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A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ; demonstrates potent in vitro antiproliferative (HT29 IC50=1.15 uM) and in vivo antitumoral activity against human xenografts in mice with low toxicity profiles.
CK-37 (ChoK-α inhibitor CK37) is 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.
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.
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;
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.
JCR 795b(JCR795b;JCR-795b) is a competitive, small molecule inhibitor of choline kinase (ChoK) with in vitro IC50 of 3.5 uM.
MN58b(MN-58b;MN 58b) 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.
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