Home ER stress & UPR IRE1 inhibitor MKC-3946 For research use only.

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.

MKC-3946 Chemical Structure

MKC-3946 Chemical Structure

CAS: 1093119-54-0

Selleck's MKC-3946 has been cited by 4 publications

Purity & Quality Control

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

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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
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].
Cell Research 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.
In Vivo
In vivo MKC-3946 inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition of MM cells[1].
Animal Research Animal Models CB17 SCID mice
Dosages 100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 380.46 Formula

C21H20N2O3S
CAS No. 1093119-54-0 SDF Download MKC-3946 SDF
Smiles CN1CCN(CC1)C(=O)C2=CC=C(S2)C3=CC4=C(C=C3)C(=C(C=C4)O)C=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 38 mg/mL ( (99.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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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