1. Others Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage
  2. Drug Derivative Interleukin Related TNF Receptor Polo-like Kinase (PLK)
  3. Salicylate choline

Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer.

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Salicylate choline

Salicylate choline Chemical Structure

CAS No. : 2016-36-6

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Description

Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer[1][2][3][4].

In Vitro

Salicylate choline (24 h) significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in HGF-1 cells[1].
Salicylate choline (2-3 mM, 48-72 h) combined with Selinexor (KPT-330) (HY-17536) exhibits potent anti-proliferative activity against hematologic malignancy cells including MCL (JeKo-1, Mino), TCL (SR-786, Karpas-299), DLBCL (OCI-Ly1, OCI-Ly3, OCI-Ly19, SU-DHL-6, RPMI), MM (U266, OPM2, Xg1, KMS2), WM (BCWM, MWCL), ALL (RPCI, CRL-1783) and solid tumor cells including pancreatic cancer (Panc-1, L3.6pl), non-small cell lung cancer (H460, A549, HCC827), small-cell lung cancer (H1048), sarcoma (FuJi, SW872), breast cancer (Hs 578T, BT-474, BT-20, MCF7)[4].
Salicylate choline (3 mM, 24 h) combined with Selinexor significantly downregulates Rad51 and thymidylate synthase (TYMS) expression and increases γ-H2AX (DNA damage marker) levels in JeKo-1 cells[4].
Salicylate choline (3 mM, 24-48 h) combined with Selinexor significantly suppresses G2/M phase-related proteins (PLK1, Bub1b, Aurora A) expression in OCI-Ly1 cells (DLBCL) after release from double-thymidine block[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[4]

Cell Line: OCI-Ly1 cells
Concentration: 3 mM combined with Selinexor
Incubation Time: 24, 36, 48 h
Result: Suppressed G2/M phase-related proteins (PLK1, Bub1b, Aurora A) expression in OCI-Ly1 cells.
In Vivo

Salicylate choline (500 mg/kg, p.o., consecutively 6 days per week, 26 days) combined with Selinexor demonstrates excellent anti-tumor efficacy in male mice xenograft model harboring JeKo-1 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: JeKo-1 cells (5 × 106) were subcutaneously implanted into the flanks of 4-6 weeks old male NSG mice[4]
Dosage: 500 mg/kg combined with Selinexor (15 mg/kg, p.o., twice weekly, 26 days)
Administration: p.o., consecutively 6 days per week, 26 days
Result: Achieved significant tumor growth inhibition.
Showed no significant changes in body weight.
Molecular Weight

241.28

Formula

C12H19NO4

CAS No.
SMILES

O=C(O)C1=CC=CC=C1[O-].C[N+](C)(CCO)C

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Salicylate choline
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HY-W338346
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