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Cat. No. Product Name CAS No. Information
PC-63366

ETC-206

1464151-33-4

ETC-206 (ETC-1907206) is a novel potent, selective MNK1/2 inhibitor with IC50 of 64/86 nM, inhibits eIF4E phosphorylation inhibition in HeLa cell line with IC50 of 321 nM; displays excellent kinase selectivity, inhibits only 2 kinases by >65% at 1 uM against a panel of 104 kinases; demonstrates potent anti-proliferative activity against 25 hematological cancer cell lines with submicromolar IC50, especially against GK-5, DOHH2, AHH1 and P3HR-1 cell lines; prevents BC CML LSC self-renewal in vitro, significantly enhances the anti-tumor activity of dasatinib in BC CML mouse xenograft model.

Blood Cancer

Phase 1 Clinical

PC-61145

MNK inhibitor 9

1889336-59-7

MNK inhibitor 9 is a potent, selective MAPK-interacting kinase (MNK1 and MNK2) inhibitor with IC50 of 3 nM for both, with no activity aginst CDK1/2 (IC50>25 uM); displays excellent selectivity against a 53 kinase panel, with 4 kinases with IC50 <1 uM; inhibits eIF4E phosphorylation in KMS11-luc myeloma with IC50 of 0.6 nM, exhibits inhibition of cell proliferation in human multiple myeloma tumor cell line with EC50 of 1.7 uM; has good solubility and permeability, and is a suitable in vivo tool compound.

PC-42035

eFT508

1849590-01-7

eFT508 (Tomivosertib) is a potent, highly selective, reversible, ATP-competitive, and orally bioavailable MNK1 and MNK2 inhibitor with IC50 of 1-2 nM in enzyme assays; dose-dependently reduces eIF4E phosphorylation at Serine 209 in tumor cell lines with IC50 of 2-16 nM; shows anti-proliferative activity against multiple DLBCL cell lines, decreases the production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10; demonstrates significant anti-tumor activity in human lymphoma xenograft models which harbor activating MyD88 mutations.

Blood Cancer

Phase 2 Clinical

PC-63078

MNKI-19

1211757-83-3 MNKI-19 is a potent and dual-specific Mnk inhibitor with Ki of 186 nM and 68 nM for Mnk1 and Mnk2, respectively; only displays moderate activity against Pim-1 (Ki=2.35 uM) in a panel of upstream activating kinases of Mnks, including B-Raf, MAPK1, MAPK2, Akt1, PI3K, p38α, and mTOR; inhibits the phosphorylation of eIF4E and 4E-BP1, arrests cancer cells in the G1 phase and induce apoptosis in FLT3-ITD expressed AML cells.
PC-63077

MNKI-85

1812885-57-6 MNKI-85 is a potent and selective Mnk2 inhibitor with Ki of 31 nM, displays no inhibitory activities against Mnk1, CDK2A, CDK9T, and CDK4D; effectively inhibits the growth of AML cells that possess an M5 subtype with FLT3-internal tandem duplication mutation, a powerful pharmacologic tool in studying the Mnk2/eIF4E-mediated tumorigenic mechanism.
PC-63076

QL-X-138

1469988-63-3 QL-X-138 is a selective and potent BTK/MNK dual kinase inhibitor with IC50 of 8, 107.4, and 26 nM for BTK, MNK1, and MNK2, respectively; exhibits covalent binding to BTK and noncovalent binding to MNK; enhances the antiproliferative efficacies in vitro against a variety of B-cell cancer cell lines, as well as AML and CLL primary patient cells; arrests cell cycle progression and strongly induces apoptosis.
PC-63075

MNK-IN-54

1613168-64-1 MNK-IN-54 is a potent, orally bioavailable dual MNK1/2 and BCR-ABL1 inhibitor with IC50 of 20/10/200/10 nM for Abl T315I/ wt Abl/MNK1/MNK2, respectively; also inhibits RET, FLT3, VEGFR2 with IC50 <20 nM; shows GI50 of 51 nM in the growth of K562 cells overexpressing eIF4E; exhibits antitumor activity in a mouse xenograft model and also reduces the level of phosphorylated eukaryotic translation initiation factor 4E in the tumor tissues.

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