An inhibitor of IRE1α
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MKC-3946

Item No. 19152

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-hydroxy-6-[5-[(4-methyl-1-piperazinyl)carbonyl]-2-thienyl]-1-naphthalenecarboxaldehyde
CAS Number
1093119-54-0
Molecular Formula
C21H20N2O3S
Formula Weight
380.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:6): 0.14 mg/mlDMSO: 14 mg/ml
λmax
226, 316 nm
SMILES
O=C([H])C1=C2C(C=C(C3=CC=C(C(N4CCN(C)CC4)=O)S3)C=C2)=CC=C1O
InChi Code
InChI=1S/C21H20N2O3S/c1-22-8-10-23(11-9-22)21(26)20-7-6-19(27-20)15-2-4-16-14(12-15)3-5-18(25)17(16)13-24/h2-7,12-13,25H,8-11H2,1H3
InChi Key
IVQVBMWPWPTSNO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $62

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    5 mg

    $266

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    10 mg

    $472

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    25 mg

    $1,030

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    Product Description

    MKC-3946 is an inhibitor of inositol-requiring enzyme 1α (IRE1α).1 It inhibits basal XBP1 splicing, a marker of IRE1α activity, in RPMI 8226 multiple myeloma cells in a concentration-dependent manner. MKC-3946 also inhibits XBP1 splicing induced by endoplasmic reticulum (ER) stress and reduces expression of the XBP1 target genes SEC61A1, p58IPK, and ERdj4 in RPMI 8226 cells. In vitro, it is cytotoxic to multiple myeloma cell lines but has no effect on normal mononuclear cells. In vivo, MKC-3946 (100 mg/kg) reduces tumor growth and XBP1 splicing in an RPMI 8226 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mimura, N., Fulciniti, M., Gorgun, G., et al. Blockade of XBP1 splicing by inhibition of IRE1α is a promising therapeutic option in multiple myeloma. Blood 119(24), 5772-5781 (2012).