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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.

Cat. No. Product Name CAS No. Information
PC-60876

JCR 795b

203190-49-2

JCR 795b is a competitive, small molecule inhibitor of choline kinase (ChoK) with in vitro IC50 of 3.5 uM.

PC-60867

Hemicholinium-3

16478-59-4

Hemicholinium-3 (HC-3) is a competitive, small molecule inhibitor of choline kinase (ChoK) with ex vivo IC50 of 500 uM, also bolcks the sodium and chloride-dependent transport system and affects choline acetyltransferase;

PC-60866

MN58b

203192-01-2

MN58b is a potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.4 uM, >30-fold selectivity over ChoKβ and does not affect MAPKs, PI3Ks, and other enzymes involved in the regulation of phospholipid metabolism; demonstrates antiproliferative properties against human tumor-derived cell lines (HT29 IC50=0.5 uM) and antitumor activity against human tumor xenografts in vivo.

PC-60865

JAS239

1630288-74-2

JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly, prevents choline phosphorylation and induces cell death in breast cancer cell lines; inhibits the phosphorylation of 14C-labeled choline in MDA-MB-231 triple-negative breast cancer cells with IC50 of 4.6 uM, significant reduces MDA-MB-231 viability with IC50 of 13.3 uM; a NIR-fluorescent ChoK inhibitor.

PC-35395

EB-3D

1839150-63-8 EB-3D is a novel potent and selective choline kinase ChoKα inhibitor with IC50 of 1.0 uM (purified ChoKα1), strongly impairs cell proliferation in a variety of different cancer cell lines; demonstrates in vitro antiproliferative effects against HeLa (IC50=79 nM), RS4,11 (IC50=45 nM), A549 (IC50=27 nM) and MDA-MB-231 (IC50=100 nM); displays excellent antiproliferative activity against a wide cohort of T-leukemic cell lines with GI50 of 0.9 nM (MOLT-16 cell)-479 nM (CCRF-CEM), reduces the intracellular pool of PCho, but also inhibits the synthesis of choline-containing lipids; induces G0/G1 arrest that lead to apoptosis in leukemia cell lines; affects AMPK-mTOR signaling pathway, synergizes with both dexamethasone and L-asparaginase.
PC-61516

CK-37

1001478-90-5 A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM cells to a slight increase in p62; suppresses MAPK and PI3K/AKT signaling, disrupts actin cytoskeletal organization, and reduces plasma membrane ruffling; significantly decreases tumor growth in a lung tumor xenograft mouse model, suppresses tumor phosphocholine, and diminishes activating phosphorylations of ERK and AKT in vivo.
PC-60877

ACG-416B

95316-15-3 A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.13 uM, >385-fold selectivity over ChoKβ; demonstrates in vitro antiproliferative activity against HT29 cells with IC50 of 1.94 uM.

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