2. Signaling Pathways
  3. Neuronal Signaling
  4. Choline Kinase

Choline Kinase

Choline Kinase; CK; ChoK; choline phosphokinase

Choline kinase (also known as CK, ChoK and choline phosphokinase) is an enzyme which catalyzes the first reaction in the choline pathway for phosphatidylcholine (PC) biosynthesis. Phosphatidylcholine (PC) is synthesized through the Kennedy pathway. In the initial step, choline is converted to phosphocholine by Choline Kinase in a reaction catalyzed by one of two enzymatic forms: choline kinase α (CHKα) and choline kinase β (CHKβ). The CHKA gene produces two proteins, CHKα1 and CHKα2, through alternative splicing. All isoforms of choline kinases catalyze the same biochemical reaction: the formation of phosphocholine. CHKα and CHKβ form homodimers and heterodimers. The expression and activity of Choline Kinases are regulated during transcription, at the mRNA level and by post-translational modification. CHKα expression is directly regulated by miR-367-3p11 and miR-876-5p. Choline kinase activity can be regulated by various proteins acting on CHKα or CHKβ. Choline kinase activity can also be regulated by changes in CHKα protein stability. Choline kinase plays an important role in various tumor types[1].

Choline Kinase Isoform Specific Products:

Choline Kinase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101144
    RSM-932A
    		Inhibitor 98.77%
    RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
    RSM-932A
  • HY-120337
    V-11-0711
    		Inhibitor 98.54%
    V-11-0711 is a potent and selective Chk-α (IC50 = 20 nM) inhibitor. V-11-0711 can significantly reduce PCho levels. V-11-0711 causes a reversible growth arrest. V-11-0711 induces apoptosis at high concentrations. V-11-0711 can be used for the study of cervical cancer and triple-negative breast cancer.
    V-11-0711
  • HY-170805
    UNC0737
    		Inhibitor 98.04%
    UNC0737 is an orthosteric choline kinase inhibitor. UNC0737 is also a poor inhibitor of G9a (IC50 = 5000 nM) and GLP (IC50 > 10000 nM) in the SAHH-coupled assays.
    UNC0737
  • HY-122675
    ACG416B
    		Inhibitor 98.99%
    ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell.
    ACG416B
  • HY-120337B
    cis-V-11-0711
    		Inhibitor
    cis-V-11-0711 is the cis form of V-11-0711 (HY-120337). V-11-0711 is a potent and selective Chk-α (IC50 = 20 nM) inhibitor. V-11-0711 can significantly reduce PCho levels. V-11-0711 causes a reversible growth arrest. V-11-0711 induces apoptosis at high concentrations. V-11-0711 can be used for the study of cervical cancer and triple-negative breast cancer.
    cis-V-11-0711
  • HY-120337A
    V-11-0711 hydrochloride
    		Inhibitor
    V-11-0711 hydrochloride is a potent and selective Chk-α (IC50 = 20 nM) inhibitor. V-11-0711 hydrochloride can significantly reduce PCho levels. V-11-0711 hydrochloride causes a reversible growth arrest. V-11-0711 induces apoptosis at high concentrations. V-11-0711 hydrochloride can be used for the study of cervical cancer and triple-negative breast cancer.
    V-11-0711 hydrochloride
  • HY-101145
    CK37
    		Inhibitor
    CK37 is a competitive choline kinase-α inhibitor. CK37 inhibits purified recombinant human choline kinase-α activity. CK37 suppresses MAPK and PI3K/AKT signaling, disrupts actin cytoskeletal organization. CK37 diminishs activating phosphorylations of ERK. CK37 exhibits anticancer activity against cervical cancer, melanoma, Lewis lung carcinoma, lung adenocarcinoma, breast cancer, and leukemia.
    CK37
  • HY-162799
    ChoKα inhibitor-6
    		Inhibitor
    ChoKα inhibitor-6 (compound Fa22) is a less specific ChoKα1 inhibitor with antitumor activity.
    ChoKα inhibitor-6
  • HY-112477
    Chk2-IN-1
    Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect.
    Chk2-IN-1
  • HY-123612
    JAS239
    		Inhibitor
    JAS239 is a blood-brain barrier-permeable ChoK inhibitor. JAS239 inhibits phosphocholine synthesis and reduces the expression level of E2F1 protein. JAS239 exhibits near-infrared fluorescence properties. JAS239 exerts anti-tumor activity against glioblastoma. JAS239 can be used in studies related to glioblastoma.
    JAS239
  • HY-101144R
    RSM-932A (Standard)
    		Inhibitor
    RSM-932A (Standard) is the analytical standard of RSM-932A (HY-101144). This product is intended for research and analytical applications. RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
    RSM-932A (Standard)
  • HY-114081A
    Hemicholinium chloride
    		Inhibitor
    Hemicholinium chloride (HC-3) is a choline kinase (ChoK) inhibitor. Hemicholinium chloride Hemicholinium chloride induces ataxia and muscular weakness.
    Hemicholinium chloride
Choline Kinase Isoform Comparison

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