal and thapsigargin induced splicing of XBP1 mRNA. These effects are observed even in cells pre-treated with thapsigargin, indicating that MKC9989 can fully reverse the onset of XPB1 splicing after the UPR is initiated. In parallel analysis, MKC9989, significantly stabilizes the RIDD target CD59 mRNA when co-administered with thapsigargin relative to thapsigargin treatment alone and modestly increases levels of CD59 mRNA in non-stressed cells, the latter likely reflects the inhibition of baseline RIDD activity. In contrast to effects on XBP1 splicing, MKC9989 moderately stabilizes CD59 levels when administered 2 hour post treatment with thapsigargin. Finally, the potency of MKC9989 against the splicing of XBP1 mRNA (EC50=0.33 μM) is comparable to its potency against RNA cleavage in vitro[1].

[1]. Sanches M, et al. Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors. Nat Commun. 2014 Aug 28;5:4202.