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Cat. No. Product Name CAS No. Information
PC-43380

Cobimetinib R-enantiomer

934660-94-3

Cobimetinib R-enantiomer (GDC-0973; XL518) is the R-enantiomer of Cobimetinib (GDC-0973; XL518), which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2).

PC-43369

Cobimetinib

934660-93-2

Cobimetinib (GDC-0973, XL-518) is a potent, selective MEK inhibitor with IC50 of 4.2 nM for MEK1; shows excellent selectivity against mTOR, DNA-dependent protein kinase (DNA-PK), and a panel of more than 228 kinases; shows strong cellular potency in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines, triggers robust apoptosis and tumor growth inhibition in vivo combined with PI3K inhibitor GDC-0941.

Skin Cancer

Approved

PC-62664

Vacquinol-1

5428-80-8

Vacquinol-1 (NSC 13316) is a MKK4 (MAP2K4, MEK4) activator that induces vacuolization, induces ATP depletion in glioblastoma cells (IC50 = 3.14 uM) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells; induces rapid and specific cell death of glioma cells via membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture; shows good brain penetrance and excellent pharmacokinetics; orally bioactive.

PC-35805

MKK7-COV-9

MKK7-COV-9 (MKK7 Covalen inhibitor 9) is a potent, selective, covalent MKK7 inhibitor, displays >1,000-fold selectivity over MKK4; displays remarkable selectivity against a kinome panel of 76 kinases; inhibits the CD86+ response in primary mouse B cells in response to LPS stimulation (EC50=4.9 uM); has half-lives >40 min in dog and rat, and significantly improved stability in human and monkey liver microsomes; MKK7-COV-9 is not cytotoxic to a panel of human cell lines.
PC-35804

MKK7-COV-13

MKK7-COV-13 (MKK7 Covalen inhibitor 13) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 10 nM, displays >1,000-fold selectivity over MKK4 (IC50>10 uM); shows EC50 of 0.3-1.0 uM for reduction of p-JNK in HEK293 cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases; inhibits the CD86+ response in primary mouse B cells in response to LPS stimulation.
PC-35803

MKK7-COV-3

MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases, with very few kinases inhibited by more than 75% at 1 uM: Aurora kinase B, LRRK2, and MKK4, as well as FLT3; inhibits 60% of the CD86+ response in primary mouse B cells in response to LPS stimulation (10 μM, 2 hr pre-incubation).
PC-43541

TAK-733

1035555-63-5 TAK-733 (TAK733,TAK 733) is a potent, selective, allosteric inhibitor of MEK with IC50 of 3.2 nM (MEK1); shows selectivity for MEK1 over a panel of 18 kinases, receptors, and ion channels at uM; inhibits ERK phosphorylation in vitro with EC50 of 1.9 nM, also inhibits proliferation of A375 and COLO 205 cells with IC50 of 3.1 nM and 2.1 nM, respectively; as well as 14 cutaneous melanoma cell lines (IC50s=<1-10 nM), espectially in those with B-RAFV600E mutations; demonstrates antitumor activity in multiple mouse xenograft models.

Solid Tumors

Phase 1 Discontinued

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