MKC-3946

Catalog No.S8286

For research use only.

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 Chemical Structure

CAS No. 1093119-54-0

Purity & Quality Control

Choose Selective IRE1 Inhibitors

Biological Activity

Description 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 [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 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[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].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: RPMI 8226 cells
  • Concentrations: 2.5, 5, 10 μM
  • Incubation Time: 3 hours
  • Method:

    RPMI 8226 cells are treated with or without Tm (5 μg/mL) in combination with MKC-3946 (0-10μM) for 3 hours. Total RNA is extracted; XBP1 and β-actin mRNA are evaluated by RT-PCR.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: CB17 SCID mice
  • Dosages: 100 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 38 mg/mL
(99.87 mM)
Ethanol 3 mg/mL
(7.88 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.46
Formula

C21H20N2O3S

CAS No. 1093119-54-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C(=O)C2=CC=C(S2)C3=CC4=C(C=C3)C(=C(C=C4)O)C=O

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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