Choline Kinase Inhibitor

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.

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.

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.

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.

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.

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.

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.

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.

ChoKα inhibitor-6 (compound Fa22) is a less specific ChoKα1 inhibitor with antitumor activity.

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.

Hemicholinium chloride (HC-3) is a choline kinase (ChoK) inhibitor. Hemicholinium chloride Hemicholinium chloride induces ataxia and muscular weakness.