A selective inhibitor of CHOKα
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RSM-932A

Item No. 21518

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,1'-[[[1,1'-biphenyl]-4,4'-diyl]bis(methylene)]bis[4-[(4-chlorophenyl)methylamino]-quinolinium, dibromide
CAS Number
850807-63-5
Molecular Formula
C46H38Cl2N4 • 2Br
Formula Weight
877.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 3 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml
λmax
233, 255, 364 nm
SMILES
ClC1=CC=C(N(C2=CC=[N+](CC3=CC=C(C4=CC=C(C[N+]5=C(C=CC=C6)C6=C(N(C7=CC=C(Cl)C=C7)C)C=C5)C=C4)C=C3)C8=C2C=CC=C8)C)C=C1.[Br-].[Br-]
InChi Code
InChI=1S/C46H38Cl2N4.2BrH/c1-49(39-23-19-37(47)20-24-39)43-27-29-51(45-9-5-3-7-41(43)45)31-33-11-15-35(16-12-33)36-17-13-34(14-18-36)32-52-30-28-44(42-8-4-6-10-46(42)52)50(2)40-25-21-38(48)22-26-40;;/h3-30H,31-32H2,1-2H3;2*1H/q+2;;/p-2
InChi Key
DGBVSSXGHKAASQ-UHFFFAOYSA-L
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    RSM-932A is a selective inhibitor of choline kinase α (CHOKα; IC50s = 1 and >50 μM for CHOKα and β, respectively).1 It induces apoptosis via CHOP signaling and endoplasmic reticulum (ER) stress in MDA-MB-231, MCF-7, SW620, and H460 cancer cells, but it only induces cell cycle arrest and not apoptosis in NCM460 and MCF-10A normal epithelial cells.2 RSM-932A inhibits the growth of HT-29 colon cancer cells in vitro (IC50 = 1.15 μM) and in vivo in a mouse xenograft model (ED50 = 7.5 mg/kg).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lacal, J.C., and Campos, J.M. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol. Cancer Ther. 14(1), 31-39 (2015).

    2. Sanchez-Lopez, E., Zimmerman, T., Gomez del Pulgar, T., et al. Choline kinase inhibition induces exacerbated endoplasmic reticulum stress and triggers apoptosis via CHOP in cancer cells. Cell Death Dis. 4(11), e933 (2013).