Home ER stress & UPR IRE1 inhibitor MKC-3946

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MKC-3946 IRE1 inhibitor

Cat.No.S8286

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.
MKC-3946 IRE1 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 380.46

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Quality Control

Batch: S828601 DMSO]38 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.89%
99.89

Chemical Information, Storage & Stability

Molecular Weight 380.46 Formula

C21H20N2O3S

 Storage (From the date of receipt)
CAS No. 1093119-54-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1CCN(CC1)C(=O)C2=CC=C(S2)C3=CC4=C(C=C3)C(=C(C=C4)O)C=O

Solubility

In vitro
Batch:

DMSO : 38 mg/mL (99.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
IRE1α endoribonuclease [1]
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 this compound. Apoptosis induced by these agents is enhanced by this chemical, associated with increased CHOP. This compound treatment does not inhibit IRE1α kinase function or binding of activated IRE1α to TRAF2 and downstream JNK signaling[1].
In vivo
MKC-3946 inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition of MM cells[1].
References

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